Wen-Wei You

Southern Medical University, Shengcheng, Guangdong, China

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Publications (14)12.69 Total impact

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    ABSTRACT: A series of novel hybrids of indole-pyrimidine containing piperazine moiety were designed, synthesized and evaluated for their antiproliferative and tubulin polymerization inhibitory activities. The results indicated that most of these compounds possessed significant cytotoxic potency against four cancer cell lines, HT-29, A549, MDA-MB-231 and MCF-7. Particularly, the most promising compound 34 showed more potent and broad-spectrum cytotoxic activities with the IC50 values ranged from 5.01 to 14.36 μM against A549, MDA-MB-231 and MCF-7 cell lines. Meanwhile, 34 also displayed the most potent tubulin polymerization inhibitory activity with IC50 value of 11.2 μM. Furthermor, molecular docking analysis demonstrated 34 interacts and binds efficiently with the tubulin protein at the colchicine binding site. It was worth noting that, the compound did not affect the normal human embryonic kidney cells, HEK-293. These results suggest that this novel class of indole-pyrimidine hybrids may have potential to be developed as new a class of tubulin polymerization inhibitors. This article is protected by copyright. All rights reserved. This article is protected by copyright. All rights reserved.
    Chemical Biology &amp Drug Design 07/2015; DOI:10.1111/cbdd.12616 · 2.51 Impact Factor
  • Jie Feng · Zhong-Qiu Liu · Yi-Chen Yan · Ming Hu · Ling Lu · Wen-Wei You
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    ABSTRACT: To prepare pravastatin sodium-loaded chitosan microspheres to allow sustained drug release. The drug-loaded chitosan microspheres were prepared by using genipin as the cross-linker. The influences of molecular weight of chitosan, volume ratio of oil and water, reaction temperature, and stirring speed on the formation of chitosan microspheres were investigated. The morphology of the microspheres was observed using scanning electron microscopy. The encapsulation efficiency, swelling ratio under different pH conditions, and in vitro drug release were measured. The in vitro release of pravastatin sodium could last for at least 31 days. The drug release rate varied with the reaction condition. The drug entrapment efficiency of the microsphere was 54.7%. The optimal processing conditions were as follows: chitosan viscosity of 200-400 mPa·s, oil-water proportion of 10:1, stirring speed of 850 r/min, and reaction temperature at 40 degrees celsius;. The pravastatin sodium-loaded microspheres show good sustained drug release property, and the drug release rate can be modified by controlling the cross-linking time.
    Nan fang yi ke da xue xue bao = Journal of Southern Medical University 06/2015; 35(6):879-82.
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    ABSTRACT: To prepare a pH fluorescence probe based on styrylcyanine dyes for live cell imaging. The Probe 1 was prepared by reaction of 4-pyridinecarboxaldehyde with 1,1,2-trimethylbenz[e]indole. The influence of pH on the fluorescent properties was examined, and the cell viability was examined using cell counting kit-8. The Probe 1 was used as a pH fluorescence probe in living cell. Probe 1 emitted green fluorescence under neutral and basic conditions but orange fluorescence under acid condition. Probe 1 selectively stained the cytoplasmic regions of living cells without significantly affecting the cell viability. The pH-sensitive fluorescent probe prepared based on styrylcyanine possesses good ability of cell membrane permeation for live cell fluorescent imaging.
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    ABSTRACT: A series of novel 2,4-diaminopyrimidines containing piperidine and piperazine moieties were synthesized via an efficient one-pot methodology. The bioassay tests demonstrated that compounds 27 and 28 displayed much stronger antitumor activities against four human cancer cell lines (HepG2, A549, MDA-MB-231 and MCF-7) than positive control fluorouracil. Particularly, compound 28 showed a two-fold improvement compared to fluorouracil in inhibiting MDA-MB-231 and A549 cell proliferation with IC50 values of 7.46 and 12.78 μM, respectively. Further flow-activated cell sorting analysis revealed that the most promising compound 28 displayed a significant effect on G2/M cell-cycle arrest in a dose-dependent manner in MDA-MB-231 cells.
