Design and Synthesis of Novel Thiazole Linked Tetrahydropyridine Analogues as Anticancer Agents.

Autor: Mohan Malothu R; Natural Products Laboratory, Department of Chemistry, University College of Science, Osmania University, 500007, Hyderabad, Telangana, India.; Aragen Life Sciences, Nacharam, Hyderabad, Telangana, India., Thalari G; Natural Products Laboratory, Department of Chemistry, University College of Science, Osmania University, 500007, Hyderabad, Telangana, India.
Jazyk: angličtina
Zdroj: Chemistry & biodiversity [Chem Biodivers] 2024 Nov 10, pp. e202402223. Date of Electronic Publication: 2024 Nov 10.
DOI: 10.1002/cbdv.202402223
Abstrakt: A library of new thiazole linked tetrahydropyridines (6a-q) synthesized and screened for their invitro anticancer activity against human breast adeno carcinoma cell viz. MCF-7 and MDA-MB-231. The two compounds 6d containing -F and -Cl functions in para and meta position of phenyl ring (9.94±1.02 μM, 9.78±1.08 μM) and 6e with -Cl and -NH 2 functions on pyridine ring (9.72±0.91 μM, 9.54±0.95 μM) demonstrated outstanding activity against both the cell lines when compared to Doxorubicin. The benzofuran analogue 6o presented good activity with an IC 50 value of 12.19±1.03 μM (MCF-7) and 12.22±1.07 μM (MDA-MB-231). The molecular docking study of potent molecule 6e against crystal structure of breast tumor kinase presented promising docking score and binding interactions. Predicted pharmacokinetics properties of compounds 6a-q and presented boiled diagram of compounds 6d and 6e implied favourable drug-likeness properties.
(© 2024 Wiley-VHCA AG, Zurich, Switzerland.)
Databáze: MEDLINE
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