Synthesis of 1,2,4-triazole and 1,3,4-oxadiazole derivatives as inhibitors for STAT3 enzymes of breast cancer.

Autor: Fawzy SM; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sinai University, Kantara Branch, Al-Ismailia, Egypt., Loksha YM; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sinai University, Al-Arish Branch, North Sinai, Egypt., El-Sadek M; Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt., Ibrahim SM; Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt., Beshay BY; Department of Pharmaceutical Chemistry, College of Pharmacy, Arab Academy for Science, Technology and Maritime Transport, Alexandria, Egypt., Shamaa MM; Department of Biochemistry, Clinical and Biological Sciences Division, College of Pharmacy, Arab Academy for Science, Technology and Maritime Transport, Alexandria, Egypt., Kothayer H; Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.
Jazyk: angličtina
Zdroj: Archiv der Pharmazie [Arch Pharm (Weinheim)] 2023 Nov; Vol. 356 (11), pp. e2300345. Date of Electronic Publication: 2023 Sep 03.
DOI: 10.1002/ardp.202300345
Abstrakt: Disubstituted five-membered heterocycles (1,2,4-triazole and 1,3,4 oxadiazole) were synthesized and investigated as inhibitors for signal transducer and activator of transcription 3 (STAT3) enzyme of breast cancer. 3-(Benzylthio)-5-(4-chlorobenzyl)-4H-1,2,4-triazol-4-amine (12d) was found to be the most active among the synthesized compounds with a half-maximal inhibitory concentration (IC 50 ) value of 1.5 µM on MCF7 cells and was found to show a great inhibitory effect on the STAT3 enzyme. Compounds 9a,b,d,e,f, 11, and 12a,b,f,e show IC 50 values in the range of 3-12 µM for the MCF7 cell line. Molecular modeling was used to investigate the biological results of the synthesized compounds.
(© 2023 Deutsche Pharmazeutische Gesellschaft.)
Databáze: MEDLINE
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