title: Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).
abstract: A high throughput screen of Abbott's compound repository revealed that the pyrazolo[3,4-d]pyrimidine class of kinase inhibitors possessed moderate potency for IGF-IR, a promising target for cancer chemotherapy. The synthesis and subsequent optimization of this class of compounds led to the discovery of 14, a compound that possesses in vivo IGF-IR inhibitory activity.
authors: Cancer Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. robert.d.hubbard@abbott.com
authors: Robert D
authors: RD
authors: Hubbard
authors: Nwe Y
authors: NY
authors: Bamaung
authors: Fabio
authors: F
authors: Palazzo
authors: Qian
authors: Q
authors: Zhang
authors: Peter
authors: P
authors: Kovar
authors: Donald J
authors: DJ
authors: Osterling
authors: Xiaoming
authors: X
authors: Hu
authors: Julie L
authors: JL
authors: Wilsbacher
authors: Eric F
authors: EF
authors: Johnson
authors: Jennifer
authors: J
authors: Bouska
authors: Jieyi
authors: J
authors: Wang
authors: Randy L
authors: RL
authors: Bell
authors: Steven K
authors: SK
authors: Davidsen
authors: George S
authors: GS
authors: Sheppard
mesh_terms: D000284:Administration, Oral; D000818:Animals; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D007275:Injections, Intravenous; D051379:Mice; D010766:Phosphorylation; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D017451:Receptors, Somatomedin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D011720:Pyrazoles; D011743:Pyrimidines; D017451:Receptors, Somatomedin; C014175:pyrazolo(3,4-d)pyrimidine; D020794:Receptor Protein-Tyrosine Kinases