A series of quinazoline clubbed 1,3,5-triazine derivatives (QCT) were synthesized and evaluated for their in vitro anticancer activity against HeLa (human cervical cancer), MCF-7 (human breast cancer cell), HL-60 (human promyelocytic leukemia cell), HepG2 (human Hepatocellular carcinoma cell), and one normal cell line HFF (human foreskin fibroblasts). In vitro assay result encouraged to further move towards in ovo anticancer evaluation using chick embryo. The series of QCT derivatives showed higher anticancer and antiangiogenic activity against HeLa and MCF-7 cell lines. In the series, synthetic molecule 8d, 8l, and 8m displayed significant activity. Further, these results substantiated by docking study on VGFR2. SAR study concluded that the potency of drugs depends on the nature of aliphatic substitution and the heterocyclic ring system.
Four series of 20 novel derivatives of benzylidene camphor with hydrazones, semicarbazones, and thiosemicarbazones were designed and synthesized. The newly synthesized compounds were evaluated for their anticonvulsant activity by maximal electroshock seizure model. Compounds showed varying degrees of anticonvulsant activity, most marked effect was observed for compounds 2f and 4d with lesser neurotoxicity. Molecular docking studies of most active compounds (2f and 4d) of the series revealed that they interact with LYS329A, GLN 301A, and THR 353B residues of 1OHV protein via hydrogen bonding and Pi interaction.
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