Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors.

Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors. Research Abstract Details 

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Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors. Abstract Text:

Yasunori Kitano,Tsuyoshi Suzuki,Eiji Kawahara,Takahisa Yamazaki,Yasunori Kitano,Tsuyoshi Suzuki,Eiji Kawahara,Takahisa Yamazaki,

The present study identified several 4-alkynyl and 4-alkenylquinazolines that serve as novel and potent EGFR tyrosine kinase inhibitors. The IC(50) values of these compounds are in the nanomolar range. In addition, the 4-(4-phenylbut-1-yn/en-yl)quinazolines provided scaffolds for potent enzyme inhibition. Chiral discrimination was observed to occur in one of the 4-alkynylquinazoline derivatives with the (R)-isomer being more than 150 times as potent as the (S)-isomer.

Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors. Publishing Authors By Initials

Y Kitano,T Suzuki,E Kawahara,T Yamazaki,Y Kitano,T Suzuki,E Kawahara,T Yamazaki,

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Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 5863-7

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 0960-894X

DAY: 15

MONTH: 08

YEAR: 2007

Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors.

AFFILIATION: Mitsubishi Pharma Corporation, Pharmaceuticals Research Division, 1000, Kamoshida-cho, Aoba-ku, Yokohama 227-0033, Japan. Kitano.Yasunori@mc.mt-pharma.co.jp

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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