The practical synthesis of a novel and highly potent analogue of bryostatin

Authors :: Wender, Paul A.; Clarke, Michael O.; Nell, Peter G.
Baryza, Jeremy L.; Horan, Joshua C.; Turner, Tim M.
Bennett, Chad E.; Kan, Cindy
Bi, F Christopher; Lacote, Emmanuel
Brenner, Stacey E.; Lippa, Blaise
Source :: Journal of the American Chemical Society. Nov 20, 2002, Vol. 124 Issue 46, p13648, 2 p.
Publication Year :: 2002
Abstract: The practical synthesis and bioassay of a new and superior analogue, PKC isozymes designed on the basis of pharmacophoric model that is over 100-fold more potent than bryostatin at inhibiting the growth of numerous human cancer cell lines is reported. In agreement with pharmacophoric model, bryostatin 1 displays picmolar affinity for PKC. When tested in vitro against various human cancer cell lines, it displayed greater potency than bryostatin 1.