Design, Synthesis, and Anticancer Activity of Novel Trimethoxyphenyl-Derived Chalcone-Benzimidazolium Salts | |
Yang, Jun-Li1,2; Ma, Yong-Hui1; Li, Yan-Hua2; Zhang, Yi-Peng1; Tian, Hong-Chang1; Huang, Yuan-Cheng1; Li, Yan3; Chen, Wen1; Yang, Li-Juan2 | |
Corresponding Author | Chen, Wen(chenwenchem@163.com) ; Yang, Li-Juan(yangljyang@sina.com) |
2019-12-03 | |
Source Publication | ACS OMEGA |
ISSN | 2470-1343 |
Volume | 4Issue:23Pages:20381-20393 |
Abstract | A series of novel trimethoxyphenyl-derived chalcone-benzimidazolium salts were synthesized. The biological properties of the compounds were screened in vitro against five different human tumor cell lines. The results suggest that the 5,6-dimethyl-benzimidazole or 2-methyl-benzimidazole ring as well as the 2-naphthylmethyl, 4-methylbenzyl, or 2-naphthylacyl substituent at position-3 of the benzimidazole ring was important to the cytotoxic activity. Notably, (E)-5,6-dimethy1-3-(naphth alen-2-ylmethyl)-1-(3-(4-(3-(3,4,5-trime thoxyphenyl) a cryloyl) phenoxy)propyl)-1H-benzo [d] imidazol-3-ium bromide (7f) was more selective to HL-60, MCF-7, and SW-480 cell lines with IC50 values 8.0-, 11.1-, and 5.8-fold lower than DDP. Studies of the antitumor mechanism of action showed that compound 7f could induce cell-cycle G1 phase arrest and apoptosis in SMMC-7721 cells. |
DOI | 10.1021/acsomega.9b03077 |
Indexed By | SCI ; SCI |
Language | 英语 |
WOS ID | WOS:000502128300033 |
Citation statistics | |
Document Type | 期刊论文 |
Identifier | http://ir.kib.ac.cn/handle/151853/70592 |
Collection | 植物化学与西部植物资源持续利用国家重点实验室 |
Corresponding Author | Chen, Wen; Yang, Li-Juan |
Affiliation | 1.Yunnan Univ, Sch Chem Sci & Technol, Key Lab Med Chem Nat Resources, Minist Educ & Yunnan Prov, Kunming 650091, Yunnan, Peoples R China 2.Yunnan Minzu Univ, Engn Res Ctr Green Preparat Technol Biobased Mat, Sch Chem & Environm, Kunming 650500, Yunnan, Peoples R China 3.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650204, Yunnan, Peoples R China |
Recommended Citation GB/T 7714 | Yang, Jun-Li,Ma, Yong-Hui,Li, Yan-Hua,et al. Design, Synthesis, and Anticancer Activity of Novel Trimethoxyphenyl-Derived Chalcone-Benzimidazolium Salts[J]. ACS OMEGA,2019,4(23):20381-20393. |
APA | Yang, Jun-Li.,Ma, Yong-Hui.,Li, Yan-Hua.,Zhang, Yi-Peng.,Tian, Hong-Chang.,...&Yang, Li-Juan.(2019).Design, Synthesis, and Anticancer Activity of Novel Trimethoxyphenyl-Derived Chalcone-Benzimidazolium Salts.ACS OMEGA,4(23),20381-20393. |
MLA | Yang, Jun-Li,et al."Design, Synthesis, and Anticancer Activity of Novel Trimethoxyphenyl-Derived Chalcone-Benzimidazolium Salts".ACS OMEGA 4.23(2019):20381-20393. |
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