Search
Now showing items 1-10 of 28
Pyrimidine-fused derivatives: Synthetic strategies and medicinal attributes
(Bentham Science Publishers B.V., 2016)
Pyrimidine-fused derivatives traits the inextricable part of DNA and RNA, exhibit indispensable role in numerous biological processes, possessing momentous chemical and biological importance. Pyrimidine-condensed derivatives ...
Epidermal Growth Factor Receptor (EGFR) and its Cross-Talks with Topoisomerases: Challenges and Opportunities for Multi-Target Anticancer Drugs
(Bentham Science Publishers B.V., 2016)
Background: The interactions of Epidermal Growth Factor Receptor (EGFR) and topoisomerases have been seen in various cancer including brain, breast, ovarian, colorectal, gastric, etc. Methods: The studies in adenocarcinoma ...
Natural products based ayurvedic formulations: Chemical constituents and treatment in neurodegenerative disorders
(Bentham Science Publishers B.V., 2017)
Neurodegenerative diseases are linked with high morbidity and mortality rates. Medical science has made considerable progress in understanding the mechanisms associated with the development of the neurodegenerative diseases. ...
Pyrimidine containing epidermal growth factor receptor kinase inhibitors: Synthesis and biological evaluation
(Blackwell Publishing Ltd, 2017)
Structure-based design and synthesis of pyrimidine containing reversible epidermal growth factor receptor (EGFR) inhibitors 1a?d are reported. The compounds (1a?d) inhibited the EGFR kinase activity in vitro with IC50 range ...
Toward an Understanding of Structural Insights of Xanthine and Aldehyde Oxidases: An Overview of their Inhibitors and Role in Various Diseases
(John Wiley and Sons Inc., 2018)
Almost all drug molecules become the substrates for oxidoreductase enzymes, get metabolized into more hydrophilic products and eliminated from the body. These metabolites sometime may be more potent, active, inactive, or ...
Synthesis and biological evaluation of new 2, 5- dimethylthiophene/furan based N-acetyl pyrazolines as selective topoisomerase II inhibitors
(Royal Society of Chemistry, 2016)
Based on the reported pharmacophores as topoiomerase inhibitors, 2,5 dimethylthiophen/furan based N-acetyl pyrazolines were designed and envisaged as topoisomerase inhibitors. The target compounds were synthesized and ...
Dual inhibitors of epidermal growth factor receptor and topoisomerase IIa derived from a quinoline scaffold
(Royal Society of Chemistry, 2016)
Based on the quinazoline bearing EGFR inhibitors, a series of thirty four compounds having a quinoline scaffold were synthesised and evaluated in vitro for EGFR kinase inhibitory activity. A structure-activity relationship ...
Unanticipated Cleavage of 2-Nitrophenyl-Substituted N-Formyl Pyrazolines under Bechamp Conditions: Unveiling the Synthesis of 2-Aryl Quinolines and Their Mechanistic Exploration via DFT Studies
(American Chemical Society, 2018)
We herein report for the first time an unusual decomposition of 2-nitrophenyl-substituted N-formyl pyrazolines under Bechamp reduction condition employed to yield 2-aryl quinolines exclusively instead of pyrazolo[1,5-c]q ...
Synthetic versus enzymatic pictet-spengler reaction: An overview
(Bentham Science Publishers B.V., 2018)
Background: Pictet-Spengler reactions is an irreplaceable part of cyclization reaction leading to the formation of indispensable heterocyclic moieties including imidazole, benzoxazole, pyrrole, indole and others having ...
Imine/amide-imidazole conjugates derived from 5-amino-4-cyano-N1-substituted benzyl imidazole: Microwave-assisted synthesis and anticancer activity via selective topoisomerase-II-? inhibition
(Elsevier Ltd, 2015)
Microwave-accelerated synthesis and anticancer activity of novel imine/amide-imidazole conjugates derived from 5-amino-4-cyano-N1-substituted benzyl imidazole against a panel of seven cancer cell lines are reported for the ...