Search results for "PYRAZOL"

Effects of cyclooxygenase-1/cyclooxygenase-2 inhibition on leukocyte/endothelial cell interactions in the rat mesentery.

2002

Nonsteroidal anti-inflammatory drugs (NSAID) inhibit cyclooxygenase activity and cause gastrointestinal damage in part by promoting leukocyte accumulation in the mucosa. Our aim was to evaluate the effects of selective blockade of the isoenzymes cyclooxygenase-1 and cyclooxygenase-2 on leukocyte adhesion in vivo. Leukocyte/endothelial cell interactions were examined in rat mesenteric venules before and after treatment with indomethacin, SC-560 (5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-trifluoromethylpyrazole, cyclooxygenase-1 inhibitor), DFP (5,5-dimethyl-3-(2-propoxy)-4-(4-methanesulfonyl)-2(5H)-furanone, cyclooxygenase-2 inhibitor), or SC-560 plus DFP (20 mg/kg, i.v. each). Indomethacin i…

s-Block metal scorpionates – A new sodium hydrido-tris(3,5-dimethyl-1-pyrazolyl)borate salt showing an unusual core stabilized by bridging and termin…

2020

Abstract Dissolution of [(μ-Me2CO)3(NaTp*)2] (1) (Tp* = hydrido-tris(3,5-dimethyl-1-pyrazolyl)borate) in DMSO at room temperature leads to the growth of colourless crystals characterized as the new salt [Na2Tp*(μ-Me2SO)3(Me2SO)3] [NaTp* 2] (2). 2 crystallized in the trigonal space group R3 with Z = 3, a = 14.1227(2) Å, b = 14.1227(10) Å, c = 33.9685(2) Å, and V = 5867.35(17) Å3. Interestingly, anion and cation of 2 both contain the Tp* ligand. Moreover, the cationic moiety highlights an unusual sodium atom hexacoordinated by six DMSO molecules acting as O-bonded ligands. Three of which exhibit a bridging coordination mode and three are in terminal position. To the best of our knowledge, the…

Exploring the anticancer potential of pyrazolo[1,2-a]benzo[1,2,3,4] tetrazin-3-one derivatives: The effect on apoptosis induction, cell cycle and pro…

2013

In order to investigate their anticancer potential, four new pyrazolo[1,2-a]benzo[1,2,3,4]-tetrazinone derivatives, designed through the chemometric protocol VLAK, and three of the most active compounds of the previous series have been evaluated on some cellular events including proliferation, apoptosis induction, and cell cycle. The NCI one dose (10 mu M) screening revealed that the 8,9-di-methyl derivative showed activity against Leukemia (CCRF-CEM) and Colon cancer cell line (COLO 205), reaching 81% and 45% of growth inhibition (GI), respectively. Replacement of the two methyl groups with two chlorine atoms maintained the activity toward Leukemia cell (CCRF-CEM, GI 77%) and selectively e…

CCDC 1917754: Experimental Crystal Structure Determination

2019

Related Article: Víctor García-López, Mario Palacios-Corella, Verónica Gironés-Pérez, Carlos Bartual-Murgui, José Antonio Real, Eric Pellegrin, Javier Herrero-Martín, Guillem Aromí, Miguel Clemente-León, Eugenio Coronado|2019|Inorg.Chem.|58|12199|doi:10.1021/acs.inorgchem.9b01526

CCDC 1577623: Experimental Crystal Structure Determination

2018

Related Article: M. Luisa Calatayud, Marta Orts-Arroyo, Miguel Julve, Francesc Lloret, Nadia Marino, Giovanni De Munno, Rafael Ruiz-García, Isabel Castro|2018|J.Coord.Chem.|71|657|doi:10.1080/00958972.2017.1421950

CCDC 233990: Experimental Crystal Structure Determination

2005

Related Article: C.Pettinari, F.Marchetti, R.Pettinari, A.Cingolani, E.Rivarola, C.Phillips, J.Tanski, M.Rossi, F.Caruso|2004|Eur.J.Inorg.Chem.||3484|doi:10.1002/ejic.200400225

SYNTHESIS AND SAR STUDIES OF NEW 3-METHYL-5-(5-PROPYL-1H-1-R'-3-PYRAZOLYL)-1H-1-R-4-NITROSOPYRAZOLES AS ANTIMICOTIC AGENTS.

2013

Synthesis and antiproliferative activity of Naphtalenyl substituted 1,2-dihydropyrazol-5-one and related fused tetrazine

2011

In recent years, besides the main field of nonsteroidal anti-inflammatory agents, the interest towards pyrazolone derivatives has been renewed because of their wide biological and pharmacological applications [1]. Currently, particular attention is focused on such a class of compounds due to the affinity with sigma receptor and their relationship with cancer [2].To these purposes we planned to design, synthesize and evaluate the antiproliferative activity (MTS assays) of a new series of 3-methyl-2-(1-R-naphthalen-2-yl)-1,2-dihydropyrazol-3-one derivatives 1 against HeLa, MCF-7, LAN-5, Caco2 in order to explore their anticancer potential. Additionally, further elaboration of the amino deriva…

1,2-Dihydropyrazole[1,2-a]benzo[1,2,4]triazine-3-one: deaza analogue tricyclic scaffold with valuable antiproliferative activity

2012

One pot-like regiospecific access to 1-aryl-1H-pyrazol-3(2H)-one derivatives and evaluation of the anticancer activity

2022

A set of variously substituted 1-arylpyrazol-3-one derivatives, including the di-ortho-aryl substituted ones, was synthesized as new potential anticancer compounds. To fulfill this aim, herein a regiospecific synthesis was proposed utilizing a new revisited one pot procedure, starting from commercial anilines and easily accessible 2,5-dimethyl-furan-3-one. In the course of the sequential ordered steps, in some cases, a nitro group displacement by chlorine took place to a minor extent. The in vitro screening against the full panel of ~60 human cancer cell lines (NCI) showed a moderate, but promising selective antiproliferative activity against the UO31 renal tumor cell line, only in compound…