3419-00-9Relevant articles and documents
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.
A new approach to 5-hydroxyindoles from 1,4-cyclohexanedione
Ozaki, Yutaka,Okamura, Kyouko,Hosoya, Ayako,Kim, Sang-Won
, p. 679 - 680 (2007/10/03)
Several kinds of 2-substituted 5-hydroxyindoles were prepared by the procedure starting from the condensation of 1,4-cyclohexanedione with N-protected α-amino aldehydes in the presence of lithium chloride. The substitutent on 2-position of the indole ring
