Synthesis and evaluation of 4/5-hydroxy-2, 3-diaryl (substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents

…, R Verma, P Rajendran, S Dutt, G Singh…

Index: Gurjar, Mukund K.; Wakharkar, Radhika D.; Singh, Anu T.; Jaggi, Manu; Borate, Hanumant B.; Shinde, Popat D.; Verma, Ritu; Rajendran, Praveen; Dutt, Sarjana; Singh, Gurvinder; Sanna, Vinod K.; Singh, Manoj K.; Srivastava, Sanjay K.; Mahajan, Vishal A.; Jadhav, Vinod H.; Dutta, Kakali; Krishnan, Karthik; Chaudhary, Anika; Agarwal, Shiv K.; Mukherjee, Rama; Burman, Anand C. Journal of Medicinal Chemistry, 2007 , vol. 50, # 8 p. 1744 - 1753

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Citation Number: 28

Abstract

A new series of 2, 3-diaryl-4/5-hydroxy-cyclopent-2-en-1-one analogues replacing the cis double bond of combretastatin A-4 (CA-4) by 4/5-hydroxy cyclopentenone moieties was designed and synthesized. The analogues displayed potent cytotoxic activity (IC50< 1 μg/mL) against a panel of human cancer cell lines and endothelial cells. The most potent analogues 11 and 42 belonging to the 5-hydroxy cyclopentenone class were further ...