Abstract
Twenty-four ester analogues of renieramycin M ( 1m) were prepared from jorunnamycin A ( 3a), which was easily transformed from marine natural 1m in three steps. These analogues, along with 1m itself, cyanojorumycin ( 2b), and jorunnamycins A ( 3a) and C ( 3b), were evaluated in vitro for cytotoxicity by measuring IC 50 values through the 3-(4,5-dimethyltriazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay using human HCT116 colon carcinoma and MDA-MB-435 breast carcinoma cell lines. Nitrogen-containing heterocyclic ester derivatives 9a– f showed similar in vitro cytotoxicity to 1m, whereas the other derivatives were slightly less cytotoxic than 1m. 2′-Pyridinecarboxylic acid ester derivative ( 9c) exhibited a threefold increase in cytotoxicity relative to 1m.
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