159307-02-5Relevant academic research and scientific papers
Total Synthesis of (+)-Dendrowardol C
Wolleb, Helene,Carreira, Erick M.
, p. 10890 - 10893 (2017)
The first total synthesis of the tetracyclic sesquiterpenoid (+)-dendrowardol C is described. It relies on an intramolecular aldol reaction to forge the central bicyclic scaffold and subsequent cyclobutane formation by cyclization of a γ-triflyloxy ketone. Key is the treatment of the latter with lithium naphthalenide. Finally, the diastereoselective hydroboration of a 1,1-disubstituted double bond is enabled by a chiral CoI catalyst.
CYANOPYRROLIDINES AS DUB INHIBITORS FOR THE TREATMENT OF CANCER
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Page/Page column 82, (2017/02/09)
The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C- terminal hydrolase L1 (UCHL1) and ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of cancer and conditions involving mitochondrial dysfunction. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1,R2,R3,R4,R5,R6,R7,R8 and R9 are as defined herein.
Fragment-based discovery of 6-azaindazoles as inhibitors of bacterial DNA ligase
Howard, Steven,Amin, Nader,Benowitz, Andrew B.,Chiarparin, Elisabetta,Cui, Haifeng,Deng, Xiaodong,Heightman, Tom D.,Holmes, David J.,Hopkins, Anna,Huang, Jianzhong,Jin, Qi,Kreatsoulas, Constantine,Martin, Agnes C. L.,Massey, Frances,McCloskey, Lynn,Mortenson, Paul N.,Pathuri, Puja,Tisi, Dominic,Williams, Pamela A.
supporting information, p. 1208 - 1212 (2014/01/06)
Herein we describe the application of fragment-based drug design to bacterial DNA ligase. X-ray crystallography was used to guide structure-based optimization of a fragment-screening hit to give novel, nanomolar, AMP-competitive inhibitors. The lead compound 13 showed antibacterial activity across a range of pathogens. Data to demonstrate mode of action was provided using a strain of S. aureus, engineered to overexpress DNA ligase.
Macrocyclic complexing agents and targeting immunoreagents useful in therapeutic and diagnostic compositions and methods
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, (2008/06/13)
A metal chelate comprising a compound having the following formula and one or more metal ions which metal ions are a radionucleotide or a paramagnetic metal ion: STR1
Unsymmetrical complexing agents and targeting immunoreagents useful in thearpeutic and diagnostic compositions and methods
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, (2008/06/13)
STR1 Unsymmetrical oligo-2,6-pyridine complexing agents, metal chelates and targeting immunoreagents containing such complexing agents are provided, as well as diagnostic and therapeutic compositions containing such immunoreagents and diagnostic and therapeutic methods of using the immunoreagents.
2-acetyl-6-cyanopyridines and their use as intermediates in the synthesis of oligo-2,6-pyridines
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, (2008/06/13)
The present invention is directed to 2-acetyl-6-cyanopyridine compounds that are useful as intermediates in the synthesis of oligo-2,6-pyridines. The present invention is also directed to new, simpler, less expensive methods for synthesizing such oligopyridines using the novel 2-acetyl-6-cyanopyridine compounds as intermediates.
