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Design and Synthesis of Novel EGFR Inhibitors with L ‐Rhamnose–Benzoxazinone Hybrids
Author(s) -
Zhang Renshuai,
Chen Shaopeng,
Wu Guanzhao,
Wan Shengbiao,
Jiang Tao
Publication year - 2016
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.2463
Subject(s) - chemistry , in vitro , epidermal growth factor receptor , tyrosine kinase , stereochemistry , rhamnose , egfr inhibitors , mass spectrometry , biochemistry , combinatorial chemistry , receptor , chromatography , polysaccharide
Four L ‐rhamnose–benzoxazinone compounds as epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors were designed and synthesized. All structures of the compounds were characterized by 1 H‐NMR, 13 C‐NMR, and high‐resolution mass spectrometry . The inhibition activities of the target compounds for the EGFR tyrosine kinase activity in vitro were determined. Compounds 6a , 6b , 6c , 6d displayed moderate activity in targeting EGFR.