Article
Synthesis of 8-hydroxy-2-iminochromene derivatives as selective and potent inhibitors of human carbonyl reductase 1.
Organic & biomolecular chemistry - 21 Jul 2015
Hu Dawei, Miyagi Namiki, Arai Yuki, Oguri Hiroaki, Miura Takeshi, Nishinaka Toru, Terada Tomoyuki, Gouda Hiroaki, El-Kabbani Ossama, Xia Shuang, Toyooka Naoki, Hara Akira, Matsunaga Toshiyuki, Ikari Akira, Endo Satoshi
Abstract excerpt
Human carbonyl reductase 1 (CBR1), a member of the short-chain dehydrogenase/reductase superfamily, reduces anthracycline anticancer drugs to their less potent anticancer C-13 hydroxy metabolites, which are linked with pathogenesis of cardiotoxicity, a side effect of the drugs. CBR1 inhibitors are thought to be promising agents for adjuvant therapy with a twofold beneficial effect in prolonging the anticancer...
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