Design and Synthesis of Novel EGFR Inhibitors with  L ‐Rhamnose–Benzoxazinone Hybrids | Zendy

Zhang Renshuai | Zendy; Chen Shaopeng | Zendy; Wu Guanzhao | Zendy; Wan Shengbiao | Zendy; Jiang Tao | Zendy

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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.

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