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Synthesis and antitumor activity of novel N-(5-benzyl-4-(tert-butyl)thiazol-2-yl)-2-(piperazin-1-yl)acetamides

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成果类型:
期刊论文
作者:
Wu, Zhilin;Ding, Na;Tang, Yuting;Ye, Jiao;Peng, Junmei;Hu, Aixi*
通讯作者:
Hu, Aixi
作者机构:
[Ye, Jiao; Ding, Na; Peng, Junmei; Wu, Zhilin; Tang, Yuting; Hu, Aixi] Hunan Univ, Coll Chem & Chem Engn, Changsha, Hunan, Peoples R China.
[Wu, Zhilin] Univ South China, Sch Chem & Chem Engn, Hengyang, Hunan, Peoples R China.
[Peng, Junmei] Univ South China, Inst Pharm & Pharmacol, Hengyang, Hunan, Peoples R China.
通讯机构:
[Hu, Aixi] Hunan Univ, Coll Chem & Chem Engn, Changsha, Hunan, Peoples R China.
语种:
英文
关键词:
Antitumor activity;Cell cycle;Double staining;Piperazinylacetamide;Thiazole
期刊:
Research on Chemical Intermediates
ISSN:
0922-6168
年:
2017
卷:
43
期:
8
页码:
4833-4850
机构署名:
本校为其他机构
院系归属:
化学化工学院
药学与生物科学学院
摘要:
A series of novel N-(5-benzyl-4-(tert-butyl) thiazol-2-yl)-2-(piperazin-1-yl)acetamides were designed, synthesized and evaluated for their antitumor activities in vitro. The structures of the synthesized compounds were characterized by<sup>1</sup>H NMR,<sup>13</sup>C NMR and elemental analysis. In general, compounds 5a, 5c and 6a showed potent antiproliferative activity against HeLa (human cervical cancer) and A549 (human lung cancer) cell lines. Compound 6a, with the best inhibitory activity against HeLa cells (IC<inf>50</inf>&nbsp;=&nbsp;1.6&nbsp;&plusmn;&nbsp;0.8&nbsp;&mu;M), was selected to investigate the induced changes of cell morphology in the HeLa cell line by means of acridine orange (AO)/ethidium bromide (EB) double staining and cell cycle analysis using flow cytometry. The results indicated that compound 6a could induce cell apoptosis and cause G1-phase arrest in the cell division cycle. &copy;2017, Springer Science+Business Media Dordrecht.

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