Küçükgüzel, Şükriye GünizHan, M. IhsanBaysal, Ozge Deniz YesilBasaran, Guzide SatirSezer, GulayTelci, DilekKucukguzel, S. GunizEczacılık Meslek Bilimleri Bölümü2025-01-112025-01-112022130040-40201464-541610.1016/j.tet.2022.1327972-s2.0-85130334037https://doi.org/10.1016/j.tet.2022.132797https://hdl.handle.net/20.500.14627/94Han, Muhammed Ihsan/0000-0001-5610-0869In this study, a series of the novel Tetracaine derivatives bearing hydrazide-hydrazone moiety were designed, synthesized, and evaluated for anticancer activity. The structures of these compounds were characterized by spectral (H-1-C-13 NMR, FT-IR, and HR-MS analyses) methods. All synthesized compounds (2a-1) were screened for anticancer activity against human hepatocellular carcinoma (HepG2) and lung carcinoma (A549) cell lines. Against HepG2 and A549 cell lines, among the synthesized compounds, 4-(Butylamino)-N'-[(2,4-dichlorophenyl)methylidene]benzohydrazide (2i) demonstrated the most potent anticancer activity with IC50 values 28 and 7 mu M, respectively. Possible cytotoxic effects of compounds (2a-1) on both normal human lung fibroblast (MCR-5) and normal human dermal fibroblast (HDF) cell lines were assessed. Inhibition of anti-apoptotic protein Bax and Bcl-2 was investigated in HepG2 and A549 cells treated with compound 2i using qRT-PCR. Apoptosis was also detected by Annexin V studies. The flow cytometric analysis results showed that compound 2i treatment of HepG2 and A549 cells significantly increased apoptotic cell populations while decreasing viabilities in these carcinomas in a dose-dependent manner after 72 h of incubation. (C) 2022 Elsevier Ltd. All rights reserved.eninfo:eu-repo/semantics/closedAccessTetracaineHydrazide-HydrazoneAnticancer ActivityQrt-PcrAnnexin VArticleQ3Q3115WOS:000832692800007