23796-95-4Relevant academic research and scientific papers
Development of androgen receptor ligands by application of ten-vertex para-carborane as a novel hydrophobic core structure
Fujii, Shinya,Ohta, Kiminori,Goto, Tokuhito,Oda, Akifumi,Masuno, Hiroyuki,Endo, Yasuyuki,Kagechika, Hiroyuki
, p. 680 - 684 (2012)
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.
The polyhedral B6C2H8, B7C2H9, and B8C2H10 carboranes and their C-monomethyl and C-monophenyl derivatives
Garrett, Philip M.,Smart, James C.,Ditta, Gary S.,Hawthorne, M. Frederick
, p. 1907 - 1910 (2008/10/08)
The pyrolysis of 1,3-B7C2H13 at 215° in the absence of diborane yields the B6C2H8, B7C2H9, and 1,6-B8C2H10 carboranes, while in the presence of diborane the yield of 1,6-B8C2H10 is considerably enhanced. Isomerization of 1,6-B8C2H10 to the 1,10-B8C2H10 isomer occurs at 300°. Pyrolysis of 1,3-NaB7C2H12 at 200° yields 1,7-B7C2H9. The C-monomethyl and C-monophenyl derivatives of these carboranes are also described.
