Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4

Autor:	Christopher J. Jelinek, George R. Pettit, Justin K. Tidmore, Tracy E. Strecker, Madhavi Sriram, G.D. Kishore Kumar, Mallinath B. Hadimani, Mary Lynn Trawick, John J. Hall, David J. Chaplin, Kevin G. Pinney
Rok vydání:	2008
Předmět:	Hydrocarbons Fluorinated Stereochemistry Clinical Biochemistry Pharmaceutical Science Ether Biochemistry Chemical synthesis Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Tubulin Bibenzyls Stilbenes Drug Discovery Combinatorial Chemistry Techniques Humans Cytotoxicity Molecular Biology chemistry.chemical_classification Combretastatin A-4 Combretastatin Molecular Structure Chemistry Organic Chemistry Aromatic amine Stereoisomerism Antineoplastic Agents Phytogenic Tubulin Modulators In vitro Drug Design Molecular Medicine Drug Screening Assays Antitumor Lead compound
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:5146-5149
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2008.07.070
Popis:	A new trifluorinated amino-combretastatin analogue, ( Z) -2-(4′-methoxy-3′-aminophenyl)-1-(3,4,5-trifluorophenyl)ethene, prepared by chemical synthesis, was found to be a potent inhibitor of tubulin assembly (IC 50 = 2.9 μM), and cytotoxic against selected human cancer cell lines. This new lead compound is among the most active from a group of related structural modifications.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5888082483e93431c2388d1229fecf9 https://doi.org/10.1016/j.bmcl.2008.07.070 Zobrazit plný text záznamu Full Text from ScienceDirect