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

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.

Cite this article as:

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