Search results for "3’"
showing 10 items of 11 documents
Pyrido[2’,3’:4,5]pyrrolo[2,1-d][1,2,3,5]tetrazine-4(3H)-ones, a new class of temozolomide heteroanalogues
2009
Twelve derivatives of new ring system pyrido[2’,3’:4,5]pyrrolo[2,1-d][1,2,3,5]tetrazine were prepared in good yields by reaction of 2-diazo-3-ethoxycarbonyl-pyrrolo[3,2-b]pyridine with alkyl- or aryl-isocyanates. Nine derivatives, screened by the National Cancer Institute (Bethesda, MD) for the in vitro one dose primary anticancer assay against a panel of about 60 human tumor cell lines, showed no significant activity.
An improvement of ComiR algorithm for microRNA target prediction by exploiting coding region sequences of mRNAs
2020
AbstractMicroRNA are small non-coding RNAs that post-transcriptionally regulate the expression levels of messenger RNAs. MicroRNA regulation activity depends on the recognition of binding sites located on mRNA molecules. ComiR is a web tool realized to predict the targets of a set of microRNAs, starting from their expression profile. ComiR was trained with the information regarding binding sites in the 3’utr region, by using a reliable dataset containing the targets of endogenously expressed microRNA in D. melanogaster S2 cells. This dataset was obtained by comparing the results from two different experimental approaches, i.e., inhibition, and immunoprecipitation of the AGO1 protein--a comp…
Nuovi inibitori di Aurora chinasi A come target biologico coinvolto nei processi carcinogenici
2011
Identificando Aurora chinasi A come target elettivo per l’inibizione dell’espansione tumorale è stato sfruttato l’approccio computazionale per effettuare un virtual screening su una libreria “in house” di strutture molecolari. L’analisi dei dati computazionali ha permesso di identificare nei derivati della serie pirido[3’,2’:4,5]furo[3,2-d]-1,2,3-triazin-4(3H)one di tipo 3 nuovi composti a potenziale attività inibitoria sul sito ATP-asico di Aurora chinasi A. La sintesi del sistema triciclico-eteroaromatico 3 prevede la diazotazione della 3-amino-furopiridina 1 e conseguente reazione di copulazione con una serie di ammine primarie opportunamente scelte, permettendo l’isolamento delle 3-tria…
Peroksīdu noteikšana ar eksprestestu metodi
2017
Peroksīdu noteikšana ar eksprestestu metodi. Bruņeniece A., darba vadītājs Dr. ķīm. docents Ģībietis J. Bakalaura darbs, 44 lappuses, 10 tabulas, 26 attēli, 23 literatūras avoti. Latviešu valodā. Darbā apskatītas dažādas ūdeņraža peroksīda un peroksietiķskābes kvantitatīvās noteikšanas metodes. Veikta ITS firmas ekprestesta „Water-Works” teststrēmeļu kalibrēšana. Eksperimentāli izpētīta jonu spēka, pH un organiskā šķīdinātāja ietekme uz teststrēmeļu darbību. Iegūti kalibrēšanas grafiki un izveidotas krāsu standartskalas, izmantojot spektrofotometru – kolorimetru AvaMouse Avantes, kā arī izpētītа teststrēmeļu piеmērotība peroksīdu koncentrācijаs noteikšanаi atšķirīgās vidēs. Iegūtie rezultāt…
Synthesis and antiproliferative activity of new derivatives containing the polycyclic system 5,7:7,13-dimethanopyrazolo[3,4-b]pyrazolo[3’,4’:2,3]azep…
2013
The reaction under reflux between 1-phenyl-3-R-5-methylaminopyrazoles and 2,5-hexanedione lead to 5,7:7,13-dimethanopyrazolo[3,4-b]pyrazolo[3′,4′:2,3]azepino[4,5-f]azocine derivatives 3b–g. These unusual molecules show the structural complexity of many biologically active natural products and are endowed with the chemical diversity that is required in drug discovery. The compounds 3b,e were reduced by hydrogen in the presence of Palladium on activated charcoal to give the dihydro derivatives 5b,e. Compounds 3b–f and 5b,e were selected by the NCI to evaluate their in vitro antiproliferative activity against 60 human cell lines derived from nine clinically isolated cancer types (leukaemia, lu…
The Reactivity of 4’-Substituted Spiro[Isoindole-1,3’-pyrazoles] Derivatives: Substitution/Elimination Reactions and Access to Biaryl Derivatives
2017
This paper describes aspects of the chemistry of 4’-substituted spiro [indole-1,3’-pyrazoles]. These compounds underwent substitution and/or elimination reactions to afford some new spiro- as well as biaryl derivatives of potential pharmaceutical relevance. Mechanistic considerations are discussed as well.
Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives
2012
Abstract A series of isochromeno[4,3-c]pyrazole-5(1H)-one derivatives 7b–h were prepared and tested at 10 μM for their ability to displace specific [3H]flunitrazepam from bovine brain membranes. The substitution pattern of the above derivatives was shown to influence the receptor affinity. The most active compound of the series was 7e, showing a 54% inhibition of [3H]flunitrazepam binding. Compounds 7a–d,i were compared with the known isomers chromeno[4,3-c]pyrazole-4(1H)-ones 14a–d,i, showing that the isochromene/chromene isomerism influences the activity.
Etude du rôle du récepteur nucléaire CAR, Constitutive Androstane Receptor, dans le métabolisme des lipides et la susceptibilité à l'athérosclérose
2011
The Constitutive Androstane Receptor (CAR) belongs to the subfamily of nuclear receptors NR1. Initially described as an orphan receptor, CAR is activated by a large number of exogenous molecules and acts as a xenosensor. The activation of CAR by these ligands stimulates transcription of phase I, II and III enzymes required for the detoxification and elimination of xenobiotics. Furthermore CAR is also involved in the metabolism of endogenous molecules such as bile acids, bilirubin or thyroid hormones. CAR has recently been the subject of numerous independent studies that have highlighted his involvement in major metabolic pathways including gluconeogenesis, lipogenesis and lipoprotein metabo…
A ceRNA analysis on LMNA gene focusing on the Hutchinson-Gilford progeria syndrome
2013
Background: Hutchinson-Gilford progeria syndrome is a rare dominant human disease of genetic origin. The average life expectancy is about 20 years, patients’ life quality is still very poor and no efficient therapy has yet been developed. It is caused by mutation of the LMNA gene, which results in accumulation in the nuclear membrane of a particular splicing form of Lamin-A called progerin. The mechanism by which progerin perturbs cellular homeostasis and leads to the symptoms is still under debate. