| Microwave assisted synthesis and in vitro cytotoxicities of substituted (Z)-2-amino-5-(1-benzyl-1H-indol-3-yl)methylene-1-methyl-1H-imidazol-4(5H)-ones against human tumor cell lines. | |
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MedLine Citation:
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PMID: 20006496 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The synthesis of several novel substituted (Z)-2-amino-5-(1-benzyl-1H-indol-3-yl)methylene-1-methyl-1H-imidazol-4(5H)-ones structurally related to aplysinopsin have been carried out under microwave irradiation and conventional heating methods. The analogs 3a, 3b, 3d-3g,3k and 3l were evaluated for their in vitro cytotoxic activity against an NCI 60 human tumor cell line panel. Compound 3f exhibited good growth inhibitory properties against all but four of the human cancer cell lines examined, and afforded LC(50) values <10microM for 30% of the cell lines in the panel. Compound 3e was an effective inhibitor of leukemia, CNS, melanoma, and breast cancer cell growth, but generally less effective as a cytotoxic agent. Thus, the aplysinopsin analog 3f was regarded as a useful lead compound for further structural optimization. |
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Authors:
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Narsimha Reddy Penthala; Thirupathi Reddy Yerramreddy; Peter A Crooks |
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Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural Date: 2009-11-22 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 20 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2010 Jan |
Date Detail:
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Created Date: 2010-02-03 Completed Date: 2010-04-20 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 591-3 Citation Subset: IM |
Copyright Information:
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Copyright 2009 Elsevier Ltd. All rights reserved. |
Affiliation:
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Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Antineoplastic Agents
/
chemical synthesis*,
chemistry,
toxicity Cell Line, Tumor Drug Screening Assays, Antitumor Humans Imidazoles / chemical synthesis*, chemistry, toxicity Indoles / chemical synthesis*, chemistry, toxicity Microwaves Tryptophan / analogs & derivatives, chemistry, pharmacology |
| Grant Support | |
ID/Acronym/Agency:
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P01 CA104457/CA/NCI NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents; 0/Imidazoles; 0/Indoles; 63153-56-0/aplysinopsin; 73-22-3/Tryptophan |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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