Hydramycin (NSC-698410, 1) is an anthraquinone-type antitumor agent that has shown broad-spectrum activity against a variety of human-derived cancer cell lines.  Among tumors evaluated (lung, colon, melanoma, breast and prostate), GI50's were <10-10 M in the NCI's 60-cell-line panel.   Our objectives were to synthesize and evaluate simplified analogues 2 and 3 that would facilitate synthesis, yet retain potent activities. Antitumor evaluation showed across-the-board GI50's of ~10-8�10-7 M for 2 (NSC-731341, -731342) and 3 (NSC-746372, -746373), with one diastereomer more potent than the other.  A total synthesis of the enantiomerically pure 2 and 3 will be discussed.                                                   

Anthraquinone-type anticancer compounds: Derivatives of hydramycin (NSC-698410)

240th National Meeting (2010)

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