ChemInform Abstract: Synthesis and in vitro Cytotoxicity of C(20)(RS)‐Camptothecin Analogues Modified at Both B (or A) and E Ring.

Abstract

Synthesis and in vitro Cytotoxicity of C(20)(RS)-CamptothecinAnalogues Modified at Both B (or A) and E Ring.-Modifications of camptothecin are carried out with the aim to increase the in vitro cytotoxicity. Substituents at both B and E ring reduce the desired activity, cf. (V), whereas the both A and E substitution enhance this activity, cf.(VII) and (IX). All compounds are isolated as racemates, the investigation of chiral forms of derivatives (VII) and (IX) is in progress. -(JEW, S.; KIM, M. G.; KIM, H.-J.; RHO, E.-Y.; PARK, H.; KIM, J.-K.; HAN, H.-J.; LEE, H.; Bioorg. Med.