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Synthesis and Biological Evaluation of Benzo [d][1, 3] Dioxol‐5‐yl Chalcones as Antiproliferating Agents

Publication Type : Journal Article

Publisher : Chemical biology & drug design

Source : Chemical biology & drug design, Vol. 86, pp. 1267-1284, 2015.

Url : https://pubmed.ncbi.nlm.nih.gov/26032623/

Campus : Kochi

School : School of Pharmacy

Department : Pharmaceutical Chemistry & Analysis

Year : 2015

Abstract : A series of chalcone derivatives were designed, synthesized, and evaluated for their cytotoxic potential. These molecules have showed promising cytotoxic activity with IC50 values ranging from 5.24 to 63.12 μm. Among them, conjugates 16k, 16m and 16t showed significant antiproliferative activity with IC50 values ranging from 5.24 to 10.39 μm in MDA-MB-231 cell line. These compounds were further investigated for their effect on cell membrane blebbing, chromatin condensation, DNA fragmentation, Hoechst staining, annexin V, and cell cycle arrest (G2/M). The Western blot experiments revealed up regulation of pro-apoptotic Bax and downregulation of antiapoptotic Bcl-2. The studies also indicated reduction of mitochondrial membrane potential and increase in the levels of caspase-3 and caspase-7.

Cite this Research Publication : Kamal, A.; Balakrishna, M.; Loka Reddy, V.; Riyaz, S.; Bagul, C.; Satyanarayana, B. M.; Venkateswar Rao, J. Synthesis and Biological Evaluation of Benzo [d][1, 3] Dioxol‐5‐yl Chalcones as Antiproliferating Agents. Chemical biology & drug design, Vol. 86, pp. 1267-1284, 2015

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