Design, synthesis, and biological evaluation of novel deguelin-based heat shock protein 90 (HSP90) inhibitors targeting proliferation and angiogenesis

…, K Kim, HH Kim, J Jung, JM Lee, NJ Kim…

Index: Chang, Dong-Jo; An, Hongchan; Kim, Kyoung-Suk; Kim, Hyun Ho; Jung, Jinkyung; Lee, Jung Min; Kim, Nam-Jung; Han, Young Taek; Yun, Hwayoung; Lee, Sujin; Lee, Geumwoo; Lee, Seungbeom; Lee, Ju Sung; Cha, Jong-Ho; Park, Ji-Hyeon; Park, Ji Won; Lee, Su-Chan; Kim, Sang Geon; Kim, Jeong Hun; Lee, Ho-Young; Kim, Kyu-Won; Suh, Young-Ger Journal of Medicinal Chemistry, 2012 , vol. 55, # 24 p. 10863 - 10884

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Citation Number: 30

Abstract

Deguelin exhibits potent apoptotic and antiangiogenic activities in a variety of transformed cells and cancer cells. Deguelin also exhibits potent tumor suppressive effects in xenograft tumor models for many human cancers. Our initial studies confirmed that deguelin disrupts ATP binding to HSP90 and consequently induces destabilization of its client proteins such as HIF-1α. Interestingly, a fluorescence probe assay revealed that deguelin and its ...