Design and development of 9,10-dihydrophenanthrene derivatives as inhibitors of human protein kinase CK2

Haidar S, Meyers A, Jose J

Abstract in digital collection (conference) | Peer reviewed

Abstract

ProteinkinaseCK2isanemergingtargetforthetherapeuticinterventioninhumandiseases,particularlyincancer.Inhibitorsofthisenzymearecurrentlyinclinicaltrials,indicatingthedruggabilityofhumanCK2.Herewereportonthedesignofseveralderivativesof9,10-Dihydrophenanthrenewithdi-substitutedfunctionalgroups,usingamolecularmodelingapproach.TheinhibitoryactivityofthesynthesizedcompoundstowardsCK2wastestedusingacapillaryelectrophoresisin-vitroapproach.Furthermore,breastcancercells(MCF-7)weretreatedwiththedesignedcompoundsandcellviabilitywasdeterminedusingtheMTTassay.MolecularmodelingstudieswereperformedusingMOEsoftwaretounderstandthebindingaffinitiesofthedesignedcompounds.

Details about the publication

StatusPublished
Release year2016
Language in which the publication is writtenEnglish
Conference2nd Electronic Conference on Medicinal Chemistry, Basel, undefined

Authors from the University of Münster

Jose, Joachim
Professur für Pharmazeutische Chemie (Prof. Jose)
Center of Interdisciplinary Sustainability Research (ZIN)