Search results for "Quinoline"
showing 10 items of 391 documents
2,2-Diphenylbenzo[c]quinoline-1-oxyl
2009
In the title compound, C25H18NO, a stable phenanthridinic nitroxide, the ring containing the nitroxide function assumes a twist-boat conformation and the dihedral angle formed by adjacent benzene rings is 21.78 (5)°. The phenyl substituents at position 2 are approximately orthogonal to each other, forming a dihedral angle of 81.04 (4)°. The crystal structure is stabilized by an intramolecular C—H...O hydrogen bond and by C—H...π interactions.
Medication-related osteonecrosis of the jaw in a cancer patient receiving lenvatinib.
2018
Medication-related osteonecrosis of the jaw (MRONJ) is an adverse drug reaction that affects the mandible and maxilla of patients exposed to bone-targeting agents such as anti-resorptive and anti-angiogenic agents. Several MRONJ cases have been reported after dental extractions in patients under treatment with anti-angiogenic agents, including receptor activator of nuclear factor κB ligand (RANKL) inhibitor, anti-vascular endothelial growth factor (anti-VEGF) monoclonal antibody, mammalian target of rapamycin (mTOR) inhibitors, and tyrosine kinase inhibitors (TKIs). The aim of this article was to describe an original case of lenvatinib-related osteonecrosis of the jaw in a patient affected …
Nonalcoholic steatohepatitis in hepatocarcinoma: new insights about its prognostic role in patients treated with lenvatinib
2021
Background Hepatocellular carcinoma (HCC) treatment remains a big challenge in the field of oncology. The liver disease (viral or not viral) underlying HCC turned out to be crucial in determining the biologic behavior of the tumor, including its response to treatment. The aim of this analysis was to investigate the role of the etiology of the underlying liver disease in survival outcomes. Patients and methods We conducted a multicenter retrospective study on a large cohort of patients treated with lenvatinib as first-line therapy for advanced HCC from both Eastern and Western institutions. Univariate and multivariate analyses were performed. Results Among the 1232 lenvatinib-treated HCC pat…
Triazolopyridines 20. Hydrogenation reactions
1999
Abstract Hydrogenation reactions of some [1,2,3]triazolo[1,5-a]pyridines and their benzo derivatives, [1,2,3]-triazolo[1,5-a]quinoline and [1,2,3]triazolo[5,1-a]isoquinoline are studied. In general, the pyridine ring is more easily hydrogenated than the triazole or benzene rings.
SYNTHESIS OF PYRROLO[3,2-H]QUINOLINONES WITH GOOD PHOTOCHEMOTHERAPEUTIC ACTIVITY AND NO DNA DAMAGE
2010
In the search for new photochemotherapeutic agents, a series of derivatives of the ring system pyrrolo[3,2-h]quinoline--bioisosters of the angular furocoumarin angelicin--were synthesized through a four-step synthetic approach, in reasonable overall yields. Eight of the synthesized derivatives showed a remarkable phototoxicity against a panel of four human tumor cell lines and a great dose UV-A dependence, reaching IC₅₀ values at submicromolar level. The mode of cellular death photoinduced by pyrrolo[3,2-h]quinolines was evaluated through a series of flow cytometric analysis and other tests were performed to clarify their mechanism of action.
Cytotoxicity of a naturally occurring furoquinoline alkaloid and four acridone alkaloids towards multi-factorial drug-resistant cancer cells
2015
Abstract Introduction Chemotherapy is one of the preferred mode of treatment of malignancies, but is complicated by the expression of diverse resistance mechanisms of cancer cells. Methods In the present study, we investigated the cytotoxicity of five alkaloids including a furoquinoline montrofoline (1) and four acridones namely 1-hydroxy-4-methoxy-10-methylacridone (2), norevoxanthine (3), evoxanthine (4), 1,3-dimethoxy-10-methylacridone (5) against 9 drug-sensitive and multidrug-resistant (MDR) cancer cell lines. The resazurin reduction assay was used to evaluate the cytotoxicity of these compounds, whilst caspase-Glo assay was used to detect caspase activation. Cell cycle, mitochondrial …
1-(2′-Bromobenzyl)-6,7-dihydroxy-N-methyl-tetrahydroisoquinoline and 1,2-Demethyl-nuciferine as Agonists in Human D2 Dopamine Receptors
2020
Certain D2-like dopamine receptor (DR) agonists are useful therapeutically as antiparkinsonian drugs, whereas D2-like DR antagonists or partial agonists are proven effective as antipsychotics. Two ...
Synthesis of hexahydrocyclopenta[ij]isoquinolines as a new class of dopaminergic agents.
2014
In this study, we have described the synthesis of the tricyclic 1,2,3,7,8,8a-hexahydrocyclopenta [ij]isoquinoline (HCPIQ). Herein, six differently substituted 5,6-dioxygenated-7-phenyl-HCPIQs have been synthesized using a new methodology via (E)-1-styryl-THIQ by Friedel-Crafts cyclization with Eaton's reagent. Results showed that HCPIQs (3, 3a-e) displayed a moderate affinity for D1 dopamine receptors (DR) in the micromolar range, furthermore the catecholic HCPIQs 3a (NH), 3c (NCH3) and 3e (NCH2CHCH2) exhibited outstanding affinity and high selectivity towards D2 DR. Indeed, 3a, 3c and 3e showed Ki values of 29 nM, 13 nM and 18 nM, respectively, and HCPIQs 3a (NH) and 3c (NCH3) displayed a …
Acetogenins, Aporphinoids, and Azaanthraquinone from Annona cherimolia Seeds.
1989
We have isolated several known steroids, glycosides, isoquinoline, and azaanthraquinone alkaloids, and five acetogenins belonging to a new group of secondary metabolites, the bis-tetrahydrofuran gamma-lactones, from the seeds of ANNONA CHERIMOLIA. The azaanthraquinone alkaloid isolated was identified as cleistopholine. One new acetogenin is reported here: laherradurine; a second new one was isolated, but its structure has not been determined. The other three: cherimoline, dihydrocherimoline, and asimicine have already been reported.
Relationships between structure and vascular activity in a series of benzylisoquinolines
1997
1 1In the present work, the properties of 3-methyl isoquinoline, 3,4-dihydropapaverine, tetrahydropapaverine and tetrahydropapaveroline were compared with those of papaverine and laudanosine. The work includes functional studies on rat isolated aorta contracted with noradrenaline, caffeine or KC1, and a determination of the affinity of the compounds for α1-adrenoceptors and calcium channel binding sites, with [#H]-prazosin, [#H]-nitrendipine and [#H]-(+)-cis-diltiazem binding to rat cerebral cortical membranes. The effects of papaverine derivatives on the different molecular forms of cyclic nucleotide phosphodiesterases (PDE) isolated from bovine aorta were also determined. 2 2The three pap…