    European Journal of Medicinal Chemistry 07/2014; 84C:127-134. DOI:10.1016/j.ejmech.2014.07.017 · 3.43 Impact Factor
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    ABSTRACT: An efficient one-pot synthesis of 3-amino-7-azaindoles was developed, starting from ethyl (3-cyanopyridin-2-yl)carbamate and α -bromoketones by microwave-assisted Thorpe–Ziegler cyclization in the presence of a base. This method features excellent yields, short reaction time (10min), and high functional group compatibility.[Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the following free supplemental resource(s): Full experimental and spectral details.]
    Synthetic Communications 03/2014; 44(8). DOI:10.1080/00397911.2013.858360 · 0.98 Impact Factor
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    ABSTRACT: A series of novel isoindoline-1,3-diones containing 1,2,4-triazole moiety were synthesized via a one-pot reaction. Bioassay indicated that compounds 33, 35, 37 and 39 exhibited much higher activities against Botryodiplodia theobromae than commercial fungicide triadimefon at the dosage of 150 mg/L. Most interestingly, compounds 36, 37 and 45 displayed much stronger antitumor activities against four human cell lines than positive control Fluorouracil. Particularly, compound 37 had four-fold improvement compared to Fluorouracil in inhibiting A549 and HepG2 cell proliferation with IC(50) values of 6.76 and 9.44 μM, respectively. Further flow-activated cell sorting analysis revealed that compound 37 displayed apoptosis-inducing effect on HepG2 cells in a dose-dependent manner. These encouraging results could be helpful for the development of new antitumor compounds.
    European Journal of Medicinal Chemistry 07/2012; 54:813-22. DOI:10.1016/j.ejmech.2012.06.041 · 3.43 Impact Factor
  • Pei-Liang Zhao · Wen-Wei You · An-Na Duan
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    ABSTRACT: Pyrimidine derivatives have been the subject of much attention in pesticide and medicine fields owing to their unique biological properties. Particularly, a large number of these compounds have recently been reported to show substantial antitumor activities, and some of them have been investigated in clinical trials. Although these structurally novel compounds have a common chemical moiety of a pyrimidine ring, there are a variety of mechanisms of their antitumor action, such as, inhibition of cyclin-dependent-kinases, inhibition of protein tyrosine kinase, inhibition of carbonic anhydrases, inhibition of dihydrofolate reductase and disruption of microtubule assembly. In this paper, we described the latest advances in the research of such pyrimidine derivatives as antitumor drug according to their action on targets.
    Yao xue xue bao = Acta pharmaceutica Sinica 05/2012; 47(5):580-7.
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    ABSTRACT: A series of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and some novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles bearing 3,4,5-trimethoxyphenyl moiety were synthesized and screened for their anticancer activity. The preliminary bioassay results indicated that compounds 14 and 16 showed much stronger cytotoxicity than Doxorubicin against HepG2 cell lines with IC(50) values of 0.58 and 3.17 μM, respectively. Meanwhile compound 16 also exhibited a broad spectrum of antitumor activity against MCF-7 and MKN45 with IC(50) values of 10.92 and 13.79 μM, respectively.
    Bioorganic & medicinal chemistry letters 03/2012; 22(13):4471-4. DOI:10.1016/j.bmcl.2012.03.023 · 2.33 Impact Factor
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    ABSTRACT: To synthesize cyclin-dependent kinase (CDKs) inhibitors and assay their antitumor activities. A series of pyrimidines containing different arylamino and 1-(methylsulfonyl)piperidin moieties were designed by combining the segments 1-(methylsulfonyl)piperidin and pyrimidine heterocycles according to the super-postion principle of the reinforcement of biological activities. Their structures were characterized by MS and 1H NMR spectra and all the synthesized compounds were screened for their antimicrobial activity with MTT assay. The preliminary bioassay showed that compound 3 b displayed good antitumor activity (IC(50)=13.6 µmol/L). The preliminary structure activity relationship analysis of these analogues suggest that the steric factor may have important impact on the anti-tumor activity.
    Nan fang yi ke da xue xue bao = Journal of Southern Medical University 05/2011; 31(5):875-7.
