Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl)benzannide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor

Uno, T; Kawai, Y; Yamashita, S; Oshiumi, H; Yoshimura, C; Mizutani, T; Suzuki, T; Chong, KT; Shigeno, K; Ohkubo, M; Kodama, Y; Muraoka, H; Funabashi, K; Takahashi, K; Ohkubo, S; Kitade, M

Uno, T (reprint author), Taiho Pharmaceut Co Ltd, Discovery & Preclin Res Div, Tsukuba, Ibaraki 3002611, Japan.

JOURNAL OF MEDICINAL CHEMISTRY, 2019; 62 (2): 531

Abstract

The molecular chaperone heat shock protein 90 (HSP90) is a promising target for cancer therapy, as it assists in the stabilization of cancer-related p......

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