Yarim Mine, Koksal Meric, Durmaz Irem, Atalay Rengul
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yeditepe University, 34755, Kayisdagi, Istanbul, Turkey.
Department of Molecular Biology and Genetics, BilGen, Genetics and Biotechnology Research Center, Faculty of Science, Bilkent University, 06800, Bilkent, Ankara, Turkey.
Int J Mol Sci. 2012;13(7):8071-8085. doi: 10.3390/ijms13078071. Epub 2012 Jun 28.
A series of novel 1-(4-substitutedbenzoyl)-4-(4-chlorobenzhydryl)piperazine derivatives 5a-g was designed by a nucleophilic substitution reaction of 1-(4-chlorobenzhydryl)piperazine with various benzoyl chlorides and characterized by elemental analyses, IR and (1)H nuclear magnetic resonance spectra. Cytotoxicity of the compounds was demonstrated on cancer cell lines from liver (HUH7, FOCUS, MAHLAVU, HEPG2, HEP3B), breast (MCF7, BT20, T47D, CAMA-1), colon (HCT-116), gastric (KATO-3) and endometrial (MFE-296) cancer cell lines. Time-dependent cytotoxicity analysis of compound 5a indicated the long-term in situ stability of this compound. All compounds showed significant cell growth inhibitory activity on the selected cancer cell lines.
通过1-(4-氯二苯甲基)哌嗪与各种苯甲酰氯的亲核取代反应设计了一系列新型的1-(4-取代苯甲酰基)-4-(4-氯二苯甲基)哌嗪衍生物5a-g，并通过元素分析、红外光谱和(1)H核磁共振光谱对其进行了表征。在来自肝癌（HUH7、FOCUS、MAHLAVU、HEPG2、HEP3B）、乳腺癌（MCF7、BT20、T47D、CAMA-1）、结肠癌（HCT-116）、胃癌（KATO-3）和子宫内膜癌（MFE-296）的癌细胞系上证明了这些化合物的细胞毒性。化合物5a的时间依赖性细胞毒性分析表明该化合物具有长期的原位稳定性。所有化合物对所选癌细胞系均显示出显著的细胞生长抑制活性。
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