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

Chem Pharm Bull (Tokyo). 1989 Aug;37(8):2253-5. doi: 10.1248/cpb.37.2253.

Abstract

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 Friedländer 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.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Camptothecin / analogs & derivatives*
  • Camptothecin / chemical synthesis
  • Camptothecin / pharmacology
  • Leukemia P388 / drug therapy
  • Mice

Substances

  • Antineoplastic Agents
  • 7-ethyl-10-hydroxy-20-deoxyaminocamptothecin
  • 7-ethyl-10-methoxy-20-deoxyaminocamptothecin
  • Camptothecin