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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Pyrrolocarbazoles as Checkpoint 1 Kinase Inhibitors

Author(s): Helene Henon, Elisabeth Conchon, Bernadette Hugon, Samir Messaoudi, Roy M. Golsteyn and Michelle Prudhomme

Volume 8, Issue 6, 2008

Page: [577 - 597] Pages: 21

DOI: 10.2174/187152008785133100

Price: $65


The carbazole framework is found in many natural compounds of biological interest. Indolocarbazoles such as rebeccamycin and staurosporine which are either a topoisomerase I inhibitor (rebeccamycin) or a non selective kinase inhibitor (staurosporine) are bacterial metabolites. In the search for new antitumor agents, DNA damage checkpoint kinases, in particular Checkpoint kinase 1, have recently emerged as attractive targets for cancer therapy. This review reports the synthesis and Chk1 inhibitory activities of pyrrolocarbazole compounds bearing four or five fused rings.

Keywords: Checkpoint kinase 1, antitumor agents, pyrrolocarbazole, granulatimide

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