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Design, Synthesis, and Biological Evaluation of a New Series of 2,4-Position Modified Pyrimidine Derivatives.

Authors :
Chen, L.
Yao, Z. D.
Chen, Y.
Zhao, L.
Source :
Russian Journal of Bioorganic Chemistry. Apr2024, Vol. 50 Issue 2, p604-616. 13p.
Publication Year :
2024

Abstract

–Objective: In this paper, a series of piperazine pyrimidines and morpholine pyrimidines have been synthesized effectively, and their biological activities have been evaluated. Methods: We examined the cytotoxicity tests of the compounds against two human tumor cells (HCT-116, HeLa), as well as one human normal cells (L02), in order to determine their anticancer activity. Results: The compound (IV) outperformed the others, and flow cytometry was used to further examine how it works against cancer. Additionally, the (IV) molecule showed strong anticancer efficacy but was marginally less effective in apoptosis assays than the control 5-FU. Discussion: The compound (IV) chemical treated HCT-116 cells and HeLa cells in the cell cycle research had a larger percentage of cells in the G1 phase. The induction of apoptosis by interfering with the cell cycle may be the anticancer mechanism of this substance. Additionally, molecular docking investigated potential interactions between the substances and the Topo II active site. Conclusions: The groundwork for the creation and structural modification of new pyrimidine medications is laid out in this study. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
10681620
Volume :
50
Issue :
2
Database :
Academic Search Index
Journal :
Russian Journal of Bioorganic Chemistry
Publication Type :
Academic Journal
Accession number :
176498781
Full Text :
https://doi.org/10.1134/S1068162024020092