Leyla Yurttaş*, Ömer Öztürk and Zerrin Cantürk Pages 645 - 655 ( 11 )
Background: In this study, novel ortho-hydroxy N-acyl hydrazone moiety including compounds (3a-l) were designed, based on procaspase activating compound (PAC-1) which is a small molecule known with antitumor activity. The antitumor activity was evaluated on A549 (human lung cancer cell line) and CCD 19Lu (human lung normal cell line).
Methods: Twelve N'-arylidene-2-[4-(methylsulfonyl)piperazin-1-yl]acetohydrazide derivatives (3a-l) were synthesized starting from ethyl 1-piperazinylacetate. All compounds were tested using MTT method and Xcelligence-Real time cell analysis system (RTCA DP) to determine their antitumor activity.
Results: Some physicochemical properties of four active compounds were also predicted using MolSoft, PreADMET and PROTOX software. Four of them, 3h, 3j, 3k and 3l bearing 3-hydroxy, 4-dimethylamino, 2,6-dichloro and 3,4-dichloro substituents in order exhibited selective cytotoxicity.
Conclusion: Eligible values were obtained in the specified ranges as to be an oral/intravenous drug considering the physicochemical calculations.
Lung cancer, hydrazone, Procaspase Activating Compound (PAC-1), real-time cell analysis, physicochemical properties, antitumor activity.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Anadolu University, Eskisehir 26470