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

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

  • Bioorg Med Chem Lett. 2006 Jul 15;16(14):3639-41. doi: 10.1016/j.bmcl.2006.04.071.
Shenlin Huang 1,  Peter J Connolly,  Ronghui Lin,  Stuart Emanuel,  Steve A Middleton
Affiliations

Affiliation

  • 1 Johnson & Johnson Pharmaceutical Research & Development LLC, 1000 Route 202, Raritan, NJ 08869, USA. [email protected]
PMID: 16682186 DOI: 10.1016/j.bmcl.2006.04.071
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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