Zhang, Long published the artcileDiscovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer, Computed Properties of 6950-53-4, the publication is European Journal of Medicinal Chemistry (2013), 833-841, database is CAplus and MEDLINE.
To develop potent dual EGFR/HER-2 inhibitors with improved druggability, a series of new lapatinib analogs were designed and synthesized. Compared with lapatinib, L-2, 6-(5-((2-(Sulfamoyl)ethylamino)methyl)furan-2-yl)-N-(4-(3-fluorobenzyloxy)-3-chlorophenyl) quinazolin-4-amine (L-4) and 1-(4-((5-(4-(3-Chloro-4-(3-fluorobenzyloxy)phenylamino) quinazolin-6-yl)furan-2-yl)methyl)piperazin-1-yl)ethanone (M-6) were more active against BT-474 or NCI-N87 cells. In vivo efficacy studies indicated that L-2 significantly suppressed tumor growth in NCI-N87 (94.8% inhibition) or SK-OV-3 xenograft (85.7% inhibition) without causing significant loss of body weight And the inhibition rates of lapatinib in the two xenograft models were 89.7% and 78.8%, resp. Moreover, further studies revealed that the potent in vivo activities of L-2 may be mainly attributed to its superior aqueous solubility and oral bioavailability. In addition, a high-yielding one-pot procedure was developed for the synthesis of lapatinib and its analogs.
European Journal of Medicinal Chemistry published new progress about 6950-53-4. 6950-53-4 belongs to catalysis-chemistry, auxiliary class Salt,sulfides,Amine,Aliphatic hydrocarbon chain, name is 2-(Methylthio)ethanamine hydrochloride, and the molecular formula is C13H19Br2ClN2O, Computed Properties of 6950-53-4.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia