Discovery of (2 S)-1-[4-(2-{6-Amino-8-[(6-bromo-1, 3-benzodioxol-5-yl) sulfanyl]-9 H-purin-9-yl} ethyl) piperidin-1-yl]-2-hydroxypropan-1-one (MPC-3100), a Purine- …

…, B Markovitz, R Trovato, M Shenderovich…

Index: Kim, Se-Ho; Bajji, Ashok; Tangallapally, Rajendra; Markovitz, Benjamin; Trovato, Richard; Shenderovich, Mark; Baichwal, Vijay; Bartel, Paul; Cimbora, Daniel; McKinnon, Rena; Robinson, Rosann; Papac, Damon; Wettstein, Daniel; Carlson, Robert; Yager, Kraig M. Journal of Medicinal Chemistry, 2012 , vol. 55, # 17 p. 7480 - 7501

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Citation Number: 28

Abstract

Modulation of Hsp90 (heat shock protein 90) function has been recognized as an attractive approach for cancer treatment, since many cancer cells depend on Hsp90 to maintain cellular homeostasis. This has spurred the search for small-molecule Hsp90 inhibitors. Here we describe our lead optimization studies centered on the purine-based Hsp90 inhibitor 28a containing a piperidine moiety at the purine N9 position. In this study, key SAR was ...