Abstract
Nine new derivatives (6-14) of the eremophilane sesquiterpene 07H239-A (5) were designed and semisynthesized with two types of R- groups by amidation. Most of them were active against five human tumor cell lines, and compounds 6-10 were more potent than the natural product 5. In particular, compounds 6 and 9 exhibited the strongest cytotoxic activity against MDA-MB-435 with IC 50 values of 0.91 and 0.96μM, respectively. Preliminary structure-activity relationships (SARs) analysis indicated that the 14-carboxyl in 5 was an ideal target for chemical modification, and the side chain of 5 might play a necessary role in facilitating their cytotoxic potencies. © 2011 Pharmaceutical Society of Japan.
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Song, Y. X., Cheng, B., Zhu, X., Qiao, L. T., Wang, J. J., Gu, Y. C., … Lin, Y. C. (2011). Synthesis and cytotoxic evaluation of eremophilane sesquiterpene 07H239-A derivatives. Chemical and Pharmaceutical Bulletin, 59(9), 1186–1189. https://doi.org/10.1248/cpb.59.1186
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