Synthesis of anticancer β-lactams: mechanism of action

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• 作者：Banik ; Bimal K. ; Becker ; Frederick F. ; Banik ; Indrani
• 关键词：β ; -Lactams ; Anticancer agents ; Cell cycle ; Apoptosis
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2004
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：May 15, 2004
• 卷：12
• 期：10
• 页码：2523-2528
• 文件大小：282 K

摘要

Synthesis of the trans 1-N-chrysenyl and 1-N-phenanthrenyl 3-acetoxy-4-phenyl-2-azetidinones has been achieved. Microwave-assisted reaction has proved useful in the synthesis of these compounds. Cell growth inhibition study has indicated selective anticancer activity against two leukemia and colon carcinoma cell lines. A mechanistic correlation of their anticancer activity has been described. Striking G₂ blockade that is clearly distinct in cell cycle analysis and demonstrated only in sensitive cell lines has been observed. They do not induce apoptosis in sensitive or resistant lines. They also do not inhibit topoisomerases. Ames test has shown they are nonmutagenic.