  • Wen-wei You · Zhao-hui Wu · Min Zou · Xiao-mei Tan
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    ABSTRACT: To establish a HPLC-based method for simultaneous determination of 2 classes of compounds (flavonoids and chromones) and 6 their effective components,(including prin-O-glucosylcimifugin, cimifugin, 4'-O-beta-D-glucosyl- 5-O-methylvisamminol, quercetin, sec-o-glucosylhamaudol and formononetin), in Yupingfeng Decoction. HPLC-based separation of the agents was performed on Agilent Extend-C(18) column (4.6 mm x 250 mm, 5 microm) at 25 degrees with the mobile phase of MeOH-1% acetic acid water solution (gradient elution), flow rate of 0.8 ml/min and detection wavelength of 254 nm. HPLC allowed simultaneous quantitative determination of the 6 components in Yupingfeng Decoction, and they showed good linear relationships when their sample amount ranged 90-1810 ng, 97-1940 ng, 190-1906 ng, 105-3144 ng, 88-2625 ng and 109-3279 ng, respectively, with correlation coefficients all beyond 0.9999 and average recovery rates of 98.2%, 99.1%, 97.3%, 97.8%, 98.8% and 99.2%, respectively. This simple and convenient method accommodated a broad linear range with high sensitivity and precise and reproducible results.
    Nan fang yi ke da xue xue bao = Journal of Southern Medical University 07/2007; 27(6):884-6.
  • Zhao-hui Wu · Wen-wei You · Feng He
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    ABSTRACT: High-performance liquid chromatography with evaporative light-scattering detection (HPLC-ELSD) was employed for determination of amygdalin content in Semen Armeniacae Amarum. The detection was performed with the column of Hypersil-ODS (4.6 mm x 250 mm, 5 microm) and column temperature of 25 degrees C. The mobile phase was methanol-water (70:30) with flow rate of 0.5 ml/min. Evaporative light-scattering detector was used and the drift tube temperature was set at 98 degrees Celsius with the gas flow rate of 3.2 L/min. A standard curve was generated, which was linear in the range of 1.0-15.1 microg for amygdalin content (r=0.999 9). The average recovery of amygdalin was 99.0% with RSD of 2.9% (n=5). Besides simplicity and rapidness, the method yields accurate and reproducible results and can therefore be used in the quality control of Semen Armeniacae Amarum.
    Di 1 jun yi da xue xue bao = Academic journal of the first medical college of PLA 01/2006; 25(12):1549-51.
  • Wen-wei You · Zhao-hui Wu · Li Tong · Xue-feng Xing
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    ABSTRACT: To develop a method for determining the serum astragaloside in rats fed with Buyanghuanwu dicoction (a preparation of a traditional Chinese medicine). A solid-phase extraction column was employed for pretreating the serum samples. The fluorescence characteristics of the extract were measured following chemical derivatization with anisic acid-sulphuric acid. The endogenous interference was removed by solid-phase extraction. The excitation and emission maxima of the reaction product from astragaloside and anisic acid were at 310 nm and 376 nm respectively. The linear range of the calibration curve was 1.0 to 10.0 microg/ml with r=0.999 9. The average recovery rate of the method was 97% with relative standard derivation of 2.59%(n=5). This method is rapid and highly sensitive, and useful for monitoring the concentration of astragaloside in rat serum.
    Di 1 jun yi da xue xue bao = Academic journal of the first medical college of PLA 05/2003; 23(4):335-6, 339.
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    ABSTRACT: To synthesize p, p'-divinylazobenzene (DVAB). Wittig reagent was initially synthesized using P-nitrobenzyl bromide and triphenylphosphine, followed by reaction with formaldehyde to produce p-nitro styrene, which was then deoxidized by Zn/NaOH for the final product of DVAB. Fourier transform infrared spectroscopy, nuclear magnetic resonance and element analysis were employed to identify the structure of DVAB, and the lambda(max) as determined by ultraviolet spectroscopy occurred at 357 nm. The synthesis procedure of DVAB was therefore optimized with high yield.
    Di 1 jun yi da xue xue bao = Academic journal of the first medical college of PLA 04/2003; 23(3):273-6.