Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from Streptomyces sp. 13F051

Ulleunganilines AC,来自链霉菌 13F051 的带有修饰侧链的曲古霉素类似物

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作者:Gwi Ja Hwang, Mina Jang, Sangkeun Son, Byeongsan Lee, Jun-Pil Jang, Jung-Sook Lee, Sung-Kyun Ko, Young-Soo Hong, Jong Seog Ahn, Jae-Hyuk Jang

Abstract

Three new trichostatin analogues, ulleunganilines A-C (1-3), and seven known trichostatins (4-10) were isolated from cultures of Streptomyces sp. 13F051. NMR, UV, and MS data indicated that the planar structures of 1-3 consisted of modified side chains in the trichostatic acid moiety. The absolute configuration of the 2,4-dimethyl-branched carbon chains in 1 and 2 was determined by the PGME method, while the amino acid group in 3 was identified by advanced Marfey's method. Based on the structure of the modified side chains, the origin of 1-3 is proposed. Further experiments indicated that 1 and 3 displayed moderate histone deacetylase inhibitory activity, suggesting that not only the hydroxamate group but also the N,N-dimethyl group were essential for the inhibitory activity.

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