The synthesis and evaluation of flexible analogues of the topoisomerase I inhibitor, camptothecin

Bioorganic & Medicinal Chemistry Letters
1994.0

Abstract

A convenient synthesis of camptothecin derivatives has been developed in which the D, or D and C rings are incomplete. This approach includes a general route to quinolines such as 12, and a short synthesis of the key lactone 3. The two components are easily coupled to give camptothecin derivatives 17- 22. The lack of activity of these compounds confirms the importance of the rigid camptothecin nucleus.

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