期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 14, 页码 3639-3641出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.04.071
关键词
CDK inhibitor; prodrug
A novel prodrug strategy for cyclin-dependent kinase inhibitor JNJ-7706621 has been explored. Through N-acylation of a sulfonamide substituent, tails containing different solubilizing groups (amino, carboxyl, alkoxyl, and hydroxyl) were attached to JNJ-7706621. Most of the prodrugs exhibited good aqueous solubility and the N-acyl groups on the sulfonamide were metabolically cleaved to generate active drug in rat PK study. (c) 2006 Elsevier Ltd. All rights reserved.
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