Synthesis and Antitumor Evaluation of Novel 5-Hydrosulfonyl-1H-benzo[d]imidazol-2(3H)-one Derivatives
| Autor: | Guang Ouyang, Rongsheng Tong, Jinqi Li, Lan Bai, Liang Ouyang, Xingmei Duan, Fengqiong Li, Pin He, Jianyou Shi, Yuxin He |
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| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: | |
| Zdroj: | Molecules, Vol 21, Iss 4, p 516 (2016) |
| Druh dokumentu: | article |
| ISSN: | 1420-3049 21040516 |
| DOI: | 10.3390/molecules21040516 |
| Popis: | A series of novel 5-hydrosulfonyl-1H-benzo[d]imidazol-2(3H)-one derivatives bearing natural product substructures has been successfully synthesized and their antitumor activity studied. These newly synthesized derivatives were characterized by 1H-NMR, 13C-NMR and high resolution mass spectral data, then screened as antitumor agents against the A549, HCC1937, and MDA-MB-468 human tumor cell lines using MTT cell proliferation assays. The results show that some of these compounds can effectively inhibit the growth of these cancerous cells, with compound 5b being the best one (IC50 = 2.6 μM). Flow cytometry data revealed that compound 5b induced apoptosis of HCC1937 cells with increased solution concentration. The structure and activity relationships (SAR) of these compounds is summarized. |
| Databáze: | Directory of Open Access Journals |
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