Document Detail

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.
MedLine Citation:
PMID:  20006496     Owner:  NLM     Status:  MEDLINE    
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.
Narsimha Reddy Penthala; Thirupathi Reddy Yerramreddy; Peter A Crooks
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural     Date:  2009-11-22
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Jan 
Date Detail:
Created Date:  2010-02-03     Completed Date:  2010-04-20     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  591-3     Citation Subset:  IM    
Copyright Information:
Copyright 2009 Elsevier Ltd. All rights reserved.
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, USA.
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MeSH Terms
Antineoplastic Agents / chemical synthesis*,  chemistry,  toxicity
Cell Line, Tumor
Drug Screening Assays, Antitumor
Imidazoles / chemical synthesis*,  chemistry,  toxicity
Indoles / chemical synthesis*,  chemistry,  toxicity
Tryptophan / analogs & derivatives,  chemistry,  pharmacology
Grant Support
Reg. No./Substance:
0/Antineoplastic Agents; 0/Imidazoles; 0/Indoles; 63153-56-0/aplysinopsin; 73-22-3/Tryptophan

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