In:
ChemMedChem, Wiley, Vol. 11, No. 13 ( 2016-07-05), p. 1446-1458
Abstract:
A series of 1‐methyl‐1 H ‐indole–pyrazoline hybrids were designed, synthesized, and biologically evaluated as potential tubulin polymerization inhibitors. Among them, compound e19 [5‐(5‐bromo‐1‐methyl‐1 H ‐indol‐3‐yl)‐3‐(3,4,5‐trimethoxyphenyl)‐4,5‐dihydro‐1 H ‐pyrazole‐1‐carboxamide] showed the most potent inhibitory effect on tubulin assembly (IC 50 =2.12 μ m ) and in vitro growth inhibitory activity against a panel of four human cancer cell lines (IC 50 values of 0.21–0.31 μ m ). Further studies confirmed that compound e19 can induce HeLa cell apoptosis, cause cell‐cycle arrest in G 2 /M phase, and disrupt the cellular microtubule network. These studies, along with molecular docking and 3D‐QSAR modeling, provide an important basis for further optimization of compound e19 as a potential anticancer agent.
Type of Medium:
Online Resource
ISSN:
1860-7179
,
1860-7187
DOI:
10.1002/cmdc.201600137
Language:
English
Publisher:
Wiley
Publication Date:
2016
detail.hit.zdb_id:
2209649-8
SSG:
15,3