SYNTHESIS AND ANTILEUKEMIC ACTIVITY OF (+)__--20-DEOXYAMINOCAMPTOTHECIN ANALOGUES

概要

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The camptothecin analogues (+)__--7-ethyl 10-methoxy-20-deoxyaminocamptothecin (2) and (+)__--7-ethyl-10-hydroxy-20-deoxyaminocamptothecin・HCl (3) were synthesized from indolizine compound 4 via Friedlander condensation to construct a pentacyclic ring system, and were tested in a P388 mouse antileukemia assay. Compounds 2 and 3 were more active and less toxic than (+)-camptothecin (1), and therefore had higher therapeutic ratios.
公益社団法人日本薬学会の論文
1989-08-25