期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 92, 期 -, 页码 501-513出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.10.077
关键词
Pyrazole-oxindole conjugates; Tubulin depolymerization; Zebrafish screening and molecular modeling
资金
- CSIR, New Delhi
- UGC, New Delhi
- CSIR [CSC0301, CSC0111]
A series of twenty one compounds with pyrazole and oxindole conjugates were synthesized by Knoe-venagel condensation and investigated for their antiproliferative activity on different human cancer cell lines. The conjugates are comprised of a four ring scaffold; the structural isomers 12b and 12c possess chloro-substitution in the D ring. Among the congeners 12b, 12c, and 12d manifested significant cytotoxicity and inhibited tubulin assembly. Treatments with 12b, 12c and 12d resulted in accumulation of cells in G2/M phase, disruption of microtubule network, and increase in cyclin B1 protein. Zebrafish screening revealed that 12b, and 12d caused developmental defects. Docking analysis demonstrated that the congeners occupy the colchicine binding pocket of tubulin. (C) 2013 Elsevier Masson SAS. All rights reserved.
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