Synthesis and structure–activity relationship of 1-and 2-substituted-1, 2, 3-triazole letrozole-based analogues as aromatase inhibitors

J Doiron, R Richard, MM Touré, N Picot…

Index: Doiron, Jeremie; Soultan, Al Haliffa; Richard, Ryan; Toure, Mamadou Mansour; Picot, Nadia; Richard, Remi; Cuperlovic-Culf, Miroslava; Robichaud, Gilles A.; Touaibia, Mohamed European Journal of Medicinal Chemistry, 2011 , vol. 46, # 9 p. 4010 - 4024

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Citation Number: 33

Abstract

A series of bis-and mono-benzonitrile or phenyl analogues of letrozole 1, bearing (1, 2, 3 and 1, 2, 5)-triazole or imidazole, were synthesized and screened for their anti-aromatase activities. The unsubstituted 1, 2, 3-triazole 10a derivative displayed inhibitory activity comparable with that of the aromatase inhibitor, letrozole 1. Compound 10a, bearing a 1, 2, 3-triazole, is also 10000-times more tightly binding than the corresponding analogue 25 ...