Article

Synthesis and topoisomerase poisoning activity of A-ring and E-ring substituted lutonin A derivatives

Albany Medical College, Albany, New York, United States
Bioorganic & Medicinal Chemistry (Impact Factor: 2.95). 07/2007; 15(12):4237-46. DOI: 10.1016/j.bmc.2007.03.067
Source: PubMed

ABSTRACT A series of A-ring and E-ring analogues of the natural product luotonin A, a known topoisomerase I poison, was evaluated for growth inhibition in human carcinoma and leukemia cell lines. Rational design of structures was based on analogues of the related alkaloid camptothecin, which has been demonstrated to exert cytotoxic effects by the same mechanism of action. When compared to luotonin A, several compounds exhibited an improved topoisomerase I-dependent growth inhibition of a human leukemia cell line.

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