Synthesis, Anticancer Activity and Docking of some substituted Benzothiazoles as EGFR Tyrosine Kinase Inhibitors and Topoisomerase II inhibitors
Hygeia.J.D.Med.7 (1) April 2015; 46-56.
Francis M Saleshier*, Sajna Hameed, Jubina Karim, and Mythri.M
Department of Pharmaceutical Chemistry, SRIPMS, Coimbatore, Tamilnadu, India, 641044.
Plan: The present study focuses on the structure based drug design approach for anticancer activity of various substituted benzothiazoles whether as an EGFR TK inhibitor or as topoisomerase inhibitor.
Preface: The development of novel therapeutic agents for the treatment of cancer is of vital importance since the currently available chemotherapeutic agents only provide palliative care. Benzothiazoles are multitarget agents with broad spectrum of biological activity. Topoisomerase II inhibitors are in clinical use as anticancer therapy for decades and works by stabilizing the enzyme induced DNA breaks.
Methodology: Computer aided drug design brings out the molecular study of the enzymes and the various other targets, it opens the new world of drug discovery into a target specific path of a drug towards disease. The Insilico method mainly includes the target selection, selection of lead and the lead optimization.
Outcome: Docking results confirmed the possibility of benzothiazole moiety possessing the anticancer activity. The structure was finally characterized by UV, IR, NMR and Mass spectra. In the present work the tumorigenic cell line activity of the substituted benzothiazole is compared with the two standard drugs Gefitinib and Doxorubicin by an Invitro assay against Dalton’s Lymphoma Ascites cell using trypan blue dye and percentage inhibition was calculated.
Keywords: Drug design Substituted Benzothiazoles, EGFR tyrosine kinase inhibitor, topoisomerase II inhibitor Anti-cancer activity
Francis M Saleshier, Sajna Hameed, and Jubina Karim, Mythri.M. Synthesis, anticancer activity and docking of some substituted benzothiazoles as egfr tyrosine kinase inhibitors and topoisomerase ii inhibitors. Hygeia.J.D.Med.7 (1) April 2015; 46-56. Available from http://www.hygeiajournal.com