New quinolines substituted with various heterocycles and chalcone moieties were synthesized and evaluated as antitumor agents. All the synthesized compounds were in vitro screened against 60 human cancer cell lines. Compound 13 showed the highest cytotoxicity toward 58 cell lines, exhibiting distinct growth inhibition values (GI 50 ) against the majority of them, including SR, HL-60 (TB) strains (leukemia), and MDA-MB-435 strains (melanoma), with GI 50 values of 0.232, 0.260, and 0.300 µM, respectively. It exhibited great selectivity toward cancer cell lines, with less toxic effect against normal cells represented by skin fibroblast (BJ) and breast epithelial cell lines (MCF-10F). The enzyme inhibitory activity of compound 13 was evaluated against topoisomerase 1 (Topo 1), epidermal growth factor receptor and vascular endothelial growth factor receptor 2, where it displayed worthy Topo 1 inhibition activity with an IC 50 value of 0.278 µM compared with camptothecin as a reference drug (IC 50 0.224 µM). Docking studies were performed to investigate the recognition profile of compound 13 with the Topo 1 enzyme binding site. K E Y W O R D S antitumor activity, chalcones, docking, EGFR, quinolone, Topo 1, VEGFR2
Pyrimidine derivatives R 0510Synthesis of Certain 6-(Arylthio)uracils and Related Derivatives as Potential Antiviral Agents. -New series of 6-(arylthio)uracils (V) and related derivatives such as piperazinylpyrazines (IX) and tricyclic pyrimidine derivatives (VII), (XIII) are synthesized and evaluated for their in vitro antiviral activity as well as cytotoxicity. Arylthiouracils (Vb) and (Vd) exhibit marginal activity against HIV-1. Moreover, compound (Vb) exhibits marginal activity against HSV-1. -(EL-EMAM*, A. A.; MASSOUD, M. A. M.; EL-BENDARY, E. R.; EL-SAYED, M. A.; Bull. Korean Chem.
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