Journal
MEDCHEMCOMM
Volume 3, Issue 6, Pages 680-684Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2md00294a
Keywords
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Funding
- Ministry of Education, Culture, Sports, Science and Technology, Japan [21790110]
- Japan Science Society [20-605]
- Grants-in-Aid for Scientific Research [21790110, 20390035, 24790115, 23790137, 23659051, 23790128, 22136013] Funding Source: KAKEN
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We report here the design, synthesis, androgenic activity and anti-androgenic activity of novel derivatives of hexadecahedral 1,10-dicarba-closo-decaborane, which is generally called ten-vertex para-carborane. The synthesized compounds exhibited very high binding affinity for the androgen receptor and showed anti-androgenic activity toward the androgen-dependent SC-3 cell line. Two compounds also exhibited partial agonistic activity in SC-3 assay. The docking studies of carborane derivatives to AR demonstrate that ten-vertex carborane is useful for development of novel bioactive compounds as well as twelve-vertex carboranes that are well known to be versatile pharmacophores. Ten-vertex carborane, which has not previously been applied in the field of medicinal chemistry, appears to have potential as a hydrophobic pharmacophore with characteristic properties.
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