jorunnamycin-a and Breast-Neoplasms

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.

Topics: Antineoplastic Agents, Phytogenic; Breast Neoplasms; Carcinoma; Cell Line, Tumor; Cell Proliferation; Colonic Neoplasms; Drug Screening Assays, Antitumor; Female; Humans; Inhibitory Concentration 50; Molecular Structure; Structure-Activity Relationship; Tetrahydroisoquinolines