Structure-activity relationships of new A,D-ring modified steroids as aromatase inhibitors: design, synthesis, and biological activity evaluation.

@article{Cepa2005StructureactivityRO,
  title={Structure-activity relationships of new A,D-ring modified steroids as aromatase inhibitors: design, synthesis, and biological activity evaluation.},
  author={Margarida Cepa and Elisi{\'a}rio J Tavares da Silva and Georgina Correia-da-Silva and Fernanda M F Roleira and Nat{\'e}rcia Teixeira},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 20},
  pages={
          6379-85
        }
}
Inhibition of aromatase is an efficient approach for the prevention and treatment of breast cancer. New A,D-ring modified steroid analogues of formestane and testolactone were designed and synthesized and their biochemical activity was investigated in vitro in an attempt to find new aromatase inhibitors and to gain insight into their structure-activity relationships (SAR). All compounds tested were less active than formestane. However, the 3-deoxy steroidal olefin 3a and its epoxide derivative… Expand
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