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Synthetic approaches to indolo[6,7-a]pyrrolo[3,4-c]carbazoles: potent cyclin D1/CDK4 inhibitors.

Authors :
Faul MM
Engler TA
Sullivan KA
Grutsch JL
Clayton MT
Martinelli MJ
Pawlak JM
LeTourneau M
Coffey DS
Pedersen SW
Kolis SP
Furness K
Malhotra S
Al-awar RS
Ray JE
Source :
The Journal of organic chemistry [J Org Chem] 2004 Apr 30; Vol. 69 (9), pp. 2967-75.
Publication Year :
2004

Abstract

Synthesis of indolo[6,7-a]pyrrolo[3,4-c]carbazoles 1, a new class of cyclin D1/CDK4 inhibitors, by oxidation of the corresponding aryl indolylmaleimides 2, will be described. Two approaches to the synthesis of 2 were identified that required new methods for the synthesis of 7-substituted indole acetamides 3 and N-methyl (indol-7-yl)oxoacetates 6. The chemistry developed enabled introduction of functionality (-OR, NR(2)) at C(12) and N(13) facilitating structure-activity relationship (SAR) evaluation of this indolocarbazole platform.

Details

Language :
English
ISSN :
0022-3263
Volume :
69
Issue :
9
Database :
MEDLINE
Journal :
The Journal of organic chemistry
Publication Type :
Academic Journal
Accession number :
15104433
Full Text :
https://doi.org/10.1021/jo035606v