1. Structurally Simple Phenanthridine Analogues Based on Nitidine and Their Antitumor Activities
- Author
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Dian-Peng Li, Song Jingru, Qin Shuqin, Li Haiyun, and Lian-Chun Li
- Subjects
phenanthridine ,Pharmaceutical Science ,Antineoplastic Agents ,Conjugated system ,Article ,Analytical Chemistry ,lcsh:QD241-441 ,03 medical and health sciences ,chemistry.chemical_compound ,Inhibitory Concentration 50 ,Structure-Activity Relationship ,0302 clinical medicine ,lcsh:Organic chemistry ,Cell Line, Tumor ,Drug Discovery ,Humans ,antitumor activity ,Physical and Theoretical Chemistry ,Cytotoxicity ,IC50 ,030304 developmental biology ,A549 cell ,Benzophenanthridines ,0303 health sciences ,Nitidine ,Phenanthridine ,Dose-Response Relationship, Drug ,Organic Chemistry ,phenanthridinone ,Combinatorial chemistry ,In vitro ,Phenanthridines ,chemistry ,Chemistry (miscellaneous) ,Cell culture ,030220 oncology & carcinogenesis ,Molecular Medicine ,nitidine - Abstract
A series of novel structurally simple analogues based on nitidine was designed and synthesized in search of potent anticancer agents. The antitumor activity against human cancer cell lines (HepG2, A549, NCI-H460, and CNE1) was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay in vitro. The results showed that some of them had good anticancer activities, especially derivatives with a [(dimethylamino)ethyl]amino side chain in the C-6 position. Planar conjugated compounds 15a, 15b, and 15c, with IC50 values of 1.20 &mu, M, 1.87 &mu, M, and 1.19 &mu, M against CNE1 cells, respectively, were more active than nitidine chloride. Compound 15b and compound 15c with IC50 values of 1.19 &mu, M and 1.37 &mu, M against HepG2 cells and A549 cells demonstrated superior activities to nitidine. Besides, compound 5e which had a phenanthridinone core displayed extraordinary cytotoxicity against all test cells, particularly against CNE1 cells with the IC50 value of 1.13 &mu, M.
- Published
- 2019