Degrasyn-like symmetrical compounds: Possible therapeutic agents for multiple myeloma (MM-I)
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- 作者：Zhenghong Peng ; David S. Maxwell ; Duoli Sun ; Basvoju A. Bhanu Prasad ; Paul T. Schuber Jr. ; Ashutosh Pal ; Yunming Ying ; Dongmei Han ; Liwei Gao ; Shimei Wang ; Alex ; er Levitzki ; Vaibhav Kapuria ; Moshe Talpaz ; Matthew Young ; Hollis D. Showalter ; Nicholas J. Donato ; William G. Bornmann
- 关键词：Degrasyn ; Multiple myeloma ; Jak2/Stat3 ; Small molecules ; Inhibitors ; Synthesis
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：15 February, 2014
- 年：2014
- 卷：22
- 期：4
- 页码：1450-1458
- 全文大小：935 K
文摘
A series of degrasyn-like symmetrical compounds have been designed, synthesized, and screened against B cell malignancy (multiple myeloma, mantle cell lymphoma) cell lines. The lead compounds T5165804 and CP2005 showed higher nanomolar potency against these tumor cells in comparison to degrasyn and inhibited Usp9x activity in vitro and in intact cells. These observations suggest that this new class of compounds holds promise as cancer therapeutic agents.