N S Hari Narayana Moorthy

Publications of N S Hari Narayana Moorthy

• QSAR and Pharmacophore Analysis of a series of Piperidinyl Urea Derivatives as hERG Blockers and H3 Antagonists.

  Authors: N S Hari Narayana Moorthy, Maria J Ramos, Pedro A Fernandes

  Current drug discovery technologies. 05/2012;

  In the present study, a computational based pharmacophore and structural analysis were performed on a series of piperidinyl urea derivatives, a limited number of compounds which have variation inIn the present study, a computational based pharmacophore and structural analysis were performed on a series of piperidinyl urea derivatives, a limited number of compounds which have variation in structure and activities that exhibit hERG blocking and H3 antagonistic activities. The conducted QSAR studies demonstrated that the developed models are statistically significant, which have been confirmed through validation. The Q2 values for the models developed with hERG blocking activity are >0.8 and with the H3 antagonistic activity are >0.6. The descriptors contributed in the models show that the distributed polar properties on the vdW surface of the molecules are important for the hERG blocking activity. The vsurf_ descriptors (surface area, volume and shape) such as vsurf_DD13 and vsurf_Wp4 correlate with the H3 antagonistic activity of these compounds. The distances between the pharmacophore sites were measured in order to confirm their significance to the activities. The results reveal that the acceptor (acc), donor (don), hydrophobic (hyd) and aromatic/hydrophobic (aro/hyd) pharmacophore properties are favorable contours sites for both the activities. Also, our study reveals that the distance between the polar contours (acc, don, etc) has to be small for better hERG blocking activity. The distances between the aro/hyd to the polar groups should be higher for better hERG blocking activity. However, the H3 antagonistic activity for these series depends upon hydrophobic property of the molecules, particularly the hyd and the hyd/aro contours of the molecules. Hence, these results reveal the requirements on the structural properties and the distances between the pharmacophore contour sites of the molecules responsible for their hERG and H3 antagonistic activities.

• Analysis of the α-glucosidase inhibitory activity of chromenone derivatives based on their molecular features: a computational study.

  Authors: N S Hari Narayana Moorthy, Maria J Ramos, Pedro A Fernandes

  Medicinal chemistry (Shāriqah (United Arab Emirates)). 11/2011; 7(6):526-33.

  α-Glucosidase is one of the important enzymes in glucose digestion and its inhibitors are known to possess a large number of therapeutic effects. In this present investigation, we have performedα-Glucosidase is one of the important enzymes in glucose digestion and its inhibitors are known to possess a large number of therapeutic effects. In this present investigation, we have performed structural feature analysis of some of these inhibitors namely, chromenone derivatives using the Molecular Operating Environment (MOE) software. The results of the QSAR study show that the derived models are statistically significant and were validated by external (test set) and internal (leave one out) methods. The crossvalidated correlation coefficients (Q2) of the models show that the training and test sets have the values > 0.6687. The physicochemical descriptors contributed for the models building in training set and complete data set show that the log of aqueous solubility (LogS) and the molar refractivity on the van der Waals surface area of the molecules (SMR_VSA4) positively contributed for the inhibitory activity. Further, the study also reveals that the polarizability and hydrogen bond acceptor/donor groups are important for the α-glucosidase inhibitory activity and these results are in agreement with the earlier studies obtained in our laboratory on α-glucosidase inhibitors which have shows that the polar surface area of the molecule is important for the interaction. The pharmacophore contours of the molecule also showed the importance of the polar surface property on the molecules. This computational analysis will help in the development of novel α-glucosidase inhibitors for various diseases.

• Comparative Structural Analysis of α-Glucosidase Inhibitors on Difference Species: A Computational Study.

