Design and synthesis of novel pinacolylboronate containing combretastatin 'antimitotic agent' analogues.
We developed a procedure to synthesize pinacolyl boronate containing stilbene derivatives and used this procedure to synthesize boron-containing combretastatin analogues. The key step involves the Wittig reaction of the ylide 4-(4,4,5,5-tetramethyl-1,3,2-dioxaboratophenyl)-methyl triphenylphosphonium bromide 11 with 3,4,5-trimethoxy benzaldehyde in the presence of (t)BuONa in DMF, providing 88% yield. We are now in a position to evaluate the biological activity of these derivatives as modulators of TGF-beta signaling pathways.
Das
Bhaskar C
BC
Department of Nuclear Medicine, Albert Einstein College of Medicine, Bronx, NY 10461, USA.
Mahalingam
Sakkarapalayam M
SM
Evans
Todd
T