Abstract
Substituted 3-phenyl,7-methoxy-benzopyran derivatives and vitamin D3 (cholecalciferol, 1) were evaluated for their estrogen agonistic and antagonistic activities in immature female Sprague–Dawley rat model. The benzopyran derivatives 17 and 18, which were made as hybrids of estrogen and vitamin D3 (pseudo vitamin D3 analogs), showed significant estrogen agonistic activity (up to 48%) and weak estrogen antagonistic activity (up to 6%) at 10 mg/kg, whereas vitamin D3 showed significant estrogen agonistic (82%) and antagonistic activities (39%) at 10 mg/kg.
Graphical abstract
Substituted 3-phenyl, 7-methoxy-benzopyran derivavtives and vitamin-D3 (Cholecalciferol, 1) were evaluated for their estrogen agonistic and antagonistic activities in mature female Sprague–Dawley rat model. The benzopyran derivatives, which were made as hybrids of estrogen and vitamin-D3 (pseudo vitamin-D3 analogs), showed significant estrogen agonistic activity (upto 48%) and weak estrogen antagonistic activity (upto 6%) at 10 mg kg-1. Whereas, vitamin-D3 showed significant estrogen agonistic (82%) and antagonistic activities (39%) at 10 mg kg-1.
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Acknowledgements
Atul Gupta thanks CSIR (INDIA) for Senior Research Fellowship. The authors thank Ms. Mohini Chhabra for efficient technical assistance and the Ministry of Health and Family Welfare, Government of India for financial support.
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Gupta, A., Keshri, G., Singh, M.M. et al. In vivo evaluation of substituted 3-phenyl,7-methoxy-benzopyrans as modified estrogens. Med Chem Res 19, 25–32 (2010). https://doi.org/10.1007/s00044-009-9169-9
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DOI: https://doi.org/10.1007/s00044-009-9169-9