Synthesis and biological evaluation of novel thiazol-2yl-amine derivatives as potential anticancer agents

Chaithanya, S. and Hegde, Mahesh and Sharath Kumar, K. S. and Ananda, H. and Mrinal, Srivastava and Harsha, K. B. and Mohan, C. D. and Kavya Ananthaswamy and Basappa and Raghavan, S. C. and Rangappa, K. S. (2018) Synthesis and biological evaluation of novel thiazol-2yl-amine derivatives as potential anticancer agents. Letters in Organic Chemistry, 15 (4). pp. 270-281. ISSN 1875-6255

Full text not available from this repository. (Request a copy)
Official URL: https://doi.org/10.2174/1570178614666170907122026

Abstract

Background: Chronic myelogenous leukemia (CML) is a myeloproliferative neoplasm that can occur in any age group but often seen in adults and contributing for about 20% of adult leukemias and it may contribute up to 15% of all types of leukemias threatening the globe. Therefore, treatment of CML remains as a major challenge in cancer therapeutics. Methods: We synthesized a library of novel 2-amino-4-(4-substituted phenyl) thiazole derivatives and evaluated their anti-leukemic activity by trypan blue and MTT assay. 4-(4'-phenoxybiphenyl-4-yl) thiazol- 2-amine (compound 3m) was identified as a lead anticancer agent and further, the effect of 3m on CML cells (K562) was investigated by flow cytometry, annexin V-FITC-propidium iodide staining, measuring the mitochondrial membrane potential (JC-1 staining) and DNA fragmentation assay. Results: MTT and trypan blue dye exclusion assay results presented 3m as the lead anticancer agent. Flow cytometric analysis revealed the accumulation of K562 cells in subG1phase in a time- and dosedependent manner. Annexin-V-FITC-PI staining demonstrated the increase in percentage of apoptotic cells on treatment with 3m. Furthermore, 3m also induced DNA fragmentation and disrupted mitochondrial membrane potential in K562 cells in dose-dependent manner. In addition, apoptosis inducing effect of 3m was reconfirmed by live-dead assay and confocal microscopic studies. Conclusion: The present study suggests that compound 3m has the potential to be a promising candidate for the treatment of CML.

Item Type: Article
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: manjula User
Date Deposited: 26 Jul 2019 10:26
Last Modified: 26 Jul 2019 10:26
URI: http://eprints.uni-mysore.ac.in/id/eprint/5939

Actions (login required)

View Item View Item