70338-47-5Relevant articles and documents
Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
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, (2015/12/18)
A pharmaceutical formulation comprising the compound of formula
Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series
Petrov, Kimberly G.,Zhang, Yue-Mei,Carter, Malcolm,Cockerill, G. Stuart,Dickerson, Scott,Gauthier, Cassandra A.,Guo, Yu,Mook Jr., Robert A.,Rusnak, David W.,Walker, Ann L.,Wood, Edgar R.,Lackey, Karen E.
, p. 4686 - 4691 (2007/10/03)
Synthetic modifications on a 6-furanylquinazoline scaffold to optimize the dual ErbB-1/ErbB-2 tyrosine kinase inhibition afforded consistent SAR whereby a 4-(3-fluorobenzyloxy)-3-haloanilino provided the best enzyme potency and cellular selectivity. Changes made to the 6-furanyl group had little impact on the enzyme activity, but appeared to dramatically affect the cellular efficacy. The discovery of lapatinib emerged from this work.
Synthesis and properties of nuclear hydroxylated derivatives of flufenamic acid and etofenamate
Boltze,Backer,Kreisfeld
, p. 183 - 186 (2007/10/02)
Synthesis of six nuclear hydroxylated derivatives of flufenamic acid and etofenamate (5-OH-, 4'-OH and 5,4'-(OH2) on a preparative scale is described. All compounds show low toxicity, by only weak anti-inflammatory activity in the rat paw kaolin edema test as compared to 2-(2-hydroxyethoxy)ethyl-N-(α,α,α-trifluoro-m-tolyl)-anthranilate (etofenamate, active substance of Rheumon Gel).