Synthesis of cis-fused indolocarbazole pyran derivatives as multikinase inhibitors

MEDI 364

Françoise M. Perron-Sierra, françoise.perron@fr.netgrs.com1, Roy Golsteyn1, Nathalie Kucharczyk1, Patrick Casara1, and Céline Boucley2. (1) Medicinal Chemistry, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, France, (2) Finorga, route Givors, Chasse sur Rhône, 38670, France
An efficient scale synthesis of enantiomerically pure N12,N13-pyran-bridged indolocarbazoles is disclosed, starting from an indole-indoline derivative. Functional diversity is presented through 15 examples allowing SAR on FLT3 and Chk1 inhibitory properties. In vitro pharmacological data are presented for the most potent compounds.
 

Poster Session
7:00 PM-9:00 PM, Wednesday, August 22, 2007 BCEC -- Exhibit Hall - B2, Poster

Division of Medicinal Chemistry

The 234th ACS National Meeting, Boston, MA, August 19-23, 2007