Cha, Mi Young; Lee, Kwang-Ok; Kim, Jong Woo; Lee, Chang Gon; Song, Ji Yeon; Kim, Young Hoon; Lee, Gwan Sun; Park, Seung Bum; Kim, Maeng Sup published the artcile< Discovery of A Novel Her-1/Her-2 Dual Tyrosine Kinase Inhibitor for the Treatment of Her-1 Selective Inhibitor-Resistant Non-Small Cell Lung Cancer>, SDS of cas: 115843-99-7, the main research area is tyrosine kinase inhibitor quinazolinyl pyrrolidine preparation SAR.
A novel series of (S)-1-acryloyl-N-[4-(arylamino)-7-(alkoxy)quinazolin-6-yl]pyrrolidine-2-carboxamides were synthesized and evaluated as Her-1/Her-2 dual inhibitors. In contrast to the Her-1 selective inhibitors, our novel compounds are irreversible inhibitors of Her-1 and Her-2 tyrosine kinases with the potential to overcome clin. relevant, mutation-induced drug resistance. The selected compounds, 19c and 19d (I), showed excellent EGFR inhibition activity even toward the T790M mutation of Her-1 tyrosine kinase with excellent selectivity. The excellent pharmacokinetic profiles of these compounds in rats and their robust in vivo efficacy in an A431 xenograft model clearly demonstrate that they merit further investigation as novel therapeutic agents for EGFR-targeting treatment of solid tumors, especially Her-1 selective inhibitor-resistant non-small cell lung cancer.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 115843-99-7 belongs to class bromides-buliding-blocks, and the molecular formula is C6H4BrClFN, SDS of cas: 115843-99-7.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary