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Antimitotic Activity on Sea Urchin Embryonic Cells of Seven Antiparasitic Morita-Baylis-Hillman Adducts: A Potential New Class Of Anticancer Drugs.
MedLine Citation:
PMID:  22830498     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
In the present work we described improvements in the 1-7 antiparasitic Morita-Baylis-Hillman Adducts synthesis and their antimitotic activity on sea urchin embryonic cells. The 2-[Hydroxy(2-nitrophenyl)methyl]acrylonitrile (1) and 2-[Hydroxy(4-bromophenyl) methyl]acrylonitrile (4) were the most effective compounds to block the progression to embryonic morula stage (EC50 = 75.8 μM and 72.6μM, respectively). Compounds 1 and 4 were also effective in blocking the first cell division but to a lesser extent. The 2-[Hydroxy(pyridin-4-yl)methyl]acrylonitrile (7) exhibited a strong inhibition of cell divisions and progression to the first cleavage and morula stage. Fluorescent dye extrusion assay suggests that these adducts are not ABC protein substrates, which confers an additional interest in these new class of potential anticancer drugs.
Authors:
Jocelmo C A Leite; Claudio G L Junior; Fábio P L Silva; Suervy C O Sousa; Mário L A A Vasconcellos; Luis F Marques-Santos
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-7-25
Journal Detail:
Title:  Medicinal chemistry (Shariqah (United Arab Emirates))     Volume:  -     ISSN:  1875-6638     ISO Abbreviation:  -     Publication Date:  2012 Jul 
Date Detail:
Created Date:  2012-7-26     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101240303     Medline TA:  Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
Laboratório de Síntese Orgânica Medicinal da Paraíba (LASOM-PB)-Departamento de Química, Universidade Federal da Paraíba, Campus I, João Pessoa, PB, Brazil; mlaav@quimica.ufpb.br; marques@ dbm.ufpb.br.
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