Mervat H. El-Hamamsy

Harnessing coumarin privilege to achieve potency and selectivity: hypoxia-targeted alkyl coumarin-tethered phenyl quinazolinones as dual hCA IX/HSP90α inhibitors with chemosensitizing activity

A series of alkyl coumarin-tethered phenyl quinazolinones were rationally designed and synthesized as hypoxia-targeted dual hCA IX/HSP90α inhibitors, exhibiting potent, highly selective inhibition of hCA IX (in the nanomolar range), while displaying negligible activity against the off-target isoforms hCA I and II.