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Genin, M.J., Biles, C., Keiser, B.J., Poppe, S.M., Swaney, S.M., Tarpley, W.G., Yagi, Y. and Romero, D.L. (2000) Novel 1,5-Diphenylpyrazole Nonnucleoside HIV-1 Reverse Transcriptase Inhibitors with Enhanced Activity versus the Delavirdine-Resistant P236L Mutant: Lead Identification and SAR of 3- and 4-Substituted Derivatives. Journal of Medicinal Chemistry, 43, 1034-1040.
https://doi.org/10.1021/jm990383f
has been cited by the following article:
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TITLE:
Molecular Modeling and Synthesis of New Heterocyclic Compounds Containing Pyrazole as Anticancer Drugs
AUTHORS:
Fiby N. Takla, Abdelbasset A. Farahat, Magda A.-A. El-Sayed, Magda N. A. Nasr
KEYWORDS:
Tubulin, CA-4, Anticancer, Pyrazole, Molecular Modeling
JOURNAL NAME:
International Journal of Organic Chemistry,
Vol.7 No.4,
December
15,
2017
ABSTRACT: Several modifications in CA-4 were reported in
literature for the development of various tubulin inhibitors. In our study,
twenty-two newly synthesized heterocyclic derivatives of Combretastatin A-4
(CA-4) have been tested for their cytotoxic effect on four different types of
cells with malignant behavior using CA-4 as a positive control. Compounds 5b, 15 and 16 showed the foremost potent antiproliferative activities
as compared to CA-4 with IC50 starting from 6.9 to 13.7 μM. Molecular docking
was performed with the crystal structure of tubulin employing a potent tubulin
inhibitor CA-4 as a parent molecule. Molecular study advised that 5b, 15, 16 and 17 are promising tubulin inhibitors.