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ChemInform Abstract: Synthesis and Structure—Activity Relationships of New Nonsteroidal Progesterone Receptor Ligands.

✍ Scribed by Ken-ichi Kurihara; Kiyoshi Tanabe; Yasuo Yamamoto; Rie Shinei; Keiichi Ajito; Tsuneo Okonogi

Publisher
John Wiley and Sons
Year
2010
Weight
37 KB
Volume
30
Category
Article
ISSN
0931-7597

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✦ Synopsis

Synthesis and Structure-Activity Relationships of New Nonsteroidal Progesterone Receptor Ligands.

-Title ligands such as (XI) and (XVI), based on a culture extract of Penicillium oblatum with a ligularenolide skeleton, are synthesized modifying the structure, mainly by introduction or removal of a methyl group. Replacement of 7β-OH of the parent compound with 7α-Me (XI) leads to an increase of binding affinity. Further modification of the basic skeleton at this position could be an attractive strategy for the higher binding affinity for the progesterone receptor. -(KURIHARA, KEN-ICHI;

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