833475-85-7Relevant academic research and scientific papers
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors
Stevens, Kirk L.,Alligood, Krystal J.,Alberti, Jennifer G. Badiang,Caferro, Thomas R.,Chamberlain, Stanley D.,Dickerson, Scott H.,Dickson, Hamilton D.,Emerson, Holly K.,Griffin, Robert J.,Hubbard, Robert D.,Keith, Barry R.,Mullin, Robert J.,Petrov, Kimberly G.,Gerding, Roseanne M.,Reno, Michael J.,Rheault, Tara R.,Rusnak, David W.,Sammond, Douglas M.,Smith, Stephon C.,Uehling, David E.,Waterson, Alex G.,Wood, Edgar R.
scheme or table, p. 21 - 26 (2009/04/10)
A novel class of pyrrolidinyl-acetyleneic thieno[3,2-d]pyrimidines has been identified which potently inhibit the EGFR and ErbB-2 receptor tyrosine kinases. Synthetic modifications of the pyrrolidine carbamate moiety result in a range of effects on enzyme and cellular potency. In addition, the impact of the absolute stereochemical configuration on cellular potency and oral mouse pharmacokinetics is described.
