Synthesis and antitumour activity of 4-aminoquinazoline derivatives / Lipunova Galina N.,Nosova Emiliya V.,Charushin Valery N.,Chupakhin Oleg N. // RUSSIAN CHEMICAL REVIEWS. - 2016. - V. 85, l. 7. - P. 759-793.

ISSN/EISSN:

0036-021X / 1468-4837

Type:

Review

Abstract:

Pieces of data on the synthesis and antitumour activity of 4-aminoquinazolines are summarized and analyzed. Key methods for the synthesis of these compounds are considered, primarily cyclocondensation of carboxylic acid derivatives, as well as the oxidation of quinazolines and the cyclization of disubstituted thioureas. Improvements of synthetic schemes for erlotinib, gefitinib and lapatinib, which are the best-known pharmaceuticals based on compounds of the title class, are also considered. Synthetic strategies and biological activities for new 4-aminoquinazoline derivatives that are EGFR-tyrosine kinase inhibitors, multiactive compounds, and labelled compounds for use as positron emission tomography (PET) imaging agents are discussed. The bibliography includes 263 references.

Author keywords:

GROWTH-FACTOR RECEPTOR; TYROSINE KINASE INHIBITORS; POTENT EGFR INHIBITORS; COMBI-TARGETING CONCEPT; TUMOR-CELL LINES; PHASE-II TRIAL; IRREVERSIBLE INHIBITORS; BIOLOGICAL EVALUATION; 4-ANILINOQUINAZOLINE DERIVATIVES; IN-VITRO

DOI:

10.1070/RCR4591

Web of Science ID:

ISI:000380955100005

Соавторы в МНС:

Другие поля

Поле	Значение
Publisher	TURPION LTD
Address	C/O TURPION LTD, IOP PUBLISHING, TEMPLE CIRCUS, TEMPLE WAY, BRISTOL BS1 6HG, ENGLAND
Language	English
EISSN	1468-4837
Keywords-Plus	GROWTH-FACTOR RECEPTOR; TYROSINE KINASE INHIBITORS; POTENT EGFR INHIBITORS; COMBI-TARGETING CONCEPT; TUMOR-CELL LINES; PHASE-II TRIAL; IRREVERSIBLE INHIBITORS; BIOLOGICAL EVALUATION; 4-ANILINOQUINAZOLINE DERIVATIVES; IN-VITRO
Research-Areas	Chemistry
Web-of-Science-Categories	Chemistry, Multidisciplinary
Author-Email	ipunova@ios.uran.ru emily74@rambler.ru charushin@ios.uran.ru chupakhin@ios.uran.ru
Funding-Acknowledgement	Russian Science Foundation {[}15-13-00077]; Government Assignment of the Ministry for Education and Science of the Russian Federation {[}2458]
Funding-Text	This survey was prepared with financial support from the Russian Science Foundation (Project No. 15-13-00077, Sections I-III) and the Government Assignment of the Ministry for Education and Science of the Russian Federation (Project No. 2458, Sections IV - VI).
Number-of-Cited-References	263
Usage-Count-Since-2013	6
Journal-ISO	Russ. Chem. Rev.
Doc-Delivery-Number	DS7HX