  Authors: N S Hari Narayana Moorthy, Maria J Ramos, Pedro A Fernandes

  Archiv der Pharmazie. 10/2011;

  Structural feature analysis of chlorogenic acid derivatives made up of varying lengths of alkyl groups as α-glucosidases inhibitors were performed by QSAR techniques. The statistically significantStructural feature analysis of chlorogenic acid derivatives made up of varying lengths of alkyl groups as α-glucosidases inhibitors were performed by QSAR techniques. The statistically significant models derived from the study were validated by leave one out, Y-randomization and test set methods. The predictive capacity of the models was assessed by its validation parameters such as crossvalidated correlation coefficients (Q(2) ), predictive residual analysis and other correlation parameters. The results obtained from the study show that the models were constructed with vsurf like properties (vsurf_ID4, vsurf_ID7 and vsurf_CW8), partial charge (Q_VSA_FNEG) and conformation dependent charged (dipoleX) descriptors. The integy moments of hydrophobicity descriptors (ID4 and ID7) are contributed for the inhibitory activity of the α-glucosidases enzymes of both the species. The vsurf_ID7 descriptor has contributed significantly (negatively) for the inhibitory activity prediction of α-glucosidases enzymes of S. cerevisiae. The partial negative charge on the surface of the molecules is detrimental for the activity, which reveals that the active site of the enzymes may have negatively charged groups. The pharmacophore analysis results also confirm the presence of hydrophilic properties on the vdW surface of the molecules. These results explain that the active sites of α-glucosidase enzymes of both the species have the same environment for the interaction. The alkyl side chain on the molecules is important for the pharmacokinetic behavior of the molecules and reduces the interaction energy of the molecules with the water. Hence, these results will be useful for designing novel molecules with multiple activities.

• Structural analysis of structurally diverse α-glucosidase inhibitors for active site feature analysis.

  Authors: N S Hari Narayana Moorthy, Maria J Ramos, Pedro A Fernandes

  Journal of enzyme inhibition and medicinal chemistry. 09/2011;

  In the present investigation, a QSAR analysis on structurally diverse α-glucosidase inhibitors (andrographolide, chromenone, triazole derivatives) was performed and the developed models wereIn the present investigation, a QSAR analysis on structurally diverse α-glucosidase inhibitors (andrographolide, chromenone, triazole derivatives) was performed and the developed models were validated by various validation methods (LMO, LOO, LSO, bootstrapping, Y-randomization and test set). The statistical parameters calculated for the models show that the developed models are statistically significant and have predicted the activities with small residual errors. The crossvalidated correlation coefficient (Q(2)) values obtained from different validation methods show >0.7 for both the models. Other correlations coefficient statistical parameters (R(2)(pred) and R(2)(m)) show that the developed models are reliable and robust. The leave-series-out (LSO) results reveal that the developed models can predict the activity of new compounds and its crossvalidated correlation coefficients' values are comparable with the Q(2) values obtained from other validation methods. The descriptors contributed in the selected models are suggested that the lower/reduced polarizability on the vdW surface area of the molecules and the presence of flexible bonds allow the substituents/side chains in the molecules with free movement and with lesser stretching energy which are favourable for the α-glucosidase inhibitory activity. These results reveal that the developed models are statistically significant and can be used with other molecular modelling works for designing novel α-glucosidase inhibitors with multiple activities (HIV, diabetics, cancer, etc).

• In silico-based structural analysis of arylthiophene derivatives for FTase inhibitory activity, hERG, and other toxic effects.

  Authors: N S Hari Narayana Moorthy, Sergio F Sousa, Maria J Ramos, Pedro A Fernandes

  Journal of biomolecular screening. 08/2011; 16(9):1037-46.

  In the present investigation, the authors have performed an in silico-based analysis on a series of arylthiophene derivatives for the determination of their structural features responsible forIn the present investigation, the authors have performed an in silico-based analysis on a series of arylthiophene derivatives for the determination of their structural features responsible for farnesyltransferase (FTase) inhibitory activity, hERG blocking activity, and toxicity by quantitative structure-activity relationship and pharmacophore analysis techniques. The statistically significant models derived through multiple linear regression analysis were validated by different validation methods. The applicability of the descriptors contributed in the selected models show that the polar and polarizable properties on the van der Waals (vdW) surface area of the molecules are important for the FTase inhibitory and hERG blocking activities, while being detrimental for the toxicity of the molecules. It is interesting to note that the topological properties, molecular flexibility, and connectivity of the molecules are positively correlated to all the activities (FTase inhibition, hERG blocking, and toxicity). This implies that the flexibility of the molecules is the common feature for interaction in all targets, whereas the presence of polar groups on the molecular surface (vdW) is a determinant for the favorable (FTase inhibition) or unwanted effect (hERG blocking and toxicity) of the molecules. The pharmacophore analysis of the molecules demonstrated that the aromatic/hydrophobicity and polarizability features are important pharmacophore contours favorable for these activities.

