A high-throughput screen of the ligand binding domain of the nuclear receptor retinoic acid-related orphan receptor gamma t (RORγt) employing a thermal shift assay yielded a quinoline tertiary alcohol hit. Optimization of the 2-, 3- and 4-positions of the quinoline core using structure-activity...
We describe 10-methyl-9,10-dihydroacridine (AcrH2), as an efficient metal-free photoredox catalyst for the synthesis of quinoline derivatives in a cascade annulation reaction. This new approach to construct multiply disubstituted quinoline derivatives is promoted by UV light. Various quinolines ...
A facile synthesis of 2-difluoromethylated quinolines via DBU-promoted cascade Michael addition/cyclization between functionalized 2-aminobenzonitriles and methyl 4,4-difluorobut-2-ynoate has been developed. Various highly functionalized quinolines were assembled in moderate to good yields under...
A mild and efficient base-mediated propargyl-allenyl isomerization and aza-electrocyclization reaction of trifluoromethylated alkynyl imines have been developed. This method provides a convenient access to 2-trifluoromethylated quinolines in high efficiency.
A new approach to arylated 2-trifluoromethylquinolines based on novel regioselective Suzuki-Miyaura coupling reactions has been developed. Moreover, site-selective, chemo-selective amination reactions were performed. The new 2-trifluoromethylquinoline derivatives were tested as potential NPPs in...
An eco-friendly protocol for the synthesis of various 2-sulfonyl quinolines/pyridines through sulfonylation of heteroaromatic N-oxides with sodium sulfinates in water at ambient temperature under metal- and oxidant-free conditions has been developed. The mild reaction conditions, high reaction e...
This paper describes the synthesis of a novel series of 2-aryl-6-(1H-indol-1-yl)-4-(trifluoromethyl)quinolines, in which aryl = C6H5, 4-CH3C6H4, 4-FC6H4, 4-CF3C6H4 and heteroaryl = 2-thienyl, by an Ullmann-type cooper-catalyzed amination cross-coupling reaction. Photophysical properties of indol...
A new class of quinoline derivatives containing 1,2,4-triazole moiety were synthesized from derivatives of 4-hydroxy-8-(trifluoromethyl)quinoline-3-carbohydrazide 4 through multi-step reactions. The compound 4, on treatment with substituted Isothiocyanates yielded quinoline-thiosemicarbazides 5a...
Quinoline-containing compounds, such as quinine and chloroquine, have a long-standing history as potent antimalarial agents. However, the increasing resistance of the Plasmodium parasite against these drugs and the lack of licensed malaria vaccines have forced chemists to develop synthetic strat...
The present study describes the synthesis of two new series of 3-hydroxy-N-(4-oxo-2-phenyl-1,3-thiazinan-3-yl)-8-(trifluoromethyl)quinoline-2-carboxamide derivatives (4a–j) and 3-((7-chloroquinolin-4-ylamino)methyl)-2-phenyl-1,3-thiazinan-4-one derivatives (5a–7j). All the compounds were synth...
Malaria, in particular infection with P. falciparum (the most lethal of the human malaria parasite species, responsible for nearly one million deaths every year), is one of the most devastating and common infectious disease throughout the world. Beginning with quinine, quinoline containing compo...
Both enantiomers of α-methoxy-(1-naphthyl) acetic acid (1-NMA) were conveniently obtained via fractional crystallization using the enantiomers of 1-(1-naphthyl) ethylamine. 1-NMA was shown to be very powerful for differentiating the enantiomeric signals of quasi-symmetrical aliphatic sulfoxides.
A series of 2,4,6-trisubstituted pyrimidines and 1,3,5-triazines have been synthesized and screened for their in vitro and in vivo antileishmanial activity against Leishmania donovani. Among all, 14 compounds have shown promising inhibition of 80–100% at 10 μg/ml against promastigotes and IC50...
Microtubules are polar cytoskeletal filaments assembled from head-to-tail and comprised of lateral associations of α/β-tubulin heterodimers that play key role in various cellular processes. Because of their vital role in mitosis and various other cellular processes, microtubules have been attr...
A series of thirty-seven 1,3,5-triazine analogues have been synthesized, characterized and evaluated for their antiproliferative activity against a panel of four different human cancer cell lines such as HeLa, HepG2, A549 and MCF-7. Most of the 1,3,5-triazine analogues exhibited promising antipr...
Phosphatidylinositide 3-kinases (PI3Ks) are widely expressed enzymes involved in membrane signalization pathways. Attempts to administer inhibitors with broad activity against different isoforms have failed due to toxicity. Conversely the PI3Kδ isoform is much more selectively expressed, enabli...
The mechanism and the thermodynamic and kinetic factors of the oxygenation of cobalt(II) complexes are discussed based on data available to date. It is shown that the essential features of the oxygenation of cobalt(II) complexes are explicable with the mechanisms to be proposed. Some other perti...
This chapter deals with one of the most exciting aspects of coordination chemistry. Before we explore further, it is very important to understand the fundamentals of this subject. New terminologies such as “ligands”, “complexes”, and “isomerism” are introduced. The applications of coordina...
The kinetics of O2 binding to a vacant coordination site on the cobalt(II) ion have been determined, revealing a radical-like character for the reaction. Reversible oxygenation of Co(II) cyclidenes (C4, C5, C6, C8, C12-bridged and unbridged) was studied by a cryogenic stopped-flow method. In the...
Electrospray ionization mass spectrometry is employed to probe the complexation and dissociation of the first-row transition-metal dications with triethylene tetramine that originate in water/methanol solutions of the corresponding metal salts and the ligand. The major complex ions emerging from...
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