Thiazole and oxazole are compounds with a heterocyclic nucleus that have attracted the attention of medicinal chemistry due to the great variety of biological activities that they enable. In recent years, their study has increased, finding a wide range of biological activities, including antifungal, antiparasitic, anti-inflammatory, and anticancer activities. This systematic review provides evidence from the literature on the antiproliferative and antitumor activities of thiazole and oxazole and their derivatives from 2014 to April 2020. Three bibliographical databases were consulted (PubMed, Web of Science, and Scopus), and a total of 32 studies were included in this paper based on our eligibility criteria. The analysis of the activity-structure relationship allows us to conclude that most of the promising compounds identified contained thiazole nuclei or derivatives.
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http://dx.doi.org/10.1016/j.biopha.2021.111495 | DOI Listing |
Bioorg Chem
December 2024
Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran. Electronic address:
In the current study, a novel series of 1,2,4-oxadiazoles were designed, synthesized, and evaluated for their biological activities. A cell-based antiproliferative screening was accomplished on the newly synthesized 1,2,4-oxadiazoles along with our previously reported aryl(alkyl)azoles (AAAs) containing middle heterocyclic cores thiazole and oxazole. Among the tested compounds, naphthyl- thiazoles demonstrated higher antiproliferative activity and B3 was identified as the most potent compound with IC values in the range of 2.
View Article and Find Full Text PDFJ Agric Food Chem
January 2025
State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, PR China.
To discover novel inhibitors of pyruvate kinase (PK) as fungicidal candidates, a series of 2-thiazol-2-yl-1,3,4-oxadiazole derivatives were designed by a prediction model with PK (RsPK) as a protein target and as a ligand. Fungicidal screening indicated that , , , , , , , and exhibited equal or higher activity compared to against , , or . To our surprise, showed comparable activity to flutriafol with an EC of 0.
View Article and Find Full Text PDFChem Asian J
December 2024
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education & Research (NIPER), Sector 67, S. A. S., Nagar, Punjab, 160 062, India.
Ru(II)-Catalyzed "On Water" direct aryl C(sp)-H amidation of 2-arylbenzo[d]-thiazole/oxazole with acyl azide is reported under silver-free condition. Deuterium scrambling experiments suggested reversible C-H activation catalyzed by active cationic ruthenium species. The organic solvents such as DCE, DMF, DMSO, MeCN, dioxane, and PhMe were not conducive for the C-H amidation except for PhCl in which case, however, inferior yield (31 %) was obtained.
View Article and Find Full Text PDFMicrobiol Resour Announc
January 2025
Ecology & Environment, Scion, Christchurch, New Zealand.
sp. Ash2021 is a free-living soil bacterium isolated from a forest in Canterbury, New Zealand. The genome comprises of a 9,328,819 bp chromosome and a 375,468 bp plasmid.
View Article and Find Full Text PDFDalton Trans
December 2024
Key Laboratory of Optoelectronic Chemical Materials and Devices of Ministry of Education, School of Optoelectronic Materials and Technologies, Jianghan University, Wuhan 430056, P. R. China.
Two novel mononuclear palladium(II) complexes, [PdL1Cl]Cl (1) and [PdL2Cl]Cl (2) with SNS-donor ligands [where L1 = -(4-(benzo[]oxazol-2-yl)phenyl)-2-(bis(2-ethylthioethyl)amino)acetamide, L2 = -(4-(benzo[]thiazol-2-yl)phenyl)-2-(bis(2-ethylthioethyl)amino)acetamide], were synthesized and characterized. antiproliferative activity tests showed that the two palladium(II) complexes displayed excellent antiproliferative activity against all tested cancer cell lines, especially human colon cancer HCT-116, human liver cancer HepG-2, and human breast cancer MDA-MB-231 cells. Spectacularly, complexes 1 and 2 exhibited approximately 8.
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