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Bioorg Med Chem Lett. 2006 Jul 15;16(14):3639-41. Epub 2006 May 6.

Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621.

Author information

1
Johnson & Johnson Pharmaceutical Research & Development LLC, 1000 Route 202, Raritan, NJ 08869, USA. shenlinhuang@hotmail.com

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.

PMID:
16682186
DOI:
10.1016/j.bmcl.2006.04.071
[Indexed for MEDLINE]

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