Synthesis and Biological Evaluation of Highly Active 7-Anilino Triazolopyrimidines as Potent Antimicrotubule Agents.

ABSTRACT: Two different series of fifty-two compounds, based on 3',4',5'-trimethoxyaniline (7a-ad) and variably substituted anilines (8a-v) at the 7-position of the 2-substituted-[1,2,4]triazolo [1,5-a]pyrimidine nucleus, had moderate to potent antiproliferative activity against A549, MDA-MB-231, HeLa, HT-29 and Jurkat cancer cell lines. All derivatives with a common 3-phenylpropylamino moiety at the 2-position of the triazolopyrimidine scaffold and different halogen-substituted anilines at its 7-position, corresponding to 4'-fluoroaniline (8q), 4'-fluoro-3'-chloroaniline (8r), 4'-chloroaniline (8s) and 4'-bromoaniline (8u), displayed the greatest antiproliferative activity with mean IC_50's of 83, 101, 91 and 83 nM, respectively. These four

SUBMITTER: Oliva P 

PROVIDER: S-EPMC9230136 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature