期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 11, 期 2, 页码 108-113出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00302
关键词
Mycothiazole; cytotoxic; picomolar; 8S configuration
资金
- NIH [RO1 CA 47135, S10OD024998]
- American Society of Pharmacognosy (ASP)
- Dominican University of California Summer Research Grants
- Fletcher Jones Endowment Fund of Dominican University of California
Reinvestigation of mycothiazole (1) revealed picomolar potency (IC50 = 0.00016, 0.00027, 0.00035 mu M) against pancreatic, (PANC-1), liver (HepG2), and colon (HCT-116) tumor cell lines. Reevaluation of 1 provided [alpha](D) data indicating Vanuatu specimens of C. mycofijiensis contain the 8S enantiomer of 1 and not the 8R configuration previously reported. Semisynthesis provided 8-O-acetylmycothiazole (2), 8-oxomycothiazole (8), mycothiazole nitrosobenzene derivatives (MND1, MND2: 9a, 9b), and MND3 (10) with IC50 = 0.00129, >1.0, >1.0, >1.0, >1.0 mu M, respectively, against PANC-1 cell lines. These results highlight the significance of the penta-2,4-dien-l-ol residue as a key structural feature of 1 required for its cytotoxicty against tumor cell lines.
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