Simplification of bottom ring and regioselective functionalization of the indolocarbazole unit of staurosporine (2) are described. The modification led to a new series of simplified staurosporine analogs, which exhibited significant inhibitory activity against Janus kinase 3 (JAK3). The structure-activity relationships (SAR) are discussed and a proposed binding model is also highlighted.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2006.10.062 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Geissospermiculatine, a New Alkaloid from Bark.
Molecules
December 2020
Department of Physical Chemistry, Faculty of Pharmacy with Laboratory Medicine Division, Medical University of Warsaw, 02-097 Warsaw, Poland.
A new alkaloid, geissospermiculatine was characterized in A. H. Gentry bark (Apocynaceae).
View Article and Find Full Text PDFMicroparticle-Assisted Precipitation Screening Method for Robust Drug Target Identification.
Anal Chem
October 2020
CAS Key Laboratory of Separation Sciences for Analytical Chemistry, National Chromatographic R&A Center, Dalian Institute of Chemical Physics, Chinese Academy of Sciences (CAS), Dalian 116023, China.
While thermal proteome profiling (TPP) shines in the field of drug target screening by analyzing the soluble fraction of the proteome samples treated at high temperature, the counterpart, the insoluble precipitate, has been overlooked for a long time. The analysis of the precipitate is hampered by the inefficient sample processing procedure. Herein, we propose a novel method, termed microparticle-assisted precipitation screening (MAPS), for drug target identification.
View Article and Find Full Text PDFAn isothermal shift assay for proteome scale drug-target identification.
Commun Biol
February 2020
Department of Molecular, Cellular and Developmental Biology, University of Colorado, Boulder, CO, 347 UCB, USA.
Most small molecule drugs act on living systems by physically interacting with specific proteins and modulating target function. Identification of drug binding targets, within the complex milieu of the human proteome, remains a challenging task of paramount importance in drug discovery. Existing approaches for target identification employ complex workflows with limited throughput.
View Article and Find Full Text PDFColonyArea: an ImageJ plugin to automatically quantify colony formation in clonogenic assays.
PLoS One
November 2014
Turku Centre for Biotechnology, University of Turku and Åbo Akademi University, Turku, Finland.
The clonogenic or colony formation assay is a widely used method to study the number and size of cancer cell colonies that remain after irradiation or cytotoxic agent administration and serves as a measure for the anti-proliferative effect of these treatments. Alternatively, this assay is used to quantitate the transforming potential of cancer associated genes and chemical agents. Therefore, there is a need for a simplified and standardized analysis of colony formation assays for both routine laboratory use and for parallelized automated analysis.
View Article and Find Full Text PDFIn vitro approach to predict post-translational phosphorylation response to mixtures.
Toxicology
November 2013
C Eugene Bennett Department of Chemistry, West Virginia University, Morgantown, WV 26506, United States. Electronic address:
While exposure to chemical mixtures is an everyday reality, an understanding of their combined effects, and any potential prediction thereof, is extremely limited. Realistic exposures potentially consist of hundreds to thousands of chemicals per day, but even relatively simple binary mixture interactions can be inherently difficult to predict based upon the lack of temporal and spatial mechanisms for the individual constituents. To this end, we explore the concept of capitalizing on downstream convergence of intracellular signal transduction to experimentally simplify the means of determining xenobiotics that, when combined, could result in increased or unexpected toxicity.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!