Synthesis of bisindolylmaleimides related to GF109203x and their efficient conversion to the bioactive indolocarbazoles.
From a structure-activity relationship perspective, the new indolocarbazoles 11 and 12 have been synthesized and evaluated biologically as novel Chk1 inhibitors. Compounds 11 and 12 were synthesized in high yield from indole via bisindolylmaleimides 18 and 24.
Roy
Sudipta
S
Department of Chemistry, Dartmouth College, Hanover, NH 03755, USA.
Eastman
Alan
A
Gribble
Gordon W
GW
D000478:Alkylation; D002227:Carbazoles / Q000737:chemistry*; D002453:Cell Cycle; D004249:DNA Damage; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008301:Maleimides / Q000138:chemical synthesis / Q000737:chemistry*; D008958:Models, Molecular; D008968:Molecular Conformation
D002227:Carbazoles; D007211:Indoles; D008301:Maleimides; C070515:bisindolylmaleimide I