[HTML][HTML] 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
… of Erlotinib derivatives containing 1,2,3-triazole ring were designed and synthesized. Cell-based
assay discovered … mutation, is still most sensitive to Erlotinib. However, several of the …

Synthesis and Biological Evaluation of Novel Carbohydrate‐Derived Derivatives of Erlotinib

W Yu, L Jiang, C Shen, P Zhang - Drug Development Research, 2016 - Wiley Online Library
… In conclusion, a series of novel erlotinib derivatives bearing different sugar moieties were
synthesized and their putative antitumor activities assessed via inhibition of cancer cell …

Synthesis and evaluation of novel erlotinib–NSAID conjugates as more comprehensive anticancer agents

Y Zhang, MD Tortorella, J Liao, X Qin… - ACS Medicinal …, 2015 - ACS Publications
… Among the derivatives made, compounds 10a, 10c, and 21g showed superb potency, … In
this study we present a series of esterase hydrolyzable NSAIDs conjugated with erlotinib, which …

New series of benzothiazole and pyrimido[2,1-b]benzothiazole derivatives: synthesis, antitumor activity, EGFR tyrosine kinase inhibitory activity and molecular …

MT Gabr, NS El-Gohary, ER El-Bendary… - Medicinal Chemistry …, 2015 - Springer
… of this novel template led to the discovery of highly selective compounds that target EGFR. …
a pharmacophore for the mode of action of erlotinib, which prevents activation of EGFR kinase …

[HTML][HTML] Discovery of Potent EGFR Inhibitors With 6-Arylureido-4-anilinoquinazoline Derivatives

M Li, N Xue, X Liu, Q Wang, H Yan, Y Liu… - Frontiers in …, 2021 - frontiersin.org
… dominant structures and discovered a series of inhibitors … , we found that the BFE of erlotinib
was lower than that of … R127 (Figure 8B), but erlotinib could not interact with this region due …

Discovery of novel 4-anilinoquinazoline derivatives as potent inhibitors of epidermal growth factor receptor with antitumor activity

YY Xu, SN Li, GJ Yu, QH Hu, HQ Li - Bioorganic & medicinal chemistry, 2013 - Elsevier
… -substituted-4-anilinoquinazolines and Erlotinib was performed in EGFR-dependent A549
… We report here two new series of EGFR inhibitors containing a 6-amino-substituted group or …

[HTML][HTML] Discovery of a series of novel phenylpiperazine derivatives as EGFR TK inhibitors

J Sun, XY Wang, PC Lv, HL Zhu - Scientific Reports, 2015 - nature.com
… first discovered that the 4-anilinoquinazoline derivative PD153035 possesses specific …
quinazoline derivatives have been synthesized, including reversible inhibitors, such as erlotinib, …

[HTML][HTML] 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
… In summary, a series of erlotinib derivatives containing 1,2,3-triazole rings were prepared …
Some of the compounds exhibited better antiproliferation activities than the parent erlotinib. …

[HTML][HTML] Novel 1, 2, 3-triazole erlotinib derivatives as potent IDO1 inhibitors: Design, drug-target interactions prediction, synthesis, biological evaluation, molecular …

GQ Xu, XQ Gong, YY Zhu, XJ Yao, LZ Peng… - Frontiers in …, 2022 - frontiersin.org
… the early stage of drug discovery can reduce the possibility of … triazole compounds based on
the erlotinib core structure in a … In this study, a series of erlotinib derivatives containing 1,2,3-…

Design, synthesis and biological evaluation of new series of hexahydroquinoline and fused quinoline derivatives as potent inhibitors of wild-type EGFR and mutant …

MA Shaheen, AA El-Emam, NS El-Gohary - Bioorganic Chemistry, 2020 - Elsevier
… followed to prepare new series of fused quinoline derivatives. Molecular hybridization involves
… to that of erlotinib over EGFR L858R and 17 times higher than that of erlotinib over EGFR …