Newly discovered orally active pure antiestrogens

Yoshitake Kanbe, Myung Hwa Kim, Masahiro Nishimoto, Yoshihito Ohtake, Takaaki Yoneya, Iwao Ohizumi, Toshiaki Tsunenari, Kenji Taniguchi, Shin ichi Kaiho, Yoshiaki Nabuchi, Hiroshi Araya, Setsu Kawata, Kazumi Morikawa, Jae Chon Jo, Hee An Kwon, Hyun Suk Lim, Hak Yeop Kim

Research output: Contribution to journalArticle

12 Scopus citations

Abstract

In order to develop orally active pure antiestrogens, we incorporated the carboxy-containing side chains into the 7α-position of the steroid scaffold and found that 17-keto derivative CH4893237 (12b) functioned as a pure antiestrogen with its oral activity much superior to clinically used pure antiestrogen, ICI182,780. Results from the pharmacokinetic evaluation indicated that the potent antiestrogen activity at oral dosing in mice attributed to both improved absorption from the intestinal wall and metabolic stability in liver.

Original languageEnglish (US)
Pages (from-to)4959-4964
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number18
DOIs
StatePublished - Sep 15 2006
Externally publishedYes

Keywords

  • Carboxy moiety
  • Pure antiestrogen
  • Steroid scaffold
  • estrogen receptor

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Kanbe, Y., Kim, M. H., Nishimoto, M., Ohtake, Y., Yoneya, T., Ohizumi, I., Tsunenari, T., Taniguchi, K., Kaiho, S. I., Nabuchi, Y., Araya, H., Kawata, S., Morikawa, K., Jo, J. C., Kwon, H. A., Lim, H. S., & Kim, H. Y. (2006). Newly discovered orally active pure antiestrogens. Bioorganic and Medicinal Chemistry Letters, 16(18), 4959-4964. https://doi.org/10.1016/j.bmcl.2006.06.047