Structural Requirements for the Antiproliferative Activity of Pre??mRNA Splicing Inhibitor FR901464

S Osman, BJ Albert, Y Wang, M Li…

Index: Osman, Sami; Albert, Brian J.; Wang, Yanping; Li, Miaosheng; Czaicki, Nancy L.; Koide, Kazunori Chemistry - A European Journal, 2011 , vol. 17, # 3 p. 895 - 904

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Citation Number: 39

Abstract

Abstract FR901464, a natural product isolated from a bacterium source, activates a reporter gene, inhibits pre-mRNA splicing, and shows antitumor activity. We previously reported the development of a more potent analogue, meayamycin, through the total synthesis of FR901464. Herein, we report detailed structure–activity relationships of FR901464 that revealed the significance of the epoxide, carbon atoms in the tetrahydropyran ring, the Z ...