一些丙烯酰苯与N-甲基哌嗪的合成及其细胞毒性评估。
Synthesis of some acrylophenones with N-methylpiperazine and evaluation of their cytotoxicities.
作者信息
Gul Halise Inci, Tugrak Mehtap, Sakagami Hiroshi
机构信息
a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Ataturk University , Erzurum , Turkey and.
b Division of Pharmacology , Meikai University School of Dentistry , Sakado , Saitama , Japan.
出版信息
J Enzyme Inhib Med Chem. 2016;31(1):147-51. doi: 10.3109/14756366.2015.1014474. Epub 2015 Feb 20.
In this study, the compounds having acrylophenone structure, 1-aryl-2-(N-methylpiperazinomethyl)-2-propen-1-one dihydrochlorides, were synthesized and their chemical structures were identified with (1)H NMR, (13)C NMR and HRMS spectra. The cytotoxicities of the compounds were tested towards Ca9-22 (human gingival carcinoma), HSC-2 (human oral squamous carcinoma), HSC-3 (human oral squamous carcinoma) and HSC-4 (human oral squamous carcinoma) cell lines as tumor cell lines and HGF (gingival fibroblasts), HPLF (periodontal ligament fibroblasts) and HPC (pulp cells) cell lines as non-tumor cell lines. PSE of the compound TA2, which has a methyl substituent on phenyl ring, pointed out the compound TA2 as a leader compound to be considered.
在本研究中，合成了具有丙烯酰苯结构的化合物1-芳基-2-(N-甲基哌嗪甲基)-2-丙烯-1-酮二盐酸盐，并通过(1)H NMR、(13)C NMR和HRMS光谱对其化学结构进行了鉴定。测试了这些化合物对Ca9-22（人牙龈癌）、HSC-2（人口腔鳞状癌）、HSC-3（人口腔鳞状癌）和HSC-4（人口腔鳞状癌）细胞系等肿瘤细胞系以及HGF（牙龈成纤维细胞）、HPLF（牙周膜成纤维细胞）和HPC（牙髓细胞）细胞系等非肿瘤细胞系的细胞毒性。在苯环上具有甲基取代基的化合物TA2的PSE指出化合物TA2是一个值得考虑的先导化合物。
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