Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue 16, Pages 3795-3803Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm070410z
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Funding
- NCI NIH HHS [R01 CA047135-19, U19 CA052955, R01 CA 47135, U19 CA052955-19, R01 CA047135] Funding Source: Medline
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The sponge-derived polyketide macrolides fijianolides A (1) and B (2), isolaulimalide and laulimalide, have taxol-like microtubule-stabilizing activity, and the latter exhibits potent cytotoxicity. Insight on the biogeographical and phenotypic variations of Cacospongia mycofijiensis is presented that will enable a future study of the biosynthetic pathway that produces the fijianolides. In addition to fijianolides A and B, six new fijianolides, D-I (7-12), were isolated, each with modifications to the C-20 side chain of the macrolide ring. Compounds 7-12 exhibited a range of in vitro activities against HCT- 116 and MDA-MB-435 cell lines. Fijianolides 8 and 10 were shown to disrupt interphase and mitotic division, but were less potent than 2. An in vivo evaluation of 2 using tumor-bearing severe combined immuno-deficiency mice demonstrated significant inhibition of growth in HCT- 116 tumors over 28 days.
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