90405-67-7Relevant articles and documents
ANTITUMOR-EFFECT ENHANCER USING PYRAZOLO[3,4-D]PYRIMIDINE COMPOUND
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Paragraph 0310; 0390, (2020/01/22)
To provide a method for treating cancer using a pyrazolo[3,4-d]pyrimidine compound or a salt thereof. The present invention provides an antitumor agent comprising a pyrazolo[3,4-d]pyrimidine compound of formula (I) wherein X, Y, Z1, Z2/su
Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold
Johansson, Henrik,Boesgaard, Michael Worch,N?rskov-Lauritsen, Lenea,Larsen, Inna,Kuhne, Sebastiaan,Gloriam, David E.,Br?uner-Osborne, Hans,Sejer Pedersen, Daniel
, p. 8938 - 8951 (2015/12/09)
G protein-coupled receptors (GPCRs) represent a biological target class of fundamental importance in drug therapy. The GPRC6A receptor is a newly deorphanized class C GPCR that we recently reported for the first allosteric antagonists based on the 2-arylindole privileged structure scaffold (e.g., 1-3). Herein, we present the first structure-activity relationship study for the 2-arylindole antagonist 3, comprising the design, synthesis, and pharmacological evaluation of a focused library of 3-substituted 2-arylindoles. In a FRET-based inositol monophosphate (IP1) assay we identified compounds 7, 13e, and 34b as antagonists at the GPRC6A receptor in the low micromolar range and show that 7 and 34b display >9-fold selectivity for the GPRC6A receptor over related GPCRs, making 7 and 34b the most potent and selective antagonists for the GPRC6A receptor reported to date.
An efficient method for one-carbon elongation of aryl aldehydes via their dibromoalkene derivatives
Huh, Dal Ho,Jeong, Ji Sang,Lee, Hee Bong,Ryu, Hoejin,Kim, Young Gyu
, p. 9925 - 9932 (2007/10/03)
Various aryl aldehydes were efficiently converted into one-carbon extended aryl acetamides or aryl acetic acids through the reaction of their dibromoalkene derivatives with pyrrolidine in the presence of water under very mild conditions.