Synthesis and antileukemic activity of (.+-.)-20-deoxyaminocamptothecin analogues.

Abstract
The camptothecin analogues (.+-.)-7-ethyl-10-methoxy-20-deoxyaminocamptothecin (2) and (.+-.)-7-ethyl-10-hydroxy-20-deoxyaminocamptothecin .cntdot. 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.