• Synthesis, in silico metabolic and toxicity prediction of some novel imidazolinones derivatives as potent anticonvulsant agents.

  Authors: N S Hari Narayana Moorthy, Vipin Saxena, C Karthikeyan, Piyush Trivedi

  Journal of enzyme inhibition and medicinal chemistry. 06/2011; 27(2):201-7.

  A series of 1,2,4-trisubstituted 5-imidazolinone derivatives were synthesized by Erlenmeyer condensation of benzoylglycine (hippuric acid) with different aldehydes in the presence of sodium acetateA series of 1,2,4-trisubstituted 5-imidazolinone derivatives were synthesized by Erlenmeyer condensation of benzoylglycine (hippuric acid) with different aldehydes in the presence of sodium acetate and acetic anhydride. The derivatives of the compounds were prepared by condensation of some known sulpha drugs with 5-oxazolone derivatives. The anticonvulsant activity of the compounds was determined by the protection of pentylenetetrazole-induced convulsions that was ranged from 10 to 60%. The compounds with p-OCH(3), p-OH and o-Cl substitutions in the phenyl ring on 4(th) position of the imidazolinone ring exhibited good anticonvulsant activity. In silico metabolic and toxicity studies showed that all the compounds in the series are not likely to exhibit toxicity except the compounds IIIa, IIIb, VIa and VIb, that is predicted to show 29% mutagenicity and 53% irritation in comparison to the other compounds. The predicted lethal effect and hERG toxicity of the compounds showed that IIa, IVa, Va and Vb might be toxic at higher concentrations. The results successfully establish the synthesized imidazolinone derivatives as novel compounds with anticonvulsant properties, low predicted cardiotoxicity and lethal effects thus can be promising leads for further development as novel anticonvulsants.

• Structural feature study of benzofuran derivatives as farnesyltransferase inhibitors.

  Authors: N S Hari Narayana Moorthy, Sergio F Sousa, Maria J Ramos, Pedro A Fernandes

  Journal of enzyme inhibition and medicinal chemistry. 03/2011; 26(6):777-91.

  Ras proteins are small GTPases (G-proteins) that play a key role in cell growth and cell proliferation in the mitogen-activated protein kinase signal transduction pathway. Farnesylation is a criticalRas proteins are small GTPases (G-proteins) that play a key role in cell growth and cell proliferation in the mitogen-activated protein kinase signal transduction pathway. Farnesylation is a critical step for membrane binding and the biological function of G-proteins. In the present investigation, we have studied the structural features of some molecules that are acting on the farnesyltransferase (FTase) enzyme for the inhibition of the farnesylation step in G-proteins. The benzofuran derivatives have activity against FTase inhibition and antiproliferative activity on QG56 cell lines. The result obtained from the quantitative structure-activity relationship study of these compounds shows that the models have significant predictive power and stability, as shown by statistical parameters such as R(2), Q(2), R(2)(pred), R(2)(m), F-value, Durbin-Watson, variable inflation factor values, Mahalanobis, and Cook's distances. The contribution of each descriptor for the activities (β-coefficients) reveals that the P-VSA descriptors (van der Waals surface area descriptors) such as vsa_pol, vsa_acc and SMR_VSA3 are the major contributors for the activity, along with other descriptors such as the partition coefficient, the partial charge, the atom and bond count and the adjacency, and distance descriptors. Earlier study on the FTase enzyme in our laboratory reveals that the existence of positively-charged groups on the FTase active site is important for drug design. It is also showing that the presence of hydrogen bonding donor and acceptor groups, together with negatively charged substituents is critical for improved activity by this series of molecules. These results offer important clues for the development of novel FTase inhibitors.

• Prediction of the relationship between the structural features of andrographolide derivatives and α-glucosidase inhibitory activity: a quantitative structure-activity relationship (QSAR) study.

