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.
Bi
Yue-Feng
YF
School of Pharmaceutical Science, Zhengzhou University, Ke Xue Da Dao 100, Zhengzhou 450001, PR China.
Xu
Hai-Wei
HW
Liu
Xiao-Qing
XQ
Zhang
Xiao-Juan
XJ
Wang
Zhen-Ji
ZJ
Liu
Hong-Min
HM
D045784:Abietanes; D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D009638:Norepinephrine / Q000378:metabolism; D010616:Phenanthrenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D027561:Salvia miltiorrhiza / Q000737:chemistry; D013329:Structure-Activity Relationship; D014665:Vasodilator Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D045784:Abietanes; D010616:Phenanthrenes; D014665:Vasodilator Agents; C021751:tanshinone; C037886:cryptotanshinone; D009638:Norepinephrine