Browsing by Author "Baviskar, Ashish T."

Now showing 1 - 3 of 3
  • Thumbnail Image
    Item
    Imine/amide-imidazole conjugates derived from 5-amino-4-cyano-N1-substituted benzyl imidazole: Microwave-assisted synthesis and anticancer activity via selective topoisomerase-II-? inhibition
    (Elsevier Ltd, 2015) Negi, Arvind; Alex, Jimi Marin; Amrutkar, Suyog M.; Baviskar, Ashish T.; Joshi, Gaurav; Singh, Sandeep; Banerjee, Uttam Chand; Kumar, Raj
    Microwave-accelerated synthesis and anticancer activity of novel imine/amide-imidazole conjugates derived from 5-amino-4-cyano-N1-substituted benzyl imidazole against a panel of seven cancer cell lines are reported for the first time. Compounds ARK-4, 10 and 12 in the series show promising in vitro anti proliferative activity with low micromolar IC 50 values against A-459 (lung), Hep-G2 (liver) and H-460 (liver) cancer cell lines. Compounds caused the increase in ROS levels as well as mitochondrial membrane depolarization, which might induce apoptosis. Further, mechanistic interventions on biological and molecular modeling data supported that compounds inhibited topoisomerase-II selectively.- 2015 Elsevier Ltd. All rights reserved.
  • Thumbnail Image
    Item
    Synthesis and biological evaluation of new 2, 5- dimethylthiophene/furan based N-acetyl pyrazolines as selective topoisomerase II inhibitors
    (Royal Society of Chemistry, 2016) Darpan; Joshi, Gaurav; Amrutkar, Suyog M.; Baviskar, Ashish T.; Kler, Harveen; Singh, Sandeep; Banerjee, Uttam C.; Kumar, Raj
    Based on the reported pharmacophores as topoiomerase inhibitors, 2,5 dimethylthiophen/furan based N-acetyl pyrazolines were designed and envisaged as topoisomerase inhibitors. The target compounds were synthesized and tested in vitro against human topoisomerases in decatenation, relaxation, cleavage complex and DNA intercalation assay. Out of 29 compounds, three (10, 11 and 29) showed potent and selective toposiomerse II inhibitory activity with no intercalation with DNA. Further, molecular docking studies also endorsed them as ATP dependent topoisomerase II catalytic inhibitors. These compounds exerted potential anticancer effects on breast, colon, lung and prostate cancer cell lines at low micromolar level as compared to etoposide and low toxicity to normal cells. Apart from the topoisomerase II inhibition, these compounds also induced the reactive oxygen species (ROS) level in cancer cells. The cell cycle analyses showed their apoptotic effect at G1 phase.
  • Thumbnail Image
    Item
    Synthesis of imine-pyrazolopyrimidinones and their mechanistic interventions on anticancer activity
    (2013) Baviskar, Ashish T.; Banerjee, Uttam C.; Gupta, Mukesh; Singh, Rajveer; Kumar, Sunil; Gupta, Manish K.; Kumar, Sanjeev; Rout, Satish K.; Khullar, Madhu; Singh, Sandeep; Kumar, Raj
    Design, synthesis and anticancer activity of a series of imine-pyrazolopyrimidinones is reported for the first time. Compounds 9d, 9n and 9o in the series show encouraging in vitro anticancer activity with low micromolar IC50 values against prostate (PC3) and breast (MCF7) cancer cell lines. Some notions about structure-activity relationships and plausible mechanism of biological activity are presented. ? 2013 Elsevier Ltd. All rights reserved.