[Synthesis of benzodihydropyran derivatives and evaluation of their preliminary biological activities on bone and vascular tissues].

AIM: 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.

CONCLUSION

Compounds b and c showed some bone and vascular protective activities which benefit postmenopausal and cardiovascular diseases.