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Synthesis of some quinolinyl chalcone analogues and investigation of their anticancer and synergistic anticancer effect with doxorubicin |
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| Authors: | Mohamed R E Aly El-Sayed I Ibrahim Fakher A El Shahed Hamdy A Soliman Zein S Ibrahim Samir A M El-Shazly |
| Institution: | 1. Chemistry Department, Faculty of Science, Taif University, 888, Alhawyah-Taif, Kingdom of Saudi Arabia 7. Chemistry Department, Faculty of Applied Science, Port Said University, Port Said, Egypt 2. Chemistry Department, Faculty of Science, Suez Canal University, Ismailia, Egypt 3. Physiology Department, Faculty of Medicine, Taif University, Taif, KSA 5. Department of Physiology, Faculty of Veterinary Medicine, KaferelSheikh University, KaferelSheikh, Egypt 4. Biotechnology Department, Faculty of Science, Taif University, Taif, KSA 6. Department of Biochemistry, Faculty of Veterinary Medicine, KaferelSheikh University, KaferelSheikh, Egypt |
| Abstract: | Two derivatives of 2-(4-acetylanilino)quinolines (IIIa, b) were synthesized as scaffolds for synthesis of open chalcone analogues (Va-f) through Claisen-Schmidt condensation with a set of aromatic aldehydes (IVa-d). Derivatives (Va, b) were further manipulated into cyclic ??,??-unsaturated ketones by Michael-addition of acetylacetone and ethylacetoacetate affording derivatives (VI?CVII). Deethoxycarboxylation of derivatives (VIIa, b) afforded cyclohexenons (VIIIa, b) allowing formation of a mini library of ??,??-unsaturated ketones for screening their anticancer and synergistic anticancer effect with doxorubicin using colon cancer cell line (Caco-2). Two open enones, (Vb) and (Ve), showed significant anticancer activity with IC50 of 5.0 and 2.5 ??M respectively. Only one cyclic enone, (VIa) showed synergistic anticancer activity with doxorubicin at 10 ??M. |
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