Generic placeholder image

Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Antimitotic Activity on Sea Urchin Embryonic Cells of Seven Antiparasitic Morita-Baylis-Hillman Adducts: A Potential New Class of Anticancer Drugs

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

Volume 8, Issue 6, 2012

Page: [1003 - 1011] Pages: 9

DOI: 10.2174/1573406411208061003

Price: $65

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

Next »

Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy