Design, synthesis, and antitumor activity of erlotinib derivatives

L Mao, ZZ Wang, Q Wu, X Chen, JX Yang… - Frontiers in …, 2022 - frontiersin.org
Nineteen erlotinib derivatives bearing different 1, 2, 3-triazole moieties were designed,
synthesized, and evaluated for their potential against different cancer cell lines. The …

Synthesis of novel pyrido [2, 3-d] pyrimidine-thiazolidine-1, 2, 3-triazoles: Potent EGFR targeting anticancer agents

SR Bandi, R Kapavarapu, R Palabindela… - Journal of Molecular …, 2023 - Elsevier
In this study, we designed and synthesized a number of novel pyrido [2, 3-d] pyrimidine-
thiazolidine-1, 2, 3-triazole derivatives and investigated them in vitro for their inhibitory …

Synthesis and Structure Determination of Substituted Thiazole Derivatives as EGFR/BRAFV600E Dual Inhibitors Endowed with Antiproliferative Activity

LH Al-Wahaibi, EM El-Sheref, AA Hassan, S Bräse… - Pharmaceuticals, 2023 - mdpi.com
2, 3, 4-trisubstituted thiazoles 3a–i, having a methyl group in position four, were synthesized
by the reaction of 1, 4-disubstituted thiosemicarbazides with chloroacetone in ethyl …

Discovery of a series of 1, 2, 3-triazole-containing erlotinib derivatives with potent anti-tumor activities against non-small cell lung cancer

G Sun, L Mao, W Deng, S Xu, J Zhao, J Yang… - Frontiers in …, 2022 - frontiersin.org
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) are emerging at
the vanguard of therapy for non-small-cell lung cancer (NSCLC) patients with EGFR …

Synthesis and antitumor activity of erlotinib derivatives linked with 1, 2, 3-triazole

P Deng, G Sun, J Zhao, K Yao, M Yuan… - Frontiers in …, 2022 - frontiersin.org
Cervical cancer is one of the most important cause of cancer-related death and presents a
major public health problem in many countries. To search for more novel antitumor agents …

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 …

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 …

In vitro and in silico evaluation of anticancer activity of new indole-based 1, 3, 4-oxadiazoles as EGFR and COX-2 inhibitors

B Sever, MD Altıntop, A Özdemir, G Akalın Çiftçi… - Molecules, 2020 - mdpi.com
Epidermal growth factor receptor (EGFR) and cyclooxygenase-2 (COX-2) are crucial
targetable enzymes in cancer management. Therefore, herein, new 2-[(5-((1 H-indol-3-yl) …

Novel anticancer fused pyrazole derivatives as EGFR and VEGFR-2 dual TK inhibitors

NM Saleh, MG El-Gazzar, HM Aly, RA Othman - Frontiers in chemistry, 2020 - frontiersin.org
EGFR and VEGFR-2 represent promising targets for cancer treatment as they are very
important in tumor development as well as in angiogenesis and metastasis. In this work, 6 …

New oxadiazole and pyrazoline derivatives as anti-proliferative agents targeting EGFR-TK: design, synthesis, biological evaluation and molecular docking study

MI Serag, SS Tawfik, SMI Badr, HM Eisa - Scientific Reports, 2024 - nature.com
Two new series of oxadiazole and pyrazoline derivatives were designed and synthesized as
promising EGFR-TK inhibitors. The in vitro antiproliferative activity was studied against three …