计算机科学
CD38
组合化学
数据科学
情报检索
化学
生物
细胞生物学
川地34
干细胞
作者
Stephen S. Scully,Zachary Minden,Ratul Mukerji,Elizaveta Andrianova,James Kaberna,Scott Lentini,Carlos Tassa,Zhaolin Wang,Susan C. Low,Kevin McDonnell
标识
DOI:10.1021/acsmedchemlett.6b00409
摘要
Several monoclonal antibodies and inhibitors targeting CD38, an ectoenzyme overexpressed on malignant plasma cells, have previously been discovered. Herein, we expand structure-activity relationships of reported small-molecule thiazoloquinolinones and show that several 4-cyclohexylamino analogues have potent binding affinity for CD38 using surface plasmon resonance. Moreover, active amine analogues could be acylated and functionalized with alkyne and fluorescein groups. Fluorescein analogue 21 bound selectively to CD38 overexpressing cells, demonstrating the potential utility of thiazoloquinolinones as small-molecule conjugates for the delivery of therapeutic and imaging agents.
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