| Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors. | |
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MedLine Citation:
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PMID: 17034150 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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2-(3',4',5'-Trimethoxybenzoyl)-3-amino-5-aryl/heteroaryl thiophene derivatives were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. SARs were elucidated with various substitutions on the aryl moiety 5-position of the thienyl ring. Substituents at the para-position of the 5-phenyl group showed antiproliferative activity in the order of F=CH(3) > OCH(3)=Br=NO(2) > CF(3)=I > OEt. Several of these compounds led to arrest of HL-60 cells in the G2/M phase of the cell cycle and induction of apoptosis. |
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Authors:
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Romeo Romagnoli; Pier Giovanni Baraldi; Vincent Remusat; Maria Dora Carrion; Carlota Lopez Cara; Delia Preti; Francesca Fruttarolo; Maria Giovanna Pavani; Mojgan Aghazadeh Tabrizi; Manlio Tolomeo; Stefania Grimaudo; Jan Balzarini; Mary Ann Jordan; Ernest Hamel |
Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 49 ISSN: 0022-2623 ISO Abbreviation: J. Med. Chem. Publication Date: 2006 Oct |
Date Detail:
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Created Date: 2006-10-12 Completed Date: 2006-12-04 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: United States |
Other Details:
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Languages: eng Pagination: 6425-8 Citation Subset: IM |
Affiliation:
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Dipartimento di Scienze Farmaceutiche, Università di Ferrara, 44100 Ferrara, Italy. rmr@unife.it |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Apoptosis Cell Cycle / drug effects Cell Line, Tumor Drug Screening Assays, Antitumor Humans Mice Structure-Activity Relationship Thiophenes / chemical synthesis*, chemistry, pharmacology Tubulin Modulators / chemical synthesis*, chemistry, pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Thiophenes; 0/Tubulin Modulators |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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