  Authors: N S Hari Narayana Moorthy, Maria J Ramos, Pedro A Fernandes

  Journal of enzyme inhibition and medicinal chemistry. 02/2011; 26(1):78-87.

  In order to predict the structural features responsible for α-glucosidase inhibitory activity, a quantitative structure-activity relationship (QSAR) analysis was performed on a series ofIn order to predict the structural features responsible for α-glucosidase inhibitory activity, a quantitative structure-activity relationship (QSAR) analysis was performed on a series of andrographolide derivatives. To determine the quantitative relationship for the statistically significant models in terms of r (>0.8), F (99%) and Q(2) (>0.71) values were selected. The promising results we obtained could be used to predict the structural requirements for the inhibition of α-glucosidase activity. The models developed included: subdivided surface area, adjacency, surface volume and shape, molecular orbital package (MOPAC) and partial charge descriptors and showed a high correlation with the inhibitory activity. The descriptors used revealed that a van der Waals (vdW) surface with significant polar volume is favourable to the activity. The positive effect of the shape descriptors; PM3-LUMO and vsurf_wp7 and the negative effect of GCUT_PEOE_2 indicated that the active site may contain some nucleophilic positions that could interact with the ligand and the hydrogen acceptor and/or donor groups for hydrogen bonding with inhibitors.

• Topological, hydrophobicity, and other descriptors on α-glucosidase inhibition: a QSAR study on xanthone derivatives.

  Authors: N S Hari Narayana Moorthy, Maria J Ramos, Pedro A Fernandes

  Journal of enzyme inhibition and medicinal chemistry. 02/2011; 26(6):755-66.

  Quantitative structure activity relationship analysis was performed on a series of xanthone derivatives to establish the structural features required for α-glucosidase inhibitory activity. TheQuantitative structure activity relationship analysis was performed on a series of xanthone derivatives to establish the structural features required for α-glucosidase inhibitory activity. The computational and statistical analysis was performed with V life MDS (Molecular Design Suite) and Statistica software. The selected models show significant predictive power, stability, and reliability in terms of cross-validated correlation coefficient (Q(2)(cv) > 0.74 and Q(2)(test) > 0.5) and other validation parameters. The results show that the SaaaC count, MMFF_6 and dipole moment are mainly contributed for the activity along with the hydrophobicity descriptors. It describes that heteroatoms (oxygen atom connected with carbon atom) in the molecules are favourable for α-glucosidase inhibitory activity. The E-state count descriptor suggests that when carbon atoms connected with three aromatic bonds and hydrogen or other atoms are favourable for the activity. The SAHA and SAMH descriptors show that the hydrophilic area in the molecule is important for the activity while high hydrophilicity is unfavourable for the activity. This study concluded that hydrophilic, polar and/or electron negative groups, which are responsible for hydrogen bonding and interaction with the enzyme for favourable activity.

• Synthesis of Some Coumarinyl Chalcones and their Antiproliferative Activity Against Breast Cancer Cell Lines

  Authors: Kuldeep Patel, Chandrabose Karthikeyan, Viswas Raja Solomon, N.S. Hari Narayana Moorthy, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora, Piyush Trivedi

  Letters in Drug Design &amp Discovery. 01/2011; 11(8):308.

  Abstract: A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7)Abstract: A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their antiproliferative activities. One of the compound 3i bearing methoxy substitutions at the R1, R2 and R3 positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells.

• Design, Synthesis and Biological Evaluation of Some Novel 3-Cinnamoyl-4-Hydroxy-2H-Chromen- 2- ones as Antimalarial Agents

  Authors: Kuldeep Patel, Karthikeyan Chandrabose, N.S. Hari Narayana Moorthy, Girdhar Singh Deora, Kapendra Sahu, Piyush Trivedi

  Medicinal Chemistry Research. 01/2011;

