设计、合成及阿朴隆宁 A-麦角甾烷醇 B 杂合化合物的生物评价。
Design, synthesis, and biological evaluations of aplyronine A-mycalolide B hybrid compound.
机构信息
Department of Chemistry, Graduate School of Pure and Applied Sciences, University of Tsukuba, Tennodai, Tsukuba 305-8571, Japan.
出版信息
Org Lett. 2012 Mar 2;14(5):1290-3. doi: 10.1021/ol300182r. Epub 2012 Feb 22.
A hybrid compound consisting of aplyronine A and mycalolide B was synthesized, and its biological activities were evaluated. The hybrid compound was found to have somewhat more potent actin-depolymerizing activity than aplyronine A. In contrast, the hybrid compound possessed about 1000-fold less cytotoxicity than aplyronine A. These results indicated that there is no direct correlation between actin-depolymerizing activity and cytotoxicity.
合成了一种由 aplronine A 和 mycalolide B 组成的杂合化合物，并评价了其生物学活性。该杂合化合物具有比 aplronine A 更强的微丝解聚活性。相比之下，该杂合化合物的细胞毒性比 aplronine A 低约 1000 倍。这些结果表明，微丝解聚活性和细胞毒性之间没有直接的相关性。
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