Romanian Society of Pharmaceutical Sciences
 

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HETEROCYCLES 45. SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-INDOLYL-1-PYRIDYL-2-PROPENONES AS ANTICANCER AGENTS

JUSTIN KAMGA 1,2, DENISA LEONTE 2, PANTALEON AMBASSA 1, ARMELLE T. MBAVENG 3,5, GHISLAIN W. FOTSO 1, FANA-MARIA COMAN 2, BONAVENTURE T. NGADJUI 1,4, VICTOR KUETE 3,5, VALENTIN ZAHARIA 2*, BATHELEMY NGAMENI 4

1.Department of Organic Chemistry, University of Yaounde I, P.O. Box 812, Yaounde, Cameroon
2 .Department of Organic Chemistry, “Iuliu Haţieganu” University of Medicine and Pharmacy, 41 Victor Babeş Street, 400012, Cluj-Napoca, Romania
3 .Department of Biochemistry, University of Dschang, P.O. Box 67, Dschang, Cameroon
4 .Department of Pharmacognosy and Pharmaceutical Chemistry, University of Yaounde I, P.O. Box 1364, Yaounde, Cameroon
5 .Institute of Pharmacy and Biochemistry, Therapeutical Life Sciences, 55128, Mainz, Germany

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A series of seven 3-indolyl-1-pyridyl-2-propenones were synthesized via Claisen-Schmidt condensation with 68.8-91.8% yields. All the synthesized compounds were purified and characterized by melting points, IR, 1H NMR, 13C NMR and HRMS. The cytotoxicity of the synthesized 3-indolyl-1-pyridyl-2-propenones 1-7 and doxorubicin, used as positive control, was determined in a panel of nine human cancer cell lines including both sensitive and drug-resistant phenotypes, as well as in normal AML12 hepatocytes. Compounds 3, 4 and 7 displayed half maximal inhibitory concentration (IC50) values below 100 µM in all tested cancer cell lines meanwhile, other compounds displayed selective activities.