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Stereoselective synthesis of beta-lactams with polyaromatic imines: entry to new and novel anticancer agents
Indrani Banik1, Frederick F Becker, Bimal K Banik
1The University of Texas M. D. Anderson Cancer Center, Department of Molecular Pathology, Box 89, 1515 Holcombe Boulevard, Houston, Texas 77030, USA.
Abstract:
We present herein stereoselective synthesis of novel beta-lactams using polyaromatic imines following the Staudinger reaction. Consistent mechanisms for these results have been advanced. As a measure of cytotoxicity, some of these compounds have been assayed against nine human cancer cell lines. Structure-activity study has revealed that 1-N-chrysenyl and 1-N-phenanthrenyl 3-acetoxy-4-aryl-2-azetidinones have potent anticancer activity. The presence of the acetoxy group at C(3) of the beta-lactams has proven to be obligatory for their anticancer activity.
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