a new group of 4-(imidazolylmethyl) quinoline derivatives possessing a methylsulfonyl cox-2 pharmacophore at the para position of the c-2 phenyl ring were designed and synthesized as selective cox-2 inhibitors and in-vitro anti breast cancer agents. in-vitro cox-1 and cox-2 inhibition studies showed that all the compounds were potent and selective inhibitors of the cox-2 isozyme with ic50 value...

Designed as a new group of planar molecule containing the proposed 2-phenylnaphthalene-type structure, a number of 11H-indolo[3.2-c]quinoline derivatives were synthesized and evaluated biologically. Several compounds were found to possess cytotoxic activity against the growth of human promyelocytic leukemia cells (HL-60), against the small cell lung cancer (SCLC), and showed good response in th...

A new series of quinoline derivatives incorporated to glycosides and biologically active heterocyclic moieties were synthesized starting with 6-bromo-4-hydroxyquinaldine (6-bromo-4-hydroxy-2-methylquinoline) compound 1. Some of the synthesized compounds were evaluated for their antibacterial and antifungal activities. Most of the tested compounds exhibited potential antibacterial activity again...

A series of quinoline derivatives as aza analogues of the naphthalene chromophore and a series of "nonfused" tricyclic aromatic systems, in particular 5-arylquinolines and 5- or 6-aryl and heteroaryl naphthalene systems, were synthesized and evaluated for growth-inhibitory properties in several human cell lines. The analysis of quantitative structure-antitumor activity relationships for the gro...

A series of prototypal metal-organic frameworks (MOFs) consisting of polyhedral cages with accessible Lewis-acid sites, have been systematically investigated for Friedländer annulation reaction, a straightforward approach to synthesizing quinoline and its derivatives. Amongst them MMCF-2 demonstrates significantly enhanced catalytic activity compared with the benchmark MOFs, HKUST-1 and MOF-505...

To discover new bioactive lead compounds for medicinal purposes, 2-cyano-3-(4-substituted)-N-(quinolin-3-yl) acrylamide derivatives 2-24, chromenes 25, 26 and benzochromenes 27, 28 were synthesized. The structures of the newly synthesized compounds were confirmed by elemental analyses, IR, 1H NMR and 13C NMR spectroscopies. In addition, the structure of compound 1 was confirmed through X-ray cr...

Two decarboxylative methods providing access to N-alkylated α-trihalomethylated heterocyclic amines have been developed. A batch protocol in which methyl trifluoroacetate acts both as a methylating reagent and subsequently as a nucleophilic trifluoromethyl anion precursor upon its addition to (iso)quinoline derivatives. Next, a telescoped continuous flow process, forming the corresponding α-tri...

An efficient, convenient, and eco-friendly biocatalytic approach was developed for the synthesis of quinoline derivatives via the α-chymotrypsin-catalyzed Friedländer reaction. Interestingly, α-chymotrypsin exhibited higher catalytic activity in an ionic liquid (IL) aqueous solution as compared to that observed in our previous relevant study, which was conducted using an organic solvent, and a ...

Abstract: Background: A series of N-(2,5-dimethylphenyl)-4-pyridin-3-ylpyrimidin-2-amine derivatives were synthesized as Imatinib derivatives, bearing 2-chloroquinoline a heteroaryl motif. Materials and Methods: The compounds by reducing in situ prepared azomethine intermediate using NaBH4 agent methanol solvent. Fourier transformation-IR, proton-NMR along with mass spectrometry used to determi...

In the present study, the synthesis of diethylene triamine supported on cellulose biopolymer as a biodegradable solid basic heterogeneous catalyst was suggested. Then, the applicability of the synthesized catalyst cellulose bonded N-propyl diethylene triamine (CBPDETA) was tested for the synthesis of oxindole derivatives, an important class of potentially bioactive compounds. A various series o...