Discovery of benzylisothioureas as potent divalent metal transporter 1 (DMT1) inhibitors

…, M Chafeev, S Chowdhury, N Chakka, J Sun…

文献索引：Zhang, Zaihui; Kodumuru, Vishnumurthy; Sviridov, Serguei; Liu, Shifeng; Chafeev, Mikhail; Chowdhury, Sultan; Chakka, Nagasree; Sun, Jianyu; Gauthier, Simon J.; Mattice, Maryanne; Ratkay, Laszlo G.; Kwan, Rainbow; Thompson, Jay; Cutts, Alison Brownlie; Fu, Jianmin; Kamboj, Rajender; Goldberg, Y. Paul; Cadieux, Jay A. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 15 p. 5108 - 5113

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被引用次数: 7

摘要

Inhibition of intestinal brush border DMT1 offers a novel therapeutic approach to the prevention and treatment of disorders of iron overload. Several series of diaryl and tricyclic benzylisothiourea compounds as novel and potent DMT1 inhibitors were discovered from the original hit compound 1. These compounds demonstrated in vitro potency against DMT1, desirable cell permeability properties and a dose-dependent inhibition of iron uptake in an ...