Pseudosaccharin Amine Derivatives: Synthesis and Elastase Inhibitory Activity.

Rode, Haridas B.; Sprang, Thomas; Besch, A.; Loose, Jutta; Otto, Hans‐Hartwig

doi:10.1002/chin.200605119

Cited by 10 publications

(12 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Based on numerous reports revealing saccharin derivatives as elastase inhibitors, a series of pseudosaccharinamine derivatives was envisaged, synthesized and evaluated for elastase inhibitory activity. Some of those were found to be potent and reversible inhibitors of HLE in the low micromolar range [56,57].…”

Section: Biologically Active Derivativesmentioning

confidence: 98%

Advances in the Chemistry of Saccharins: From Synthetic Novelties Towards Biologically Active Compounds

Ms¹

2010

CMC

View full text Add to dashboard Cite

The saccharin ring system has gained considerable attention in the past decades, especially in the field of medicinal chemistry. The wide applicability of saccharin derivatives remains the driving force behind the constant development of novel routes and methods that provide new access to the construction of saccharin. Since the functionalization of this heterocycle has proved difficult, except for N- and O-alkylation, novel strategic approaches are much sought-after and thus constitute a great value to any medicinal chemist. In addition to the synthetic novelties introduced into the synthesis and functionalization of this particular heterocycle, the numerous newly discovered biological activities of saccharin and its derivatives are also reviewed. Saccharin may be considered to constitute a privileged framework on account of its role as a key structural element in several biologically active compounds ranging from enzyme inhibitors to receptor ligands and beyond.

show abstract

Section: Biologically Active Derivativesmentioning

confidence: 98%

Advances in the Chemistry of Saccharins: From Synthetic Novelties Towards Biologically Active Compounds

Ms¹

2010

CMC

View full text Add to dashboard Cite

show abstract

“…). Quinoxaline itself is prepared by the reaction of o ‐phenylenediamine and α‐ketocarboxylic acids through different methods including one‐pot and microwave methods . One‐pot efficient green synthesis of 1,4‐dihydroquinoxaline‐2,3‐dione derivatives has been achieved in a one‐pot reaction at room temperature under solvent free conditions by a simple grinding method .…”

Section: Synthetic Strategies For Quinoxalinesmentioning

confidence: 99%

Quinoxaline‐Based Scaffolds Targeting Tyrosine Kinases and Their Potential Anticancer Activity

Newahie

Ismail

Ella

et al. 2016

Archiv der Pharmazie

View full text Add to dashboard Cite

Quinoxaline derivatives, also called benzopyrazines, are an important class of heterocyclic compounds. Quinoxalines have drawn great attention due to their wide spectrum of biological activities. They are considered as an important basis for anticancer drugs due to their potential activity as protein kinase inhibitors. In this review, we focus on the chemistry of the quinoxaline derivatives, the strategies for their synthesis, their potential activities against various tyrosine kinases, and on the structure-activity relationship studies reported to date.

show abstract

“…Saccha-rine was chlorinated using phosphorous pentachloride by fusion to give 3-chloropseudosaccharine 4. Compounds 5a-c were obtained by reacting amine derivatives ( 3a-c )with compound 4 in refl uxing dioxane and purifi cation of the resulted precipitate [ 26 ]. Carbonyl group are historically recognized as a biosiostere for the sulfoxide group [ 27 ].…”

Section: Chemistrymentioning

confidence: 99%

“…The resulted solid was fi ltered washed with dioxane twice and washed with diethyl ether and dried to give compounds ( 5a-c, 8, 9 ) in a pure form. [ 26 ]…”

Section: Conclusion ▼mentioning

confidence: 99%

Virtual Screening and Synthesis of New Chemical Scaffolds as VEGFR-2 Kinase Inhibitors

Elsayed

El‐Araby

Serya

et al. 2012

Arzneimittelforschung

View full text Add to dashboard Cite

VEGFR-2 tyrosine kinase inhibitors are currently receiving high interest in drug discovery process as anticancer agents. We have used virtual screening techniques in order to discover new scaffolds that can be used for developing new VEGFR-2 kinase inhibitors.Similarity ensemble approach was used to reduce the chemical space of ZINC database to select a subset of compounds. A validated structure-based pharmacophore was developed and adopted to screen the selected subset. Initial hits mapped to the pharmacophore were filtered using docking and scoring. Selected compounds were synthesized and biologically tested. Compound 9 showed very good cytotoxicity profile against the NCI 60 cancer cell lines, while compound 8 showed reasonable inhibition of VEGFR-2 tyrosine kinase.Stepwise virtual screening of databases such as ZINC may result in new scaffolds for developing VEGFR-2 kinase inhibitors.

show abstract

Pseudosaccharin Amine Derivatives: Synthesis and Elastase Inhibitory Activity.

Cited by 10 publications

References 0 publications

Advances in the Chemistry of Saccharins: From Synthetic Novelties Towards Biologically Active Compounds

Advances in the Chemistry of Saccharins: From Synthetic Novelties Towards Biologically Active Compounds

Quinoxaline‐Based Scaffolds Targeting Tyrosine Kinases and Their Potential Anticancer Activity

Virtual Screening and Synthesis of New Chemical Scaffolds as VEGFR-2 Kinase Inhibitors

Contact Info

Product

Resources

About