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Bioorg Med Chem. 2004 May 15;12(10):2523-8.

Synthesis of anticancer beta-lactams: mechanism of action.

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  • 1The University of Texas M.D. Anderson Cancer Center, Department of Molecular Pathology, Unit 89, 1515 Holcombe Boulevard, Houston, TX 77030, USA. bbanik@mail.mdanderson.org


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.

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