16382-24-4Relevant academic research and scientific papers
Pd-catalyzed direct and selective C-H functionalization: C3-acetoxylation of indoles
Liu, Qiang,Li, Gang,Yi, Hong,Wu, Pan,Liu, Jie,Lei, Aiwen
, p. 2353 - 2357 (2011)
Direct functionalization of C-H bonds has been a hot topic in organic chemistry during recent years. Arenes-one of the most abundant chemical motifs-usually have multiple C-H bonds. Although, some examples of direct functionalizations of arenes have been
2-Aryl-3,3,3-trifluoro-2-hydroxypropionic acids: A new class of protein tyrosine phosphatase 1B inhibitors
Adams, David R.,Abraham, Achamma,Asano, Jun,Breslin, Catherine,Dick, Colin A.J.,Ixkes, Ulrich,Johnston, Blair F.,Johnston, Derek,Kewnay, Justin,Mackay, Simon P.,MacKenzie, Simon J.,McFarlane, Morag,Mitchell, Lee,Spinks, Daniel,Takano, Yasuo
, p. 6579 - 6583 (2008/09/16)
A new series of non-peptidic, mono-acid protein tyrosine phosphatase 1B (PTP1B) inhibitors has been identified by structure-based design. Compounds with 2-(indol-3-yl)- and 2-phenyl-3,3,3-trifluoro-2-hydroxypropionic acid core units targeted at the enzyme's primary site and a hydrophobic chlorophenylthiazole extension in its 2° site exhibit 3-60 μM IC50s for PTP1B inhibition in an Sf9 cell-based assay.
A novel class of inhibitors for human steroid 5α-reductase: Synthesis and biological evaluation of indole derivatives. II
Igarashi, Susumu,Inami, Hiroshi,Hara, Hiromu,Fujii, Masahiro,Koutoku, Hiroshi,Oritani, Hiroyuki,Mase, Toshiyasu
, p. 382 - 388 (2007/10/03)
In a search for novel nonsteroidal inhibitors of human prostatic 5α- reductase, we found a new series of indole derivatives that showed potent inhibitory activities for the human enzyme. Among them, 4-[(1-benzyl-1- Hindol-5-yl)oxy]-3-chlorobenzoic acid (2d, YM-32906) showed more potent inhibitory activity than finasteride with an IC50 value of 0.44 nM. 3- Chloro-4-{[1-(4-phenoxybenzyl)-1H-indol-5-yl]oxy}benzoic acid (2m) showed inhibitory activities for both human and rat prostatic 5α-reductase with IC50 values of 2.1 and 73 nM, respectively. The synthesis and structure- activity relationships of these indole derivatives are presented.
