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Text
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URL Address
<a href="http://doi.org/10.1016/j.bmcl.2014.07.072" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2014.07.072</a>
Pages
4553–4556
Issue
18
Volume
24
Dublin Core
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Title
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Screening and identification of novel compounds with potential anti-proliferative effects on gallium-resistant lung cancer through an AXL kinase pathway.
Publisher
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Bioorganic & medicinal chemistry letters
Date
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2014
2014-09
Subject
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Antineoplastic Agents/chemical synthesis/chemistry/*pharmacology; Antitumor; AXL; Cell Line; Cell Proliferation/drug effects; Cell Survival/drug effects; Dose-Response Relationship; Drug; Drug Resistance; Drug Screening Assays; Gallium; Gallium-resistance; Gallium/pharmacology; Humans; Lung cancer; Lung Neoplasms/drug therapy/*enzymology/*pathology; Molecular Structure; Naphthalenes/chemistry/*pharmacology; Neoplasm/drug effects; Proto-Oncogene Proteins/*antagonists & inhibitors/metabolism; Pyrazoles/chemistry/*pharmacology; Quinolines/chemistry/*pharmacology; Receptor Protein-Tyrosine Kinases/*antagonists & inhibitors/metabolism; Structure-Activity Relationship; Tetrazoles/chemistry/*pharmacology; Tumor; Virtual screening
Creator
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Oyewumi Moses O; Alazizi Adnan; Liva Sophia; Lin Li; Geldenhuys Werner J
Description
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The clinical application of gallium compounds as anticancer agents is hampered by development of resistance. As a potential strategy to overcome the limitation, eight series of compounds were identified through virtual screening of AXL kinase homology model. Anti-proliferative studies were carried using gallium-sensitive (S) and gallium-resistant (R) human lung adenocarcinoma (A549) cells. Compounds 5476423 and 7919469 were identified as leads. The IC50 values from treating
Identifier
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<a href="http://doi.org/10.1016/j.bmcl.2014.07.072" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2014.07.072</a>
Rights
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Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
2014
Alazizi Adnan
Antineoplastic Agents/chemical synthesis/chemistry/*pharmacology
Antitumor
AXL
Bioorganic & medicinal chemistry letters
Cell Line
Cell Proliferation/drug effects
Cell Survival/drug effects
Department of Pharmaceutical Sciences
Dose-Response Relationship
Drug
Drug Resistance
Drug Screening Assays
Gallium
Gallium-resistance
Gallium/pharmacology
Geldenhuys Werner J
Humans
Lin Li
Liva Sophia
Lung cancer
Lung Neoplasms/drug therapy/*enzymology/*pathology
Molecular Structure
Naphthalenes/chemistry/*pharmacology
NEOMED College of Pharmacy
Neoplasm/drug effects
Oyewumi Moses O
Proto-Oncogene Proteins/*antagonists & inhibitors/metabolism
Pyrazoles/chemistry/*pharmacology
Quinolines/chemistry/*pharmacology
Receptor Protein-Tyrosine Kinases/*antagonists & inhibitors/metabolism
Structure-Activity Relationship
Tetrazoles/chemistry/*pharmacology
Tumor
Virtual screening