Synthesis and vasodilative activity of tanshinone IIA derivatives

A series of 2,2'-(substituted methylene)bis-(1,6,6-trimethyl-6,7,8,9-tetrahydrophenanthro[1,2-b]furan-10,11-dione) derivatives were synthesized by the reaction of tanshinone IIA (D(1)) and aromatic aldehyde in the presence of p-TsOH. Bromination derivative of D(1) and hydrolysis product of cryptotanshinone (D(2)) were also prepared in this work. Vasodilation activity in vitro of them was valuated on the contractile response of vascular thoracic aorta smooth muscle from Wistar rats for the first time. Most of them exhibited a concentration-dependent inhibition on the contractile response of norepinephrine. (c) 2010 Elsevier Ltd. All rights reserved.