Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1.
Anticancer
Antitumor
Dual inhibitor
EGFR
HER2
Irreversible
Quinazoline
Tyrosine kinase
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
15 02 2019
15 02 2019
Historique:
received:
09
10
2018
revised:
17
12
2018
accepted:
24
12
2018
pubmed:
3
1
2019
medline:
7
3
2020
entrez:
3
1
2019
Statut:
ppublish
Résumé
Overexpression of EGFR and HER2 are observed in many breast, ovarian, colon and prostate cancers. The second and third generation irreversible EGFR/HER2 dual kinase inhibitors became popular after the approval of Afatinib by FDA to overcome the mutation related problem. To find efficacious drug candidates, a series of novel quinazoline derivatives were designed, synthesized and evaluated as dual EGFR/HER2 tyrosine kinase (TK) inhibitors. Selected twenty four compounds were reported here with significant inhibitory activities against EGFR/HER2 tyrosine kinases. Several compounds showed nanomolar IC
Identifiants
pubmed: 30600209
pii: S0960-894X(18)31002-3
doi: 10.1016/j.bmcl.2018.12.056
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Quinazolines
0
ERBB2 protein, human
EC 2.7.10.1
ErbB Receptors
EC 2.7.10.1
Receptor, ErbB-2
EC 2.7.10.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
591-596Informations de copyright
Copyright © 2018 Elsevier Ltd. All rights reserved.