Design, Synthesis, and In Vitro Antiproliferative Activity of 4,5,6-Trisubstituted 2-Aminopyrimidines as Potential TGF-β Inhibitors.

Autor: Sachkova, A. A., Rysina, Yu. D., Svirshchevskaya, E. V., Grishin, I. D., Fedorov, A. Yu., Shchegravina, E. S.
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Zdroj: Russian Journal of Organic Chemistry; Apr2024, Vol. 60 Issue 4, p672-683, 12p
Abstrakt: Signaling proteins involved in the TGF-β (transforming growth factor beta) pathway regulate cellular processes such as cell growth, division, differentiation, migration, invasion, and apoptosis. Due to the large contribution of the TGB-β signaling pathway to carcinogenesis, these proteins are promising oncotargets. Based on the literature data, we propose a new structural type of TGF-β receptor inhibitors that are 2-amino-pyrimidine derivatives. Two general approaches to their synthesis have been proposed, where the key step is the three-component Biginelli condensation producing the pyrimidine fragment. Sixteen new compounds have been synthesized, and their in vitro antiproliferative activity has been evaluated against a panel of tumor cell lines. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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