Synthesis of 8-hydroxy-2-iminochromene derivatives as selective and potent inhibitors of human carbonyl reductase 1

Author:

Hu Dawei1234,Miyagi Namiki5674,Arai Yuki5674,Oguri Hiroaki5674,Miura Takeshi589104,Nishinaka Toru589104,Terada Tomoyuki589104,Gouda Hiroaki1112134,El-Kabbani Ossama14154,Xia Shuang16234,Toyooka Naoki123416,Hara Akira1718194,Matsunaga Toshiyuki5674,Ikari Akira5674,Endo Satoshi5674ORCID

Affiliation:

1. Graduate School of Innovative Life Science

2. University of Toyama

3. Toyama 930-8555

4. Japan

5. Laboratory of Biochemistry

6. Gifu Pharmaceutical University

7. Gifu 501-1196

8. Faculty of Pharmacy

9. Osaka Ohtani University

10. Osaka 584-8540

11. School of Pharmacy

12. Showa University

13. Tokyo 142-8555

14. Nagoya University Graduate School of Medicine

15. Nagoya 466-8550

16. Graduate School of Science and Technology

17. Faculty of Engineering

18. Gifu University

19. Gifu 501-1193

Abstract

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.

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry

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