1257653-85-2Relevant academic research and scientific papers
Synthesis of imidazothiazole-chalcone derivatives as anticancer and apoptosis inducing agents
Kamal, Ahmed,Dastagiri,Ramaiah, M. Janaki,Reddy, J. Surendranadha,Bharathi, E. Vijaya,Srinivas, Chatla,Pushpavalli,Pal, Dhananjaya,Pal-Bhadra, Manika
, p. 1937 - 1947 (2011/06/20)
A new class of imidazo[2,1-b]thiazole chalcone derivatives were synthesized and evaluated for their anticancer activity. These chalcone derivatives show promising activity, with logGI50 values ranging from -7.51 to -4.00. The detailed biological aspects of these derivatives toward the MCF-7 cell line were studied. Interestingly, these chalcone derivatives induced G 0/G1-phase cell-cycle arrest, down-regulation of G 1-phase cell-cycle regulatory proteins such as cyclin D1 and cyclin E1, and up-regulation of CDK4. Moreover, these compounds elicit the characteristic features of apoptosis such as enhancement in the levels of p53, p21, and p27, suppression of NF-κB, and up-regulation of caspase-9. One of these chalcone derivatives, 3d, is potentially well suited for detailed biological studies, either alone or in combination with existing therapies. Breaking the cycle: We undertook an extensive examination of the ability of a series of new chalcone derivatives to regulate the cell cycle and to induce apoptosis in various cancer cell lines. Compound 3d is a particularly suitable candidate for further detailed biological investigations, especially in the treatment of breast cancer.
