Design,synthesis and anti-tumor activities in vitro of novel 3-substituted indolin-2-one compounds
10.3969/j.issn.1006-0111.2015.02.010
- VernacularTitle:3-取代吲哚-2-酮类化合物的设计、合成及抗肿瘤活性研究
- Author:
Hao ZHOU
1
;
Feng ZHOU
;
Youjun ZHOU
Author Information
1. 第二军医大学药学院药物化学教研室
- Keywords:
vascular targeting drug;
3-substituted indolin-2-one compounds;
tubulin inhibitory activities;
kinase inhibi-tory activities
- From:
Journal of Pharmaceutical Practice
2015;(2):131-133,142
- CountryChina
- Language:Chinese
-
Abstract:
Objective To compose and evaluate anti‐tumor activities of 3‐substituted indole‐2‐one compounds which may have dual inhibitory activities against both tubulin protein and VEGFR‐2 tyrosine kinase .Methods Target compounds were prepared starting from substituted aniline viacondensation ,cyclization and reduction .Results 11 target compounds were syn‐thesized and all the compounds displayed moderate anti‐proliferative activities against three tumor cell lines .Compound j9 showed a certain inhibitory activity against both VEGFR‐2 kinase and tubulin protein in vitro .Conclusion This series of indo‐lin‐2‐one derivatives were found to be a novel kind of multi‐target inhibitor .
