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Trimeric Hemibastadin Congener from the Marine Sponge Ianthella basta

机译:来自海洋海绵Ianthella basta的三聚物Hemibastadin同系物

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摘要

The first naturally occurring trimeric hemibastadin congener, sesquibastadin 1 (1), and the previously reported bastadins 3, 6, 7, 11, and 16 (2-6) were isolated from the marine sponge Ianthella basta, collected in Indonesia. The structure of 1 was elucidated on the basis of 1D and 2D NMR measurements and by HRMS. Among all the isolated compounds, the linear sesquibastadin 1 (1) and bastadin 3 (2) showed the strongest inhibition rates for at least 22 protein kinases (IC50 = 0.1-6.5 mu M), while the macrocyclic bastadins (3-6) demonstrated a strong cytotoxic potential against the murine lymphoma cell line L5178Y (IC50 = 1.5-5.3 mu M).
机译:从印度尼西亚收集的海生海绵伊恩氏菌中分离出第一个天然存在的三聚半胱氨酸同源物倍半素1(1)和先前报道的巴斯德丁3、6、7、11和16(2-6)。根据1D和2D NMR测量并通过HRMS阐明了1的结构。在所有分离的化合物中,线性倍半胱氨酸1(1)和巴斯塔丁3(2)对至少22种蛋白激酶(IC50 = 0.1-6.5μM)表现出最强的抑制率,而大环巴斯塔丁(3-6)表现出对鼠淋巴瘤细胞株L5178Y具有很强的细胞毒性(IC50 = 1.5-5.3μM)。

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