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

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