Design and Synthesis of some new 2, 4, 6-trisubstituted quinazoline EGFR inhibitors as targeted anticancer agents

HA Allam, EE Aly, AK Farouk, AM El Kerdawy… - Bioorganic …, 2020 - Elsevier
The present study describes the synthesis of 6-bromo-2-(pyridin-3-yl)-4-substituted
quinazolines starting from 4-chloro derivative VI via the reaction with either phenolic …

Design and synthesis of 4, 6-substituted-(diaphenylamino) quinazolines as potent EGFR inhibitors with antitumor activity

HQ Li, DD Li, X Lu, YY Xu, HL Zhu - Bioorganic & medicinal chemistry, 2012 - Elsevier
A type of novel 4, 6-substituted-(diaphenylamino) quinazolines, which designed based on
the 4-(phenylamino) quinazoline moiety, have been discovered as potential EGFR …

6, 7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells

Y Zhang, L Chen, H Xu, X Li, L Zhao, W Wang… - European Journal of …, 2018 - Elsevier
Abstract A series of novel 6, 7-dimorpholinoalkoxy quinazoline derivatives was designed,
synthesized and evaluated as potent EGFR inhibitors. Most of synthesized derivatives …

Novel quinoline-3-carboxamides (Part 2): Design, optimization and synthesis of quinoline based scaffold as EGFR inhibitors with potent anticancer activity

RM Aly, RAT Serya, AM El-Motwally, A Esmat… - Bioorganic …, 2017 - Elsevier
EGFR has a key role in cell growth. Its mutation and overexpression share in epithelial
malignancies and tumor growth. Quinazoline and quinoline derivatives are common …

Novel Pyrazoloquinolin-2-ones: Design, synthesis, docking studies, and biological evaluation as antiproliferative EGFR-TK inhibitors

MAI Elbastawesy, AA Aly, M Ramadan… - Bioorganic …, 2019 - Elsevier
Two new series of diethyl 2-[2-(substituted-2-oxo-1, 2-dihydroquinolin-4-yl) hydrazono]-
succinates 6a-g and 1-(2-oxo-1, 2-dihydroquinolin-4-yl)-1H-pyrazoles 7a-f have been …

[PDF][PDF] Design, synthesis, anticancer activity and docking studies of novel quinazoline-based thiazole derivatives as EGFR kinase inhibitors

MS Raghu, HA Swarup, T Shamala, BS Prathibha… - Heliyon, 2023 - cell.com
The in vitro anticancer efficacy of a new series of quinazoline-based thiazole derivatives was
explored. Three cancer cell lines, MCF-7, HepG2, and A548, as well as the normal Vero cell …

Synthesis and in vitro anticancer evaluation of some fused indazoles, quinazolines and quinolines as potential EGFR inhibitors

EA Abdelsalam, WA Zaghary, KM Amin… - Bioorganic …, 2019 - Elsevier
Abstract derivatives of benzo [g] indazole 5a, b, benzo [h] quinazoline 7, 12a-c, 13a-c and
15a-c and benzo [h] quinoline 17a-c and 19a-c were synthesized from 6-methoxy-3, 4 …

Development of a series of novel 4-anlinoquinazoline derivatives possessing quinazoline skeleton: Design, synthesis, EGFR kinase inhibitory efficacy, and evaluation …

J Chang, H Ren, M Zhao, Y Chong, W Zhao… - European Journal of …, 2017 - Elsevier
anilinoquinazoline-based derivatives represent an attractive scaffold for small molecular
EGFR-TKIs in the field of medicinal chemistry. A series of novel heterocyclic substituted …

Design and synthesis of novel quinazolinone-based derivatives as EGFR inhibitors with antitumor activity

A Sonousi, RA Hassan, EO Osman… - Journal of Enzyme …, 2022 - Taylor & Francis
Abstract Nineteen new quinazolin-4 (3 H)-one derivatives 3a–g and 6a–l were designed
and synthesised to inhibit EGFR. The antiproliferative activity of the synthesised compounds …

Novel 4-(2-arylidenehydrazineyl) thienopyrimidine derivatives as anticancer EGFR inhibitors: Design, synthesis, biological evaluation, kinome selectivity and in silico …

HA Elsebaie, EA El-Bastawissy, KM Elberembally… - Bioorganic …, 2023 - Elsevier
The current study discovered fifteen new thieno [2, 3-d] pyrimidine derivatives with potential
anticancer action, including 5a-l, 6, and 7a-b. Results from the NCI screening revealed that …