2. Academic Validation
  3. Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11β-hydroxydehydrogenase 1 (11β-HSD1)

Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11β-hydroxydehydrogenase 1 (11β-HSD1)

  • Bioorg Med Chem Lett. 2011 Nov 15;21(22):6693-8. doi: 10.1016/j.bmcl.2011.09.058.
Shung C Wu 1,  David Yoon,  Janice Chin,  Katy van Kirk,  Ramakrishna Seethala,  Rajasree Golla,  Bin He,  Thomas Harrity,  Lori K Kunselman,  Nathan N Morgan,  Randolph P Ponticiello,  Joseph R Taylor,  Rachel Zebo,  Timothy W Harper,  Wenying Li,  Mengmeng Wang,  Lisa Zhang,  Bogdan G Sleczka,  Akbar Nayeem,  Steven Sheriff,  Daniel M Camac,  Paul E Morin,  John G Everlof,  Yi-Xin Li,  Cheryl A Ferraro,  Kasia Kieltyka,  Wilson Shou,  Marianne B Vath,  Tatyana A Zvyaga,  David A Gordon,  Jeffrey A Robl
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Research & Development, PO Box 5400, Hopewell, NJ 08534-5400, USA. shung.wu@bms.com
PMID: 21983444 DOI: 10.1016/j.bmcl.2011.09.058
Abstract

Derived from the HTS hit 1, a series of hydroxyisoquinolines was discovered as potent and selective 11β-HSD1 inhibitors with good cross species activity. Optimization of substituents at the 1 and 4 positions of the isoquinoline group in addition to the core modifications, with a special focus on enhancing metabolic stability and aqueous solubility, resulted in the identification of several compounds as potent advanced leads.

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