Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.

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Title

Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.

Content partner

The University of Auckland Library

Collection

ResearchSpace@Auckland

Description

Structure−activity relationships for inhibition of erbB1, erbB2, and erbB4 were determined for a series of alkynamide analogues of quinazoline- and pyrido[3,4-d]pyrimidine-based compounds. The compounds were prepared by coupling the appropriate 6-aminoquinazolines or 6-aminopyrido[3,4-d]pyrimidines with alkynoic acids, using EDCI·HCl in pyridine. The compounds showed pan-erbB enzyme inhibition but were on average about 10-fold more potent against erbB1 than against erbB2 and erbB4. For cellul...

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Format

Research paper

Research format

Journal article

Date created

2006

Creator

Klutchko, SR / Zhou, H / Winters, RT / Tran, TP / Bridges, AJ / Althaus, IW / Amato, DM / Elliott, WL / Ellis, PA / Meade, MA / Roberts, BJ / Fry, DW / Gonzales, AJ / Harvey, PJ / Nelson, JM / Sherwood, V / Hahn, HK / Pace, G / Smaill, Jeffrey / Denny, William / Showalter, HD

URL

http://hdl.handle.net/2292/9397

Related subjects

GROWTH-FACTOR RECEPTOR / CELL LUNG-CANCER / BINDING-SITE INHIBITORS / IN-VIVO / EGFR MUTATIONS / MURINE TUMORS / GEFITINIB / POTENT / DOMAIN / 4-(PHENYLAMINO)QUINAZOLINE

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