Bioorganic & medicinal chemistry letters

Discovery of structurally simplified analogs of colchicine as an immunosuppressant

DJ Chang, WJ Kim

文献索引：Chang, Dong-Jo; Kim, Wan-Joo Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 14 p. 3121 - 3125

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被引用次数: 1

摘要

Abstract We have discovered a new class of colchicine-derived therapeutic agents for immune diseases including rejection of organ-transplantation and autoimmune disease. Compound 2, which had been developed to overcome poor pharmacokinetic properties of compound 1, a first-generation colchicine analog, turned out to show toxicity such as intestinal toxicity and loss of weight during in vivo tests. The deletion of 7-carboxamide ...