Synthesis and biological evaluation of 5-methyl-4-phenyl thiazole derivatives as anticancer agents

doi:10.1080/10426507.2018.1550642

Paper

Synthesis and biological evaluation of 5-methyl-4-phenyl thiazole derivatives as anticancer agents

Published Feb 22, 2019 · A. Evren, Leyla Yurttaş, Busra Eksellı

Phosphorus, Sulfur, and Silicon and the Related Elements

UNKNOWN SJR score

20

Citations

0

Influential Citations

Full textSemantic Scholar

Abstract

Abstract New N-(5-methyl-4-phenylthiazol-2-yl)-2-(substituted thio)acetamides were synthesized and studied for their anticancer activity. The title compounds were procured by reacting 2-chloro-N-(5-methyl-4-phenylthiazol-2-yl)acetamide with some mercapto derivatives. The structural elucidation of the compounds was performed by 1H-NMR, 13C-NMR and LC-MS/MS spectral data and elemental analyses. The synthesized compounds were investigated for their antitumor activities against A549 human lung adenocarcinoma cells and NIH/3T3 mouse embryoblast cell line for determining their selective cytotoxicity. 2-[(1-methyl-1H-tetrazol-5-yl)thio]-N-(5-methyl-4-phenylthiazol-2-yl)acetamide (4c) showed high selectivity, and whose IC50 value was determined as 23.30 ± 0.35 µM and >1000 µM against A549 human lung adenocarcinoma cells and NIH/3T3 mouse embryoblast cell lines, respectively. 2-[(1-Methyl-1H-imidazol-2-yl)thio]-N-(5-methyl-4-phenyl thiazol-2-yl)acetamide (4a) and 2-[(1-Methyl-1H-tetrazol-5-yl)thio]-N-(5-methyl-4-phenyl thiazol-2-yl)acetamide (4c) exhibited the highest apoptosis percentage among those tested, but not as high as the standard, cisplatin. GRAPHICAL ABSTRACT

In Vitro Study

Study Snapshot

New N-(5-methyl-4-phenylthiazol-2-yl)-2-(substituted thio)acetamides show high selectivity and anticancer activity against A549 human lung adenocarcinoma cells and NIH/3T3 mouse embryoblast

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Sign up to use Study Snapshot

Consensus is limited without an account. Create an account or sign in to get more searches and use the Study Snapshot.

Create an account

Paper

Synthesis and biological evaluation of 5-methyl-4-phenyl thiazole derivatives as anticancer agents

Sign up to use Study Snapshot

References

Osimertinib resistance in non-small cell lung cancer: Mechanisms and therapeutic strategies.

Osimertinib resistance in non-small cell lung cancer can be overcome through additional mutations and alternative kinase activation, requiring novel therapeutic strategies.

Long noncoding RNAs in cancer cells.

Long noncoding RNAs (lncRNAs) play key roles in regulating cancer cell biology and can potentially serve as diagnostic markers and therapeutics in various malignancies.

The Genetic/Non-genetic Duality of Drug 'Resistance' in Cancer.

Drug resistance in cancer involves both genetic and non-genetic mechanisms, and understanding this duality may lead to new treatment strategies.

The role of alternative splicing in cancer drug resistance.

Alternative splicing plays a significant role in cancer drug resistance, and splicing modulation therapy may be a promising approach to combat this resistance.

Synthesis and biological evaluation of novel thiazole- VX-809 hybrid derivatives as F508del correctors by QSAR-based filtering tools.

Novel thiazole-VX-809 hybrid derivatives show promising corrector activity for F508del-CFTR, with potential for further development as CFTR correctors.

Citations