Editor-in-Chief Hatice Kübra Elçioğlu Vice Editors Levent Kabasakal Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy Articles in Press
Synthesis and in vitro anticancer activity of some new hydrazide-hydrazones derived from articaine
Sevgi KARAKUŞ1,Fatih TOK2,Burçin İrem ABAS3,Elif TÜTÜNCÜ2,Nigar Kübra KALKAN2,Sevda TÜRK4,Özge ÇEVİK3
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, İstanbul Aydın University, 34295 İstanbul, Türkiye
2Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, 34854 İstanbul, Türkiye
3Department of Biochemistry, School of Medicine, Aydın Adnan Menderes University, 09010 Aydın, Türkiye
4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Karadeniz Technical University, 61000 Trabzon, Türkiye
DOI : 10.29228/jrp.2022.00 In this study, synthesis of some new hydrazone derivatives based on articaine was carried out. MDA-MB- 231 (triple negative human breast cancer cells) and HUVEC (human umbilical vein endothelial cells) cells were used to investigate the cytotoxic activity of hydrazone compounds. Induction of apoptosis and cell viability were assessed by AnnexinV-PI binding levels and Bax-Bcl2 gene expression levels. Inhibitory activities of the compounds against carbonic anhydrase enzyme were also evaluated. Compounds 2b and 2m exhibited the highest cytotoxic activity against MDAMB- 231 cells with IC50 values of 16.62±1.18 μM and 18.56±2.36 μM, respectively. Similarly, the CA inhibition of 2b and 2m was also determined to be the highest in the series. Keywords : Hydrazone; Articaine; breast cancer; carbonic anhydrase; bax
Marmara University