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Stereoselective synthesis of β-lactams with polyaromatic imines:: Entry to new and novel anticancer agents

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JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 1, 页码 12-15

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AMER CHEMICAL SOC
DOI: 10.1021/jm0255825

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  1. NCI NIH HHS [5-P30-CA16672-25] Funding Source: Medline

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We present herein stereoselective symthesis of novel beta-lactams using polyaromatic imines following the Staudinger reaction. Consistent mechanisms for these results have been advanced. As a measure of cytotaxicity, 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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