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Synthesis and Biological Evaluation of Benzo[ d ][1,3]Dioxol‐5‐yl Chalcones as Antiproliferating Agents
Author(s) -
Kamal Ahmed,
Balakrishna Moku,
Loka Reddy Velatooru,
Riyaz Syed,
Bagul Chandrakant,
Satyanarayana Bethu Murali,
Venkateswar Rao Janapala
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12597
Subject(s) - apoptosis , chalcone , dna fragmentation , cytotoxic t cell , chemistry , annexin , fragmentation (computing) , prophase , cytotoxicity , ic50 , microbiology and biotechnology , cell culture , biochemistry , stereochemistry , biology , programmed cell death , in vitro , ecology , meiosis , gene , genetics
A series of chalcone derivatives were designed, synthesized, and evaluated for their cytotoxic potential. These molecules have showed promising cytotoxic activity with IC 50 values ranging from 5.24 to 63.12 μ m . Among them, conjugates 16k , 16m and 16t showed significant antiproliferative activity with IC 50 values ranging from 5.24 to 10.39 μ m 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.