N-((1-Benzyl-1 H-1, 2, 3-triazol-4-yl) methyl) arylamide as a new scaffold that provides rapid access to antimicrotubule agents: synthesis and evaluation of …
…, R Palchaudhuri, PA Miller, RJ Peterson…
文献索引：Stefely, Jonathan A.; Palchaudhuri, Rahul; Miller, Patricia A.; Peterson, Rebecca J.; Moraski, Garrett C.; Hergenrother, Paul J.; Miller, Marvin J. Journal of Medicinal Chemistry, 2010 , vol. 53, # 8 p. 3389 - 3395
A series of N-((1-benzyl-1 H-1, 2, 3-triazol-4-yl) methyl) arylamides was synthesized by copper-catalyzed azide− alkyne cycloaddition (CuAAC) and afforded inhibitors of cancer cell growth. For example, compound 13e had an IC50 of 46 nM against MCF-7 human breast tumor cells. Structure− activity relationship (SAR) studies demonstrated that (i) meta- phenoxy substitution of the N-1-benzyl group is important for antiproliferative activity and ( ...
