159307-02-5Relevant articles and documents
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.
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.
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.
