Girdhar Singh Deora

Publications

• 1.04

  Impact points

  In Vitro Screening of Dry Fruit Extracts of Piper attenuatum for Antioxidant and Anticancer Activity

  Renu Ohlyan, Ajit Kandale, Girdhar Singh Deora, Vandana Rathore, Jagbir Chahal

  Medicinal Chemistry Research. 05/2012; DOI: 10.1007/s00044-012-0122-y.

  Indian traditional medicinal plant Piper attenuatum (Buch-Ham) was investigated for its antioxidant and anticancer activity. Three extracts were prepared using ethyl acetate, ethanol and methanol. In vitro antioxidant activity was performed by ABTS {2,2'-azino-bis(3-ethylbenzothiazoline-6-sulpho... [more] Indian traditional medicinal plant Piper attenuatum (Buch-Ham) was investigated for its antioxidant and anticancer activity. Three extracts were prepared using ethyl acetate, ethanol and methanol. In vitro antioxidant activity was performed by ABTS {2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)} free radical scavenging method. All three extracts reduced the free radicals produced by ABTS in a concentration dependent manner which could be compared to the standard (Gallic acid). Invitro anticancer activity of all extracts was carried out by MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay method against MCF7 (Michigan Cancer Foundation-7) cell lines. None of the extract showed anticancer activity when compared with the standard (Mitomycin-C) indicating that p. attenuatum is deprived of antiproliferative or cytotoxic components.
• 1.04

  Impact points

  Identification of ZINC02765569: a potent inhibitor of PTP1B by vHTS

  Prashant Joshi, Girdhar Singh Deora, Vandana Rathore, Omprakash Tanwar, Arun K. Rawat, A. K. Srivastava, Deepti Jain

  Medicinal Chemistry Research. 02/2012;

  The present study describes identification of a novel lead molecule ZINC02765569 for inhibition of Protein tyrosine phosphatase 1B (PTP1B) enzyme by a high throughput virtual screening of Zinc database against catalytic domain of PTP1B employing docking algorithm Glide. The identified hit molecule Z... [more] The present study describes identification of a novel lead molecule ZINC02765569 for inhibition of Protein tyrosine phosphatase 1B (PTP1B) enzyme by a high throughput virtual screening of Zinc database against catalytic domain of PTP1B employing docking algorithm Glide. The identified hit molecule ZINC02765569 was synthesized and evaluated for in-vitro PTP1B enzyme inhibition, in-vitro cellular glucose uptake assay and animal models of hyperglycemia. ZINC02765569 shows promising inhibition of PTP1B enzyme at 10 μm assay, positively up-regulate the cellular glucose uptake in skeletal cell muscle myotubes and SLM/STZ hyperglycemic animal experiments. The novel hit reported here should provide a platform for the further development of its analogues as potential PTP1B enzyme inhibitors.
• 1.04

  Impact points

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

  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 against chloroquine sensitive and chloroquine resistant strains. The most potent compound 4-hydroxy-3-(3-(4-nitrop... [more] 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 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.
• 1.04

  Impact points

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

  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 compounds were characterized by using physicochemical, topological, and electrotopological descriptors, calculat... [more] 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 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.
• 0.81

  Impact points

  Coumarinyl Chalcones and their Antiproliferative Activity Against Breast Cancer Cell Lines

  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 one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity... [more] 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.