Synthesis and SAR of [1, 2, 4] triazolo [1, 5-a] pyrimidines, a class of anticancer agents with a unique mechanism of tubulin inhibition

…, S Ayral-Kaloustian, T Nguyen, J Afragola…

Index: Zhang, Nan; Ayral-Kaloustian, Semiramis; Nguyen, Thai; Afragola, Jay; Hernandez, Richard; Lucas, Judy; Gibbons, James; Beyer, Carl Journal of Medicinal Chemistry, 2007 , vol. 50, # 2 p. 319 - 327

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Citation Number: 110

Abstract

The synthesis and SAR of a series of triazolopyrimidines as anticancer agents are described. Treatment of 5-chloro-6-(trifluorophenyl)-N-fluoroalkyl [1, 2, 4] triazolo [1, 5-a] pyrimidin-7-amine with an alcohol, a thiol, or an alkylamine provided the corresponding final compounds. A clear SAR requirement has been established for optimal activity. A (1 S)-2, 2, 2-trifluoro-1-methylethylamino group or an achiral 2, 2, 2-trifluoroethylamino group is ...