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3,5-Disubstituted Thiadiazine-2-thiones: New Cell-Cycle Inhibitors
Awwad A. Radwan,Tarek Aboul-Fadl,Abdullah Al-Dhfyan,Mohammed K. Abdel-Hamid,Abdullah A. Al-Badr 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.1
Two series, a and b, of 3-cyclopentyl or (3-cyclohexyl)-5-substituted-3,4,5,6-tetrahydro-2H-1,3,5-thiadiazine-2-thiones (THTT) 2a-9a and 3b, 4b, 6b-9b, were synthesized to develop new cell cycle inhibitors. Variable and promising in vitro antiproliferative activities were shown with the synthesized THTT derivatives. Compound 5a with a 5-cyclopentyl group on position-3 and a glutamine residue on position-5 of the THTT moiety showed maximum activity (IC50 = 8.98 μM). Compound 5a possessed notable cell cycle disrupting and apoptotic activities with enhanced selectivity against cancer cells, suggesting the potential for the development of new selective cell cycle inhibitors. There is no evident relationship between the cytotoxic activity of the tested compounds and their lipophilicity. In addition, a pharmacophore based study was performed to explain the biological activity on structural bases. A successful model was generated with a good correlation with the observed activity.
Hatem A. Abdel-Aziz,Tarek Aboul-Fadl,Abdul-Rahman M. Al-Obaid,Mohamed Ghazzali,Abdullah Al-Dhfyan,Alessandro Contini 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.9
Novel 6-aryl-2-methylnicotinic acid hydrazides 4a-c and their corresponding hydrazones 5a-c and 6a-i were synthesized. X-ray single crystal diffraction of 6h confirmed the chemical structure of hydrazones 6a-i. Antiproliferative activity of the synthetic compounds was investigated against K562 leukemia cell lines. Variable cell growth inhibitory activities were obtained with IC50 range from 24.99 to 66.78 μM where the compound 6c exhibited the maximum activity. Structure activity relationship analysis has been performed and a common pharmacophore model for the synthesized derivatives has been obtained by using the pharmacophore elucidation module of the software MOE. The best model obtained is characterized by two projected locations of potential H-bond donors (F3 and F4) and two Aromatic annotations (F1 and F2).