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^-7mol·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 osteoporosis and cardiovascular diseases.