  A novel series of 3-cinnamoyl-4-hydroxy-2Hchromen-2-ones were designed, synthesized and screened for antiplasmodial activity. Eleven compounds of the series exhibited micromolar potency againstA novel series of 3-cinnamoyl-4-hydroxy-2Hchromen-2-ones were designed, synthesized and screened for antiplasmodial activity. Eleven compounds of the series exhibited micromolar potency against chloroquine sensitive and chloroquine resistant strains. The most potent compound 4-hydroxy-3-(3-(4-nitrophenyl) acryloyl) -2Hchromen- 2-one showed inhibitory potency (IC50) of 3.1 and 4 lg/ml against chloroquine sensitive and chloroquine resistant strains, respectively. A structure activity relationship study was performed by correlating the effect of substituents with the antimalarial activity of the title compounds. The novel 3-cinnamoyl-4-hydroxy-2H-chromen- 2-ones reported here should be good lead for further development of antimalarial agents that can overcome resistance.

• Coumarinyl Chalcones and their Antiproliferative Activity Against Breast Cancer Cell Lines

  Authors: Kuldeep Patel, Chandrabose Karthikeyan, Viswas Raja Solomon, N. S. Hari Narayana Moorthy, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora, Piyush Trivedi

  Letters in Drug Design &amp Discovery. 01/2011; 8:308.

  A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and oneA series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their antiproliferative activities. One of the compound 3i bearing methoxy substitutions at the R1, R2 and R3 positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells.

• Synthesis of Some Coumarinyl Chalcones and their Antiproliferative Activity against Breast Cancer Cell Lines

  Authors: Kuldeep Patel, Chandrabose Karthikeyan, Viswas Raja Solomon, N.S. Hari Narayana Moorthy, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora, Piyush Trivedi

  Letters in Drug Design & Discovery. 01/2011; 8:323-327.

• Synthesis of Some Coumarinyl Chalcones and their Antiproliferative Activity Against Breast Cancer Cell Lines

  Authors: Kuldeep Patel, Chandrabose Karthikeyan, Viswas Raja Solomon, N.S. Hari Narayana Moorthy, Moorthy, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora, Piyush Trivedi

  Letters in Drug Design & Discovery. 01/2011; 8:308-311.

  A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and oneA series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their anti-proliferative activities. One of the compound 3i bearing methoxy substitutions at the R1, R2 and R3 positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells.

• Modeling VEGFR kinase inhibition of aminopyrazolopyridine urea derivatives using topological and physicochemical descriptors: a quantitative structure activity analysis study

  Authors: Ashutosh Kumar Pandey, Omprakash Tanwar, Girdhar Singh Deora, Chandrabose Karthikeyan, N. S. Hari Narayana Moorthy, Piyush Trivedi

  Medicinal Chemistry Research. 01/2011;

  A QSAR study has been performed on a series of aminopyrazolopyridine urea derivatives with potent VEGFR kinase inhibitory activity. Structural features responsible for the activity of the compoundsA QSAR study has been performed on a series of aminopyrazolopyridine urea derivatives with potent VEGFR kinase inhibitory activity. Structural features responsible for the activity of the compounds were characterized by using physicochemical, topological, and electrotopological descriptors, calculated from the Molecular Design Suite software (V-life MDSTM 3.5). Correlations between the inhibitory activities (KDR and KDRcell) of aminopyrazolopyridine urea derivatives and the calculated descriptors were established through simulated annealing method. The best QSAR models generated from the study explain 89 and 88% of the variation in KDR and KDRcell inhibitory activities, respectively. Internal and external validation methods were used to evaluate the predictive capacity of the generated models. The significant cross-validated correlation coefficient (Q2[0.6) and other statistical parameters suggest that the models exhibited considerable predictivity. The generated QSAR models divulge that factors related to lipophilicity and topological state of atoms in the molecule influences KDR and KDRcell inhibitory activities of aminopyrazolopyridine urea derivatives.

• 3D QSAR of aminophenyl benzamide derivatives as histone deacetylase inhibitors.

  Authors: Mahipal, Om Prakash Tanwar, C Karthikeyan, N S Hari Narayana Moorthy, Piyush Trivedi

  Medicinal chemistry (Shāriqah (United Arab Emirates)). 10/2010; 6(5):277-85.

