Structurally Simple Phenanthridine Analogues Based on Nitidine and Their Antitumor Activities

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 bromid...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2019-01, Vol.24 (3), p.437
Main Authors: Qin, Shu-Qin, Li, Lian-Chun, Song, Jing-Ru, Li, Hai-Yun, Li, Dian-Peng
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antitumor activity
Benzophenanthridines - chemistry
Cancer
Cell Line, Tumor
Chloride
Cytotoxicity
Dose-Response Relationship, Drug
Humans
Inhibitory Concentration 50
nitidine
Phenanthridine
Phenanthridines - chemical synthesis
Phenanthridines - chemistry
Phenanthridines - pharmacology
phenanthridinone
Structure-Activity Relationship
Toxicity testing
Tumor cell lines
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Summary: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 , , and , with IC values of 1.20 μM, 1.87 μM, and 1.19 μM against CNE1 cells, respectively, were more active than nitidine chloride. Compound and compound with IC values of 1.19 μM and 1.37 μM against HepG2 cells and A549 cells demonstrated superior activities to nitidine. Besides, compound which had a phenanthridinone core displayed extraordinary cytotoxicity against all test cells, particularly against CNE1 cells with the IC value of 1.13 μM.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules24030437