Abstract
Leinamycin, a novel antitumor antibiotic, was isolated from a culture broth of Streptomyces sp. The unique structural features of leinamycin include the 1-oxo-1, 2-dithiolan-3-one moiety which is fused in a spiro fashion to an 18-membered lactam with an extensively conjugated thiazole ring. Leinamycin causes single strand scission of plasmid DNA in the presence of thiol cofactor. Isolation of a guanine-leinamycin adduct revealed the unprecedented chemical reactions which would be responsible for the thiol-mediated DNA cleavage by leinamycin. As a part of our program aimed at discovering clinically useful leinamycin derivatives, chemical modification of natural leinamycin have been investigated. In this review, synthesis and chemistry of novel leinamycin derivatives with potent antitumor activity are described. Thioester derivatives with 3-isothiazolidinone 1-oxide moiety are more stable than leinamycin and serve as prodrugs that could be converted into active form in biological media.
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