Zobrazeno 1 - 3
of 3
pro vyhledávání: '"Wiesia Maniara"'
Autor:
Wrona Wojciech, Deborah J. Davis, Hayley Angove, Christopher Thomas Brain, Alison Jo-Anne Woolford, Fan Yang, Kim Lewry, Hong Cheng, Steven Kovats, Chen Christine Hiu-Tung, Alice Loo, Mei Xu, Claudio Dagostin, Miles Congreve, David C. Rees, John William Giraldes, Yaping Wang, Young Shin Cho, Glyn Williams, Rachel McMenamin, Troy Smith, Junqing Shen, Rajiv Chopra, Ruth Feltell, Yipin Lu, Wiesia Maniara, Bharat Lagu, Steven Howard, Kristy Chung, Robert Cheng, Steven Douglas Hiscock, Sunkyu Kim, Luzzio Michael, Marc O'Reilly, Rajdeep Benning, Paul N. Mortenson
Publikováno v:
ACS Medicinal Chemistry Letters. 3:445-449
Herein, we describe the discovery of potent and highly selective inhibitors of both CDK4 and CDK6 via structure-guided optimization of a fragment-based screening hit. CDK6 X-ray crystallography and pharmacokinetic data steered efforts in identifying
Autor:
Christopher Higgs, Wiesia Maniara, Neil Victor Harris, Sussie L. Krintel, Kenji Namoto, Alokesh Duttaroy, Finton Sirockin, Christopher A. Hurley, Nils Ostermann, Daniel K. Baeschlin, Robert Edward Mackenzie, Eric Gangl, David E. Clark, Garry Fenton, Jörg Trappe, Amanda Fillmore, Ulrich Hassiepen, Stephen J. Dunsdon, Jon Sutton, Richard Sedrani, Bernd Gerhartz
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(3)
Novel deazaxanthine-based DPP-4 inhibitors have been identified that are potent (IC(50)10nM) and highly selective versus other dipeptidyl peptidases. Their synthesis and SAR are reported, along with initial efforts to improve the PK profile through d
Autor:
Christopher A. Hurley, Robert Edward Mackenzie, Christopher Higgs, David E. Clark, Richard Sedrani, Nils Ostermann, Stephen J. Dunsdon, Sussie L. Krintel, Bernd Gerhartz, Neil Victor Harris, Daniel K. Baeschlin, Jon Sutton, Jörg Trappe, Wiesia Maniara, Kenji Namoto, Finton Sirockin, Eric Gangl, Garry Fenton, Amanda Fillmore, Ulrich Hassiepen, Alokesh Duttaroy
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2359