Search results for "Indazole"
showing 10 items of 63 documents
Equilibrium, Kinetic, and Computational Studies on the Formation of Cu2+ and Zn2+ Complexes with an Indazole-Containing Azamacrocyclic Scorpiand: Evi…
2015
Cu(2+) and Zn(2+) coordination chemistry of a new member of the family of scorpiand-like macrocyclic ligands derived from tris(2-aminoethyl)amine (tren) is reported. The new ligand (L1) contains in its pendant arm not only the amine group derived from tren but also a 6-indazole ring. Potentiometric studies allow the determination of four protonation constants. UV-vis and fluorescence data support that the last protonation step occurs on the indazole group. Equilibrium measurements in the presence of Cu(2+) and Zn(2+) reveal the formation of stable [ML1](2+), [MHL1](3+), and [ML1(OH)](+) complexes. Kinetic studies on the acid-promoted decomposition of the metal complexes were carried out usi…
Behavioural and pharmacological characterization of a novel cannabinomimetic adamantane-derived indole, APICA, and considerations on the possible mis…
2015
The novel adamantane derivative APICA (N-(adamantan-1-yl)-1-pentyl-1H-indole-3-carboxamide) was recently identified as a cannabinomimetic indole of abuse. Despite its novel structure, APICA recalls cannabinomimetic indoles, such as representative member JWH-018.In present study, the effects of APICA (1-3 mg/kg, i.p.) were tested in C57BL/6J mice, in the Tetrad task which includes the assessment of: body temperature; locomotor activity and behavioural reactivity; nociception; motor coordination; declarative memory. Furthermore, pre-treatment with the CB1 antagonist AM251 (3 mg/kg, i.p.) or the CB2 antagonist AM630 (3 mg/kg, i.p.) was carried out to characterize APICA activity.Our results sho…
Cisplatin and epirubicin plus oral lonidamine as first-line treatment for metastatic breast cancer: A phase II study of the Southern Italy Oncology G…
1998
Lonidamine (LND) is a unique antineoplastic drug derived from indazole-3-carboxylic acid which inhibits oxygen consumption and aerobic glycolysis, interfering with energy metabolism of neoplastic cells. LND has been experimentally shown to potentiate the cytotoxic effects of epirubicin (EPI) in human breast cancer cell lines, cisplatin activity in both platinum-sensitive and -resistant human ovarian carcinoma cell lines, and EPI antineoplastic activity in some recent phase III trials carried out in advanced breast cancer. A multicenter phase II trial was carried out with the combination of cisplatin 60 mg/m2, EPI 100 mg/m2 and LND 450 mg/day p.o. in three refracted doses/day starting 2 days…
Selective electrochemical discrimination between dopamine and phenethylamine-derived psychotropic drugs using electrodes modified with an acyclic rec…
2010
Electrochemical discrimination between dopamine and psychotropic drugs which have in common a skeletal structure of phenethylamine, can be obtained using acyclic receptors L(1) and L(2), containing two terminal 3-alkoxy-5-nitroindazole rings. Upon attachment to graphite electrodes, L(1) and L(2) exhibit a well-defined, essentially reversible solid state electrochemistry in contact with aqueous media, based on electrolyte-assisted reduction processes involving successive cation and anion insertion/binding. As a result, a distinctive, essentially Nernstian electrochemical response is obtained for phenethylammonium ions of methamphetamine (METH), p-methoxyamphetamine (PMA), amphetamine (AMPH),…
Entrectinib: a potent new TRK, ROS1, and ALK inhibitor
2015
Abstract: Introduction: Receptor tyrosine kinases (RTKs) and their signaling pathways, control normal cellular processes; however, their deregulation play important roles in malignant transformation. In advanced non-small cell lung cancer (NSCLC), the recognition of oncogenic activation of specific RTKs, has led to the development of molecularly targeted agents that only benefit roughly 20% of patients. Entrectinib is a pan-TRK, ROS1 and ALK inhibitor that has shown potent anti-neoplastic activity and tolerability in various neoplastic conditions, particularly NSCLC. Areas covered: This review outlines the pharmacokinetics, pharmacodynamics, mechanism of action, safety, tolerability, pre-cl…
CCDC 644638: Experimental Crystal Structure Determination
2009
Related Article: D.Raffa, B.Maggio, S.Cascioferro, M.V.Raimondi, D.Schillaci, G.Gallo, G.Daidone, S.Plescia, F.Meneghetti, G.Bombieri, A.Di Cristina, R.M.Pipitone, S.Grimaudo, M.Tolomeo|2009|Eur.J.Med.Chem.|44|165|doi:10.1016/j.ejmech.2008.03.023
CCDC 1942014: Experimental Crystal Structure Determination
2020
Related Article: Antonio A. Garcı́a-Valdivia, Manuel Pérez-Mendoza, Duane Choquesillo-Lazarte, Javier Cepeda, Belén Fernández, Manuel Souto, Marcos González-Tejero, Jose A. Garcı́a, Guillermo Mı́nguez Espallargas, Antonio Rodrı́guez-Diéguez|2020|Cryst.Growth Des.|20|4550|doi:10.1021/acs.cgd.0c00345
CCDC 1942013: Experimental Crystal Structure Determination
2020
Related Article: Antonio A. Garcı́a-Valdivia, Manuel Pérez-Mendoza, Duane Choquesillo-Lazarte, Javier Cepeda, Belén Fernández, Manuel Souto, Marcos González-Tejero, Jose A. Garcı́a, Guillermo Mı́nguez Espallargas, Antonio Rodrı́guez-Diéguez|2020|Cryst.Growth Des.|20|4550|doi:10.1021/acs.cgd.0c00345
Interpenetrated Luminescent Metal-Organic Frameworks based on 1H-Indazole-5-carboxylic Acid
2020
Herein we report the formation and characterization of two novel Zn-based multifunctional metal-organic frameworks (MOFs) based on 1H-indazole-5-carboxylic acid and bipyridine-like linkers, synthesized by soft solvothermal routes. These materials possess isoreticular 2-fold interpenetrated three-dimensional structures that afford a flexible character and allow porosity modulation of the MOFs as confirmed by CO2 sorption measurements. Apart from this attractive structural feature, the MOFs exhibit fascinating luminescent properties involving both luminescence thermometry and long-lasting phosphorescence.
Heterocyclic rearrangements.N,N-diphenylhydrazones, oximes andO-methyloximes of 3-benzoyl-5-phenyl-1,2,4-oxadiazole
1985
The behaviour of (E)- and (Z)-N,N-diphenylhydrazones and O-Methyloximes of 3-benzoyl-5-phenyl-1,2,4-oxadiazole has been studied. When refluxed in benzene, or in dioxane-water (1:1), the (Z)-N,N-diphenylhydrazone 8Z gave the indazole 11 or the substituted semicarbazide 12, respectively. The O-methyloxime 14Z did not give any rearrangement. A criticism of the oximation reaction of 3-benzoyl-5-phenyl-1,2,4-oxadiazole is also reported.