Search results for "IPR"
showing 10 items of 1515 documents
Synthesis and antiproliferative activity of triazenoindazoles and triazenopyrazoles: a comparative study.
2003
Several triazenoindazoles and triazenopyrazoles were prepared transforming the appropriate aminoindazoles and aminopyrazoles in the corresponding diazonium salts which were reacted with dimethylamine, diethylamine and pyrrolidine. All the triazenes were tested for their antiproliferative activity against K562, HL60, L1210 and MCF7 cell lines. The biological data showed that the benzocondensation plays a positive role on the antiproliferative activity. The (1)H-NMR spectra showed that the rotational barrier around the N(2)-N(3) bond in the triazene group can be influenced both by the position of this group in the indazole nucleus and by the substitution pattern in the benzene moiety.
Synthesis of substituted 3-amino-N-phenyl-1H-indazole-1-carboxamides endowed with antiproliferative activity
2010
Abstract Several new N-phenyl-1H-indazole-1-carboxamides 1c–h and 4l,m were prepared by reacting phenyl isocyanate derivatives 3a,b with 3-amino-1H-indazole derivatives 2c,e,g or 1H-indazole 2l respectively. Chemical transformations of compounds 1a,b and 1g,h gave 3-acetamido-N-phenyl-1H-indazole-1-carboxamide derivatives 5a,b, and 3,5-diamino-N-phenyl-1H-indazole-1-carboxamide derivatives 4i, j respectively. Finally, 3,5-diacetamido-N-phenyl-1H-indazole-1-carboxamide derivatives 6a,b were prepared by acetylation of 4i, j. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell lines panel derived from nine clinically isolat…
Isoindolo[2,1-c]benzo[1,2,4]triazines: a new ring system with antiproliferative activity.
2006
Abstract A series of isoindolo-benzo-triazines of type 4 was obtained by diazotization of 2-(2-aminoaryl)-1-cyanoisoindoles 3a – j . All the synthesized derivatives were screened by the National Cancer Institute (NCI, Bethesda, USA), for in vitro antitumor activity against a 3-human cancer cell line panel consisting of MCF7 (breast), NCI-H460 (lung), and SF-268 (CNS). Derivatives 4a , f , i , j were selected to be evaluated in the full panel of about 50 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity generally in the micromolar range. The most sensitive cell lines were: MOLT-4 and SR of the leukemia subpanel, A549/ATCC and EKVX of the n…
3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin Analogues with antiproliferative activity
2015
A new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (~60) having GI50 values ranging from low micromolar to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and mitochondrial dysfunctio…
THIOPYRANO[2,3-E]INDOL-2-ONES: ANGELICIN HETEROANALOGUES WITH POTENT PHOTOANTIPROLIFERATIVE ACTIVITY
2008
A new class of compounds, the thiopyrano[2,3-e]indol-2-ones, bioisosters of the angular furocoumarin angelicin, was synthesized with the aim of obtaining new photochemotherapeutic agents. In particular 7,8-dimethyl-thiopyranoindolone 6c s showed a remarkable phototoxicity and a great dose UVA dependence reaching IC(50) values at submicromolar level. This latter photoinduced a massive apoptosis and a remarkable photodamage to lipids and proteins. Although it did not intercalate DNA, it was able to cause photooxidation of DNA bases.
A New Oxadiazole-Based Topsentin Derivative Modulates Cyclin-Dependent Kinase 1 Expression and Exerts Cytotoxic Effects on Pancreatic Cancer Cells
2021
Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal form of cancer characterized by drug resistance, urging new therapeutic strategies. In recent years, protein kinases have emerged as promising pharmacological targets for the treatment of several solid and hematological tumors. Interestingly, cyclin-dependent kinase 1 (CDK1) is overexpressed in PDAC tissues and has been correlated to the aggressive nature of these tumors because of its key role in cell cycle progression and resistance to the induction of apoptosis. For these reasons, CDK1 is one of the main causes of chemoresistance, representing a promising pharmacological target. In this study, we report the synthesis of new 1,2,4…
Troponina e infarto periprocedurale: filo di Arianna o folle volo di Icaro?
2013
Percutaneous coronary interventions cause frequently an increase in myocardial necrosis markers. Is troponin elevation after percutaneous coronary intervention a predictor of events at follow-up or a consequence of the procedure with no cause-effect relationship with prognosis? The debate is still open
Heterocyclic Diamines with Leishmanicidal Activity.
2021
Leishmaniasis is one of the world's most neglected diseases with a worldwide prevalence of 12 million people. There are no effective human vaccines for its prevention, and outdated drugs hamper treatment. Therefore, research aimed at developing new therapeutic tools to fight leishmaniasis remains a crucial goal today. With this purpose in mind, here, we present 10 new compounds made up by linking alkylated ethylenediamine units to pyridine or quinoline heterocycles with promising in vitro and in vivo efficacy against promastigote and amastigote forms of Leishmania infantum, Leishmania donovani, and Leishmania braziliensis species. Three compounds (2, 4, and 5) showed a selectivity index muc…
Periprotēžu infekcijas ārstēšanas efektivitāte pielietojot DAIR metodi TOS slimnīcā no 2015.-2019.gadam
2021
Ik gadu Traumatoloģijas un ortopēdijas slimnīcā, kā arī visā Latvijā veic simtiem gūžas locītavu endoprotezēšanu, taču ne visas ir veiksmīgas. Pastāv dažādas pēc operācijas komplikācijas, kas var parādīties pat vairākus gadus pēc primārās endoprotezēšanas operācijas. Kā viena no biežākajām un smagākajām ir periprotēzes infekcija. Akūtas periprotēžu infekcijas dažādos tās stāvokļos ir sastopamas regulāri ik gadu. Kā viena no ārstēšanas iespejām ir DAIR metode, kas savā abreviatūrā izskaidro tās būtību: iekaisušo audu eradikācija, antibakteriālā terapija un endoprotēzes kustīgo elementu nomaiņa. Iekaisušo audu eradikācija norit operatīvi, atkārtoti atverot gūžas locītavu. Antibakteriālā terap…
Influència de Kohlberg en el programa de compromís social del centre penitenciari d' "El Dueso"
2018
espanolTras anos de innovacion i puesta en practica de diferentes formas de intervencion en el mundo penitenciario, en el Centro Penitenciario de El Dueso se aplica el programa de Compromiso Social. La Teoria del Desarrollo Moral de Kohlberg esta sirviendo de apoyo para potenciar la prosocialidad asi como el desarrollo moral de los internos a traves de aquellas actividades en las que se convierten en protagonistas de la ayuda a terceras personas, promoviendo su propio cambio personal i generando un proceso de reciprocidad con el exterior de la prision. Se defienden las actividades de tipo prosocial como excelente herramienta de trabajo en las prisiones. catalaDespres d’anys d’innovacio i de…