  The article describes the development of a robust pharmacophore model and the investigation of structure activity relationship analysis of 48 aminophenyl benzamide derivatives reported for HistoneThe article describes the development of a robust pharmacophore model and the investigation of structure activity relationship analysis of 48 aminophenyl benzamide derivatives reported for Histone Deacetylase (HDAC) inhibition using PHASE module of Schrodinger software. A five point pharmacophore model consisting of two aromatic rings (R), two hydrogen bond donors (D) and one hydrogen bond acceptor (A) with discrete geometries as pharmacophoric features was developed and the generated pharmacophore model was used to derive a predictive atom-based 3D QSAR model for the studied dataset. The obtained 3D QSAR model has an excellent correlation coefficient value (r(2)=0.99) along with good statistical significance as shown by high Fisher ratio (F=631.80). The model also exhibits good predictive power confirmed by the high value of cross validated correlation coefficient (q(2) = 0.85). The QSAR model suggests that hydrophobic character is crucial for the HDAC inhibitory activity exhibited by these compounds and inclusion of hydrophobic substituents will enhance the HDAC inhibition. In addition to the hydrophobic character, hydrogen bond donating groups positively contributes to the HDAC inhibition whereas electron withdrawing groups has a negative influence in HDAC inhibitory potency. The findings of the QSAR study provide a set of guidelines for designing compounds with better HDAC inhibitory potency.

• A new approach for PEGylation of dendrimers.

  Authors: Hemant Khambete, Surya P Gautam, C Karthikeyan, Suman Ramteke, N S Hari Narayana Moorthy, Piyush Trivedi

  Bioorganic & medicinal chemistry letters. 07/2010; 20(14):4279-81.

  Dendrimers have emerged as one of the most interesting themes for researchers as a result of unique functional architecture and macromolecular characteristics. The reported methods of PEGylation areDendrimers have emerged as one of the most interesting themes for researchers as a result of unique functional architecture and macromolecular characteristics. The reported methods of PEGylation are very time consuming and required multisteps for synthesis. In present work we have synthesized PEGylated polyamidoamine (PAMAM) dendrimers using epichlorohydrin as a linker. The PEGylated dendrimers were evaluated for color reaction UV, IR and NMR studies and compared with standard data.

• Design, synthesis, cytotoxic evaluation, and QSAR study of some 6H-indolo[2,3-b]quinoxaline derivatives.

  Authors: N S Hari Narayana Moorthy, C Karthikeyan, Piyush Trivedi

  Journal of enzyme inhibition and medicinal chemistry. 03/2010; 25(3):394-405.

  In the pathway of anticancer drug development, we designed and synthesized some 6H-indolo[2,3-b]quinoxaline derivatives (which act as DNA intercalators) by structural modification. The structure ofIn the pathway of anticancer drug development, we designed and synthesized some 6H-indolo[2,3-b]quinoxaline derivatives (which act as DNA intercalators) by structural modification. The structure of the 6H-indolo[2,3-b]quinoxaline derivatives was confirmed by IR, NMR, Mass and elemental analysis. The compounds (IDQ-5, IDQ-10, IDQ-11, IDQ-13, and IDQ-14) exhibited significant in vitro activity against a human leukemia (HL-60) cell line. The QSAR derived for modeling the cytotoxic activity of 6H-indolo[2,3-b]quinoxaline derivatives suggests that candidate structures for increased cytotoxic potency should incorporate cyclic substituents or substituents with primary carbon atoms.

• RP-HPLC Method for Estimation and Stability Study of Drotaverine HCl as per ICH Guidelines

  Authors: Prafull Tailor, Kapendra Sahu, Kuldeep Patel, C Karthekeyan, N.S. Hari Narayana Moorthy, Mahipal, Blessy Joseph, Piyush Trivedi

  Latin American journal of pharmacy. 01/2010;

• Design,synthesis,biological evaluation and molecular modelling studies of some coumarin based antimalarial agents

  Authors: Kuldeep patel.c.karthikeyan, N S Hari Narayana moorthy, Girdhar singh Deora, Piyush Trivedi

  4th International conference on Recent advances in cardiovascular sciences, DIPSAR, NEW DELHI; 01/2010