[Synthesis of benzodihydropyran derivatives and evaluation of their preliminary biological activities on bone and vascular tissues].
OBJECTIVE
To screen optimal drugs against postmenopausal osteoporosis with cardiovascular protective activities.


METHODS
A series of benzodihydropyran derivatives were designed and synthesized in view of comprehensive observations of raloxifene and ipriflavone. The antiosteoporosis activities of compounds a-e (10(-7) mol.L-1) on the proliferation of human osteoblast cell HOS TE85 were studied. The cardiovascular protective activities were evaluated by observing their effects on proliferation of human vascular endothelium cell ECV-304 and their protective effects on ECV-304 damaged by H2O2.


RESULTS
Their structures were determined by spectrums. Compounds a, b and c (10(-7) mol.L-1) were shown to significantly help proliferation of HOS TE85. In addition, b, d and e (10(-8) mol.L-1) helped proliferation of ECV-304 significantly. Compounds b and c (10(-6) mol.L-1) showed strong protective activity on ECV-304 damaged by H2O2. Compounds b and c shifted the KCl dose-response curves to the right and decreased the maximal response.


CONCLUSIONS
Compounds b and c showed some bone and vascular protective activities which benefit postmenopausal and cardiovascular diseases.
Xiong
X Y
XY
Pharmacology Department, Fourth Military Medical University, Xi'an 710032, China. xiongxiaoyun71@hotmail.com
Zou
Y
Y
Chen
Y Q
YQ
Gan
H Q
HQ
Mei
Q B
QB
Zhao
D H
DH
D000818:Animals; D001011:Aorta / Q000187:drug effects; D001578:Benzopyrans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects*; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D010006:Osteoblasts / Q000166:cytology / Q000187:drug effects*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014470:Umbilical Cord / Q000166:cytology
D001578:Benzopyrans