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Design, synthesis, docking and mechanistic studies of new thiazolyl/thiazolidinylpyrimidine-2,4-dione antiproliferative agents

مؤلف البحث
1- Ashraf A. Aly, Mohammed B. Alshammari, Akil Ahmad, Hesham A. M. Gomaa, Bahaa G. M. Youssif, Stefan Brase, Mahmoud A. A. Ibrahim, Asmaa H. Mohamed
مجلة البحث
Arabian Journal of Chemistry
الناشر
Science Direct
تصنيف البحث
Medicinal Chemistry (Q1)
عدد البحث
16
سنة البحث
2023
المشارك في البحث
ملخص البحث

In this article, we display on the synthesis and biological evaluation of a new series of
thiazolylpyrimidine 3a-l and thiazolidinylpyrimidine derivatives 5a-e. The structures of the new
compounds were confirmed by using different spectral techniques including NMR, IR, mass spectroscopy
in addition to elemental analyses. The cell viability of the new compounds was assessed
against normal human mammary gland epithelial (MCF-10A) cell line. Data revealed that none
of the compounds examined exhibited cytotoxic effects, and the cell viability for the compounds
examined at 50 mM was greater than 87%. The antiproliferative activity of 3a-l and 5a-e was evaluated
against four human cancer cell lines where the compounds showed promising activity. The
most potent derivatives were compounds 3a, 3c, 3f, 3i, and 5b with GI50 values ranging from