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Synthesis and Biological Evaluation of Novel Thiazol-2yl-amine Derivatives as Potential Anticancer Agents

Somu, Chaithanya and Hegde, Mahesh and Kumar, Kothanahally S. Sharath and Hanumappa, Ananda and Srivastava, Mrinal and Harsha, Kachigere B and Mohan, Chakrabhavi D and Ananthaswamy, Kavya and Basappa, and Raghavan, Sathees C and Rangappa, Kanchugarakoppal S (2018) Synthesis and Biological Evaluation of Novel Thiazol-2yl-amine Derivatives as Potential Anticancer Agents. In: LETTERS IN ORGANIC CHEMISTRY, 15 (4). pp. 270-281.

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Official URL: http://dx.doi.org/10.2174/157017861466617090712202...

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 dose-dependent 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: Journal Article
Additional Information: Copy right for the article belong toBENTHAM SCIENCE PUBL LTD, EXECUTIVE STE Y-2, PO BOX 7917, SAIF ZONE, 1200 BR SHARJAH, U ARAB EMIRATES
Department/Centre: Division of Biological Sciences > Biochemistry
Depositing User: Id for Latest eprints
Date Deposited: 03 Apr 2018 18:26
Last Modified: 03 Apr 2018 18:26
URI: http://eprints.iisc.ac.in/id/eprint/59466

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