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1. Aza and diaza bioisosteric anthracene-9,10-diones as antitumor agents.

Author

Krapcho AP, Maresch MJ, Hacker MP, Menta E, Oliva A, Giuliani FC, and Spinelli S

Subjects
Animals, Humans, Mitoxantrone chemical synthesis, Mitoxantrone pharmacology, Tumor Cells, Cultured, Antineoplastic Agents chemical synthesis, Antineoplastic Agents pharmacology, Mitoxantrone analogs & derivatives
Abstract

Synthetic routes to aza and diaza bioisosteres related to the anthracene-9,10-dione, mitoxantrone, have been developed. The antitumor properties of these chemotypes are compared with those exhibited by the corresponding carbocyclic analogues. The sensitivity of the expressed cytotoxicities on the position(s) of the nitrogen atom(s) are discussed in terms of potential cellular targets. Several analogues show potential for clinical evaluations.

Published
1995

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