Abstract
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 M and 72.6 M, 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.
Keywords: Antimitotic activities, Sea-urchin embryonic cells, Morita-Baylis-Hillman adducts, Cancer
Medicinal Chemistry
Title:Antimitotic Activity on Sea Urchin Embryonic Cells of Seven Antiparasitic Morita-Baylis-Hillman Adducts: A Potential New Class of Anticancer Drugs
Volume: 8 Issue: 6
Author(s): Jocelmo C. A. Leite, Claudio G. L. Junior, Fabio P. L. Silva, Suervy C.O. Sousa, Mario L. A. A. Vasconcellos and Luis F. Marques-Santos
Affiliation:
Keywords: Antimitotic activities, Sea-urchin embryonic cells, Morita-Baylis-Hillman adducts, Cancer
Abstract: 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 M and 72.6 M, 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.
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C. A. Leite Jocelmo, G. L. Junior Claudio, P. L. Silva Fabio, C.O. Sousa Suervy, L. A. A. Vasconcellos Mario and F. Marques-Santos Luis, Antimitotic Activity on Sea Urchin Embryonic Cells of Seven Antiparasitic Morita-Baylis-Hillman Adducts: A Potential New Class of Anticancer Drugs, Medicinal Chemistry 2012; 8 (6) . https://dx.doi.org/10.2174/1573406411208061003
DOI https://dx.doi.org/10.2174/1573406411208061003 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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