Synthesis and preliminary structure-activity relationship study of 3-methylquinazolinone derivatives as EGFR inhibitors with enhanced antiproliferative activities against tumour cells

Synthesis and preliminary structure-activity relationship study of 3-methylquinazolinone derivatives as EGFR inhibitors with enhanced antiproliferative activities against tumour cells

In this paper, a set of 3-methylquniazolinone derivatives were designed, synthesised, and studied the preliminary structure-activity relationship for antiproliferative activities. All target compounds performed significantly inhibitory effects against wild type epidermal growth factor receptor tyros...

Full description

Bibliographic Details
Main Authors:	Yan Zhang, Qin Wang, Luolan Li, Yi Le, Li Liu, Jing Yang, Yongliang Li, Guochen Bao, Longjia Yan
Format:	Article
Language:	English
Published:	Taylor & Francis Group 2021-01-01
Series:	Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:	quinazolinone egfr kinase inhibitor structure-activity relationship antiproliferative
Online Access:	http://dx.doi.org/10.1080/14756366.2021.1933466

Similar Items

New Multi-Targeted Antiproliferative Agents: Design and Synthesis of IC261-Based Oxindoles as Potential Tubulin, CK1 and EGFR Inhibitors
by: Momen R. Fareed, et al.
Published: (2021-10-01)

Synthesis of some quinazolinones inspired from the natural alkaloid L-norephedrine as EGFR inhibitors and radiosensitizers
by: Mostafa M. Ghorab, et al.
Published: (2021-01-01)

Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors
by: Yaqing Zuo, et al.
Published: (2022-12-01)

A Review on Fused Pyrimidine Systems as EGFR Inhibitors and Their Structure–Activity Relationship
by: Tanuja T. Yadav, et al.
Published: (2022-06-01)

Design, synthesis, and apoptotic antiproliferative action of new 1,2,3-triazole/1,2,4-oxadiazole hybrids as dual EGFR/VEGFR-2 inhibitors
by: Mohamed A. Mahmoud, et al.
Published: (2024-12-01)

Synthesis, DFT Analyses, Antiproliferative Activity, and Molecular Docking Studies of Curcumin Analogues
by: Mohamed Jawed Ahsan, et al.
Published: (2022-10-01)

Design, synthesis, and analysis of antiproliferative and apoptosis-inducing activities of nitrile derivatives containing a benzofuran scaffold: EGFR inhibition assay and molecular modelling study
by: Salma Fares, et al.
Published: (2021-01-01)

Novel piperine-carboximidamide hybrids: design, synthesis, and antiproliferative activity via a multi-targeted inhibitory pathway
by: Lamya H. Al-Wahaibi, et al.
Published: (2023-12-01)

Phenylpyrazalopyrimidines as Tyrosine Kinase Inhibitors: Synthesis, Antiproliferative Activity, and Molecular Simulations
by: Bhupender S. Chhikara, et al.
Published: (2020-05-01)

Design, Synthesis and Biological Evaluation of Benzohydrazide Derivatives Containing Dihydropyrazoles as Potential EGFR Kinase Inhibitors
by: Hai-Chao Wang, et al.
Published: (2016-08-01)

Semi-Synthesis of Harringtonolide Derivatives and Their Antiproliferative Activity
by: Xiutao Wu, et al.
Published: (2021-03-01)

Synthesis, anticancer and apoptosis-inducing activities of quinazoline–isatin conjugates: epidermal growth factor receptor-tyrosine kinase assay and molecular docking studies
by: Adel S. El-Azab, et al.
Published: (2017-01-01)

Design, synthesis, apoptotic, and antiproliferative effects of 5-chloro-3- (2-methoxyvinyl)-indole-2-carboxamides and pyrido[3,4-b]indol-1-ones as potent EGFRWT/EGFRT790M inhibitors
by: Lamya H. Al-Wahaibi, et al.
Published: (2023-12-01)

Structural Modifications of Nature-Inspired Indoloquinolines: A Mini Review of Their Potential Antiproliferative Activity
by: Ning Wang, et al.
Published: (2019-06-01)

Design, Synthesis, and Biological Evaluation of Indole-2-carboxamides as Potential Multi-Target Antiproliferative Agents
by: Lamya H. Al-Wahaibi, et al.
Published: (2023-07-01)

Synthesis and Biological Evaluation of Indole-2-Carboxamides with Potent Apoptotic Antiproliferative Activity as EGFR/CDK2 Dual Inhibitors
by: Lamya H. Al-Wahaibi, et al.
Published: (2022-08-01)

Synthesis and Antiproliferative Activities of 5-Azacytidine Analogues in Human Leukemia Cells
by: Lin-Xiang Zhao, et al.
Published: (2008-07-01)

Molecular Engineering of Curcumin, an Active Constituent of <i>Curcuma longa</i> L. (Turmeric) of the Family <i>Zingiberaceae</i> with Improved Antiproliferative Activity
by: Amena Ali, et al.
Published: (2021-07-01)

Design, synthesis, docking and mechanistic studies of new thiazolyl/thiazolidinylpyrimidine-2,4-dione antiproliferative agents
by: Ashraf A. Aly, et al.
Published: (2023-04-01)

Design and synthesis of novel quinazolinone-based derivatives as EGFR inhibitors with antitumor activity
by: Amr Sonousi, et al.
Published: (2022-12-01)

Combining genomic analyses with tumour-derived slice cultures for the characterization of an EGFR-activating kinase mutation in a case of glioblastoma
by: Lea Loriguet, et al.
Published: (2018-10-01)

Discovery of dual tubulin-NEDDylation inhibitors with antiproliferative activity
by: Dong-Jun Fu, et al.
Published: (2023-12-01)

A preliminary results of integrated chemotherapy with EGFR receptor tyrosine kinase inhibitors in patients with non-small-cell-lung cancer harboring EGFR mutation
by: K. K. Laktionov, et al.
Published: (2019-06-01)

Globally Approved EGFR Inhibitors: Insights into Their Syntheses, Target Kinases, Biological Activities, Receptor Interactions, and Metabolism
by: Mohammed A. S. Abourehab, et al.
Published: (2021-11-01)

Evaluation of antiproliferative activity of pyrazolothiazolopyrimidine derivatives
by: N. S. Finiuk, et al.
Published: (2018-04-01)

Antiproliferative and Antimicrobial Activities of Selected Bryophytes
by: Martin Vollár, et al.
Published: (2018-06-01)

Structural Insight and Development of EGFR Tyrosine Kinase Inhibitors
by: Tasia Amelia, et al.
Published: (2022-01-01)

Structural insights into conformational stability and binding of thiazolo-[2,3-b] quinazolinone derivatives with EGFR-TKD and in-vitro study
by: Showkat Ahmad Mir, et al.
Published: (2022-12-01)

Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones
by: Valentina Onnis, et al.
Published: (2016-04-01)

Antioxidant, Cytotoxic, Genotoxic, and DNA-Protective Potential of 2,3-Substituted Quinazolinones: Structure—Activity Relationship Study
by: Jana Hricovíniová, et al.
Published: (2021-01-01)

Antitumor activity of aumolertinib, a third-generation EGFR tyrosine kinase inhibitor, in non-small-cell lung cancer harboring uncommon EGFR mutations
by: Chen Shi, et al.
Published: (2023-06-01)

Mechanochemical synthesis of indolyl chalcones with antiproliferative activity
by: Zuzana Kudličková, et al.
Published: (2022-04-01)

Discovery of YS-363 as a highly potent, selective, and orally eﬃcacious EGFR inhibitor
by: Pengxing He, et al.
Published: (2023-11-01)

1,3,4-Thiadiazoline−coumarin hybrid compounds containing D-glucose/D-galactose moieties: Synthesis and evaluation of their antiproliferative activity
by: Vu Ngoc Toan, et al.
Published: (2021-04-01)

Antiproliferative activity of peels, pulps and seeds of 61 fruits
by: Fang Li, et al.
Published: (2013-07-01)

Emerging strategies to overcome resistance to third-generation EGFR inhibitors
by: Kunyu Shi, et al.
Published: (2022-07-01)

Stability and Antiproliferative Activity of Malvidin-Based Non-Oxonium Derivative (Oxovitisin A) Compared with Precursor Anthocyanins and Pyranoanthocyanins
by: Muci Wu, et al.
Published: (2022-08-01)

Resistance of Lung Cancer to EGFR-Specific Kinase Inhibitors: Activation of Bypass Pathways and Endogenous Mutators
by: Ilaria Marrocco, et al.
Published: (2023-10-01)

Chemical Constituents With Antiproliferative Activity From Pogostemon cablin (Blanco) Benth.
by: Xingjia Peng, et al.
Published: (2022-07-01)

Synthesis and Structure Determination of Substituted Thiazole Derivatives as EGFR/BRAF<sup>V600E</sup> Dual Inhibitors Endowed with Antiproliferative Activity
by: Lamya H. Al-Wahaibi, et al.
Published: (2023-07-01)