منابع مشابه
Synthesis and preliminary evaluation of 5,7-dimethyl-2-aryl-3H-pyrrolizin-3-ones as angiogenesis inhibitors.
Sunitinib (Sutent®) is a receptor tyrosine kinase (RTK) and angiogenesis inhibitor approved for the treatment of renal cell carcinomas, gastrointestinal stromal tumours and pancreatic neuroendocrine tumours. A key structural motif retained throughout medicinal chemistry efforts during sunitinib's development was the indoline-2-one group. In the search for new anti-angiogenic scaffolds, we previ...
متن کامل1,2-dithiole-3-ones as potent inhibitors of the bacterial 3-ketoacyl acyl carrier protein synthase III (FabH).
The enzyme FabH catalyzes the initial step of fatty acid biosynthesis via a type II dissociated fatty acid synthase. The pivotal role of this essential enzyme, combined with its unique structural features and ubiquitous occurrence in bacteria, has made it an attractive new target for the development of antibacterial and antiparasitic compounds. We have searched the National Cancer Institute dat...
متن کاملSome fused heterocyclic compounds as eukaryotic topoisomerase II inhibitors.
Our previously synthesized 37 compounds, which are 2,5,6-substituted benzoxazole, benzimidazole, benzothiazole, and oxazolo(4,5-b)pyridine derivatives, were tested for their eukaryotic DNA topoisomerase II inhibitory activity in cell free system and 28 were found to inhibit the topoisomerase II at an initial concentration of 100 microg/ml. After further testing at a lower range of concentration...
متن کاملAmido-3-hydroxypyridin-4-ones as iron(III) ligands.
The synthesis and physicochemical properties of a range of 2- and 6-amido-3-hydroxypyridin-4-ones are described. All the amido-substituted 3-hydroxypyridin-4-ones have lower pK(a) values than 1,2-dimethyl-3-hydroxypyridin-4-one (deferiprone). This is due to the inductive effect of the amido group. Furthermore, the pK(a) values of the 3-hydroxy group in 1-nonsubstituted pyridinones are dramatica...
متن کاملSynthesis and Antimicrobial Evaluation of 4H-Pyrans and Schiff Bases Fused 4H-Pyran Derivatives as Inhibitors of Mycobacterium Bovis (BCG)
The focus of our study is the synthesis and biological activity evaluation of a series of 4H-Pyran compounds and schiff bases fused 4H-Pyran derivatives which are known to possess a wide variety of biological activities. In this paper at first a simple and efficient one-pot synthesis of 4H-Pyran s from the three-component reaction between malononitrile, aldehydes, and active methylene compounds...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2014
ISSN: 1948-5875,1948-5875
DOI: 10.1021/ml500090s