ArticleMolecules (Basel, Switzerland)2022
Development of Novel Pyridine-Thiazole Hybrid Molecules as Potential Anticancer Agents.
Article in Molecules (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 29 citations in OpenAlex.
- A Review of Recent Advances in the Anticancer Mechanisms of Activity of Novel Thiazoles and 4-Thiazolidinones/Thiazolidinediones (2021-2025).Molecules (Basel, Switzerland) · 2026Review
- Development and Biological Assessment of Thiazole-Based Pyridines for Targeted Therapy in Lung Cancer.ACS omega · 2025Article
- Synthesis and Evaluation of Thiazolyl-indole-2-carboxamide Derivatives as Potent Multitarget Anticancer Agents.ACS omega · 2024Article
- Applications of Pyrrole and Pyridine-based Heterocycles in Cancer Diagnosis and Treatment.Current pharmaceutical design · 2024Review
- Synthesis, In Vitro Evaluation and Molecular Docking Studies of Novel Thiophenyl Thiazolyl-Pyridine Hybrids as Potential Anticancer Agents.Molecules (Basel, Switzerland) · 2023Article
- Nitrogen Containing Heterocycles as Anticancer Agents: A Medicinal Chemistry Perspective.Pharmaceuticals (Basel, Switzerland) · 2023Review
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Authors and funding
16 authors at 5 institutions in 2 countries.
Funding
Abstract
Novel pyridine-thiazole hybrid molecules were synthesized and subjected to physico-chemical characterization and screening of their cytotoxic action towards a panel of cell lines derived from different types of tumors (carcinomas of colon, breast, and lung, glioblastoma and leukemia), and normal human keratinocytes, for comparison. High antiproliferative activity of the 3-(2-fluorophenyl)-1-[4-methyl-2-(pyridin-2-ylamino)-thiazol-5-yl]-propenone 3 and 4-(2-{1-(2-fluorophenyl)-3-[4-methyl-2-(pyridin-2-ylamino)-thiazol-5-yl]-3-oxopropylsulfanyl}-acetylamino)-benzoic acid ethyl ester 4 was revealed. The IC50 of the compound 3 in HL-60 cells of the acute human promyelocytic leukemia was 0.57 µM, while in the pseudo-normal human cell lines, the IC50 of this compound was >50 µM, which suggests that the compounds 3 and 4 might be perspective anticancer agents. The detected selectivity of the derivatives 3 and 4 for cancer cell lines inspired us to study the mechanisms of their cytotoxic action. It was shown that preincubation of tumor cells with Fluzaparib (inhibitor of PARP1) reduced the cytotoxic activity of the derivatives 3 and 4 by more than twice. The ability of these compounds to affect DNA nativity and cause changes in nucleus morphology allows for the suggestion that the mechanism of action of the novel pyridine-thiazole derivatives might be related to inducing the genetic instability in tumor cells.
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