N-(2-chlorophenyl)-4-[[2-[4-[2-(4-ethyl-1-piperazinyl)-2-oxoethyl]anilino]-5-fluoro-4-pyrimidinyl]amino]benzamide and Lung-Neoplasms

N-(2-chlorophenyl)-4-[[2-[4-[2-(4-ethyl-1-piperazinyl)-2-oxoethyl]anilino]-5-fluoro-4-pyrimidinyl]amino]benzamide has been researched along with Lung-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for N-(2-chlorophenyl)-4-[[2-[4-[2-(4-ethyl-1-piperazinyl)-2-oxoethyl]anilino]-5-fluoro-4-pyrimidinyl]amino]benzamide and Lung-Neoplasms

Article	Year
Discovery and Synthesis of a Pyrimidine-Based Aurora Kinase Inhibitor to Reduce Levels of MYC Oncoproteins. Journal of medicinal chemistry, 2021, 06-10, Volume: 64, Issue:11 The A-type Aurora kinase is upregulated in many human cancers, and it stabilizes MYC-family oncoproteins, which have long been considered an undruggable target. Here, we describe the design and synthesis of a series of pyrimidine-based derivatives able to inhibit Aurora A kinase activity and reduce levels of cMYC and MYCN. Through structure-based drug design of a small molecule that induces the DFG-out conformation of Aurora A kinase, lead compound Topics: Animals; Aurora Kinase A; Aurora Kinase B; Binding Sites; Cell Proliferation; Down-Regulation; Drug Design; Drug Evaluation, Preclinical; Humans; Lung Neoplasms; Male; Mice; Mice, Inbred ICR; Molecular Docking Simulation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-myc; Pyrimidines; Small Cell Lung Carcinoma; Structure-Activity Relationship; Xenograft Model Antitumor Assays	2021

Article

Year

Discovery and Synthesis of a Pyrimidine-Based Aurora Kinase Inhibitor to Reduce Levels of MYC Oncoproteins.

Journal of medicinal chemistry, 2021, 06-10, Volume: 64, Issue:11

The A-type Aurora kinase is upregulated in many human cancers, and it stabilizes MYC-family oncoproteins, which have long been considered an undruggable target. Here, we describe the design and synthesis of a series of pyrimidine-based derivatives able to inhibit Aurora A kinase activity and reduce levels of cMYC and MYCN. Through structure-based drug design of a small molecule that induces the DFG-out conformation of Aurora A kinase, lead compound

Topics: Animals; Aurora Kinase A; Aurora Kinase B; Binding Sites; Cell Proliferation; Down-Regulation; Drug Design; Drug Evaluation, Preclinical; Humans; Lung Neoplasms; Male; Mice; Mice, Inbred ICR; Molecular Docking Simulation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-myc; Pyrimidines; Small Cell Lung Carcinoma; Structure-Activity Relationship; Xenograft Model Antitumor Assays

2021