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- Title
Design and Synthesis of Some New Quinoline-thiazolidine-2,4-dione-isoxazole Conjugates as EGFR Targeting Agents.
- Authors
Swapna, K.; Kumar, N. Satheesh; Reddy, N. Malla; Ravinder, M.
- Abstract
A series of new quinoline-thiazolidine-2,4-dione-isoxazole conjugates was synthesized and evaluated for in vitro anticancer potency against two breast cancer cell lines, such as MCF-7, MDA-MB231, and the normal cancer cell line MCF-10 A (breast cell line) using erlotinib as a standard drug. (Z)-3-{[5-(4-Methoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione and (Z)-3-{[5-(3,5-dimethoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione showed higher anticancer activities against two cancer cell lines, with IC50 ranging from 3.10 ± 0.43, 2.01 ± 0.03, 3.04 ± 0.05, and 2.00 ± 0.07 μM. Furthermore, (Z)-3-{[5-(4-methoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione, and (Z)-3-{[5-(3,5-dimethoxyphenyl)isoxazol-3-yl]methyl}-5-(quinolin-4-ylmethylene)thiazolidine-2,4-dione displayed more inhibitory activity over tyrosine kinase EGFR when compared with the standard erlotinib.
- Subjects
PROTEIN-tyrosine kinases; CELL lines; MOLECULAR docking; DRUG standards; ANTINEOPLASTIC agents
- Publication
Russian Journal of General Chemistry, 2024, Vol 94, Issue 7, p1758
- ISSN
1070-3632
- Publication type
Article
- DOI
10.1134/S1070363224070193