1457-52-9Relevant academic research and scientific papers
Nickel-Catalyzed Tandem Knoevenagel Condensation and Intramolecular Direct Arylation: Synthesis of Pyrazolo[5,1-a]-isoquinoline Derivatives
Dhiman, Shiv,Nandwana, Nitesh Kumar,Saini, Hitesh Kumar,Kumar, Dalip,Rangan, Krishnan,Robertson, Katherine N.,Jha, Mukund,Kumar, Anil
, p. 1973 - 1983 (2018/03/27)
A simple and efficient method for the synthesis of pyrazolo[5,1-a]isoquinoline derivatives has been developed using the nickel-catalyzed reaction of 1-aryl-2-(1H-pyrazol-1-yl)ethan-1-ones and 2-bromo aldehydes. The overall transformation involves tandem K
Synthesis and biological evaluation of novel azole derivatives as selective potent inhibitors of brassinosteroid biosynthesis
Yamada, Kazuhiro,Yajima, Osamu,Yoshizawa, Yuko,Oh, Keimei
, p. 2451 - 2461 (2013/06/27)
Brassinosteroids (BRs) are phytohormones that control several important agronomic traits, such as flowering, plant architecture, seed yield, and stress tolerance. To manipulate the BR levels in plant tissues using specific inhibitors of BR biosynthesis, a series of novel azole derivatives were synthesized and their inhibitory activity on BR biosynthesis was investigated. Structure-activity relationship studies revealed that 2RS, 4RS-1-[4-(2- allyloxyphenoxymethyl)-2-(4-chlorophenyl)-[1,3]dioxolan-2-ylmethyl]-1H-[1,2,4] triazole (G2) is a highly selective inhibitor of BR biosynthesis, with an IC50 value of approximately 46 ± 2 nM, which is the most potent BR biosynthesis inhibitor observed to date. Use of gibberellin (GA) biosynthesis mutants and BR signaling mutants to analyze the mechanism of action of this synthetic series indicated that the primary site of action is BR biosynthesis. Experiments feeding BR biosynthesis intermediates to chemically treated Arabidopsis seedlings suggested that the target sites of this synthetic series are CYP90s, which are responsible for the C-22 and/or C-23 hydroxylation of campesterol.
PYRROLO [2,3-D] PYRIMIDIN DERIVATIVES AS PROTEIN KINASE B INHIBITORS
-
Page/Page column 145-146, (2009/05/30)
The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I)
