通过偶氮点击/钉合方法鉴定能有效抑制急性髓系白血病细胞系的新型FLT3抑制剂。
Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach.
作者信息
Ma Xiaochu, Zhou Jie, Wang Changhao, Carter-Cooper Brandon, Yang Fan, Larocque Elizabeth, Fine Jonathan, Tsuji Genichiro, Chopra Gaurav, Lapidus Rena G, Sintim Herman O
机构信息
Institute for Drug Discovery, Department of Chemistry, Purdue University Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, United States.
Department of Chemistry and Biochemistry, University of Maryland, College Park, Maryland 20742, United States.
出版信息
ACS Med Chem Lett. 2017 Apr 14;8(5):492-497. doi: 10.1021/acsmedchemlett.6b00468. eCollection 2017 May 11.
Abstract
Acute myeloid leukemia (AML) is an aggressive malignancy with only a handful of therapeutic options. About 30% of AML patients harbor mutated FLT3 kinase, and thus, this cancer-driver has become a hotly pursued AML target. Herein we report a new class of FLT3 inhibitors, which potently inhibit the proliferation of acute myeloid leukemia (AML) cells at nanomolar concentrations.
摘要
急性髓系白血病（AML）是一种侵袭性恶性肿瘤，治疗选择有限。约30%的AML患者携带FLT3激酶突变，因此，这种癌症驱动因子已成为热门的AML治疗靶点。在此，我们报告了一类新型的FLT3抑制剂，它们在纳摩尔浓度下就能有效抑制急性髓系白血病（AML）细胞的增殖。
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