Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621 |
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Authors: | Huang Shenlin Connolly Peter J Lin Ronghui Emanuel Stuart Middleton Steve A |
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Affiliation: | Johnson & Johnson Pharmaceutical Research & Development LLC, 1000 Route 202, Raritan, NJ 08869, USA. shenlinhuang@hotmail.com |
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Abstract: | 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. |
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