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.