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- Title
The effect of heterocyclic substituent at C-3 position of 1-(4-methylpiperazin-1-yl)isoquinolines on their anticancer activity.
- Authors
Konovalenko, A. S.; Zhirnov, V. V.; Shablykin, O. V.; Shablykina, O. V.; Moskvina, V. S.; Brovarets, V. S.
- Abstract
Aim. A comparative analysis of the anti-cancer activity of 1-(4-methylpiperazin-1-yl)isoquinolines with different heteroaromatic substituents in C-3 position: 2-methylthiazol-4-yl, 2-phenylthiazol-4-yl, 2-(pyridin-4-yl)thiazol-4-yl, imidazo[2,1-b]thiazol-6-yl, quinoxalin-2-yl, 6,7-dimethylquinoxalin-2-yl. Methods. Biological tests; statistic methods. Results. In vitro screening of the anticancer activity showed that the derivatives with 2-phenylthiazol-4-yl, quinoxaline-2-yl, 6,7-dimethylquinoxalin-2-yl substituents demonstrated the highest level of anticancer activity; however, they were inferior to 2-(pyridin-4-yl)thiazol-4-yl. The product with the 2-methylthiazol-4-yl residue almost did not demonstrated cytotoxicity. Comparative analysis showed no significant correlation with known drugs; hence these compounds have specific molecular targets. Conclusions. The resulting 1-amino-3-hetarylisoquinolines are a promising class of compounds for anticancer drug development. The level and direction of the activity significantly depend on the nature of heterocyclic substituents.
- Subjects
ANTINEOPLASTIC agents; DRUG target; DOSAGE forms of drugs; DRUG development; ISOQUINOLINE alkaloids; ISOQUINOLINE; TEST methods
- Publication
Biopolymers & Cell, 2022, Vol 38, Issue 1, p37
- ISSN
0233-7657
- Publication type
Article
- DOI
10.7124/bc.000A71