756834-58-9Relevant academic research and scientific papers
Rationally simplified bistramide analog reversibly targets actin polymerization and inhibits cancer progression in vitro and in vivo
Rizvi, Syed Alipayam,Liu, Song,Chen, Zhonglei,Skau, Colleen,Pytynia, Matthew,Kovar, David R.,Chmura, Steven J.,Kozmin, Sergey A.
supporting information; experimental part, p. 7288 - 7290 (2010/08/13)
We describe structure-based design and chemical synthesis of a simplified analog of bistramide A, which potently and reversibly binds monomeric actin with a Kd of 9.0 nM, depolymerizes filamentous actin in vitro and in A549 (nonsmall cell lung cancer) cells, inhibits growth of cancer cell lines in vitro at submicromolar concentrations, and significantly suppresses proliferation of A549 cells in a nude mice tumor xenograft model in terms of both tumor growth delay and average tumor volume. This study provides a conceptual framework for the design and development of new antiproliferative compounds that target cytoskeletal organization of cancer cells in vivo by a combination of reversible G-actin binding and effective F-actin severing.
Synthesis of bistramide A
Statsuk, Alexander V.,Liu, Dong,Kozmin, Sergey A.
, p. 9546 - 9547 (2007/10/03)
We have developed an efficient and highly stereocontrolled synthesis of bistramide A, a selective activator of protein kinase C isotype δ. Our synthetic strategy featured a novel bidirectional approach for spiroketal construction based on the ring-opening
