Richard I Feldman, Bob Mintzer, Daguang Zhu, James M Wu, Sandra L Biroc, Shendong Yuan, Kumar Emayan, Zheng Chang, Deborah Chen, Damian O Arnaiz, Judi Bryant, Xue Snow Ge, Marc Whitlow, Marc Adler, Mark A Polokoff, Wei-Wei Li, Mike Ferrer, Takashi Sato, Jian-Ming Gu, Jun Shen, Jih-Lie Tseng, Harald Dinter, Brad Buckman
Heat-shock protein-90 is an attractive target for anticancer drugs, as heat-shock protein-90 blockers such as the ansamycin 17-(allylamino)-17-demethoxygeldanamycin greatly reduce the expression of many signaling molecules that are disregulated in cancer cells and are key drivers of tumor growth and metastasis. While 17-(allylamino)-17-demethoxygeldanamycin has shown promise in clinical trials, this compound class has significant template-related drawbacks. In this paper, we describe a new, potent non-ansamycin small-molecule inhibitor of heat-shock protein-90, BX-2819, containing resorcinol and triazolothione rings...
July 2009: Chemical Biology & Drug Design