title: Synthesis and biological evaluation of benzo[d][1,3]dioxol-5-yl chalcones as antiproliferating agents.
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.
authors.affiliation: Medcinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology, Hyderabad, 500007, India.|Biomaterials Group, CSIR- Indian Institute of Chemical Technology, Hyderabad, 500007, India.
authors.forename: Ahmed
authors.initials: A
authors.lastname: Kamal
authors.affiliation: Medcinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology, Hyderabad, 500007, India.
authors.forename: Moku
authors.initials: M
authors.lastname: Balakrishna
authors.affiliation: Biology Division, CSIR- Indian Institute of Chemical Technology, Hyderabad, 500007, India.
authors.forename: Velatooru
authors.initials: V
authors.lastname: Loka Reddy
authors.affiliation: Medcinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology, Hyderabad, 500007, India.
authors.forename: Syed
authors.initials: S
authors.lastname: Riyaz
authors.affiliation: Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Hyderabad, 500037, India.
authors.forename: Chandrakant
authors.initials: C
authors.lastname: Bagul
authors.affiliation: Biology Division, CSIR- Indian Institute of Chemical Technology, Hyderabad, 500007, India.
authors.forename: Bethu Murali
authors.initials: BM
authors.lastname: Satyanarayana
authors.affiliation: Biology Division, CSIR- Indian Institute of Chemical Technology, Hyderabad, 500007, India.
authors.forename: Janapala
authors.initials: J
authors.lastname: Venkateswar Rao
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001940:Breast / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D053148:Caspase 3 / Q000378:metabolism; D053179:Caspase 7 / Q000378:metabolism; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D005260:Female; D006801:Humans
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones; D053148:Caspase 3; D053179:Caspase 7
keywords: antiproliferative activity; apoptosis; caspase-3 and caspase-7; cell cycle arrest; chalcones