852569-36-9Relevant academic research and scientific papers
A bioisosteric approach to the discovery of indole carbinol androgen receptor ligands
Lanter, James C.,Fiordeliso, James J.,Allan, George F.,Musto, Amy,Hahn, Do Won,Sui, Zhihua
, p. 5646 - 5649 (2007/10/03)
Two potential bioisosteres of the nonsteroidal antiandrogen bicalutamide, an imidazolidinone and an indole, were synthesized and tested for their androgen receptor binding. Indole was discovered to be a suitable bioisostere for the acyl anilide moiety in the parent compound. Several analogs in the indole series were found to be 10-fold better than bicalutamide in binding to the recombinant androgen receptor binding domain.
Silicon-directed oxa-Pictet-Spengler cyclization and an unusual dimerization of 2-trimethylsilanyl tryptophols
Zhang, Xuqing,Li, Xiaojie,Lanter, James C.,Sui, Zhihua
, p. 2043 - 2046 (2007/10/03)
(Chemical Equation Presented) The tetrahydro-pyrano[3,4-b]indoles 6 were synthesized from 2-(2-trimethylsilanyl-1H-indol-3-yl)-ethanols 5 and various ketones or aldehydes through silicon-directed oxa-Pictet-Spengler cyclizations. An unusual reaction led to the dimeric products 7 when some of 5 was treated with acetone using BF3 as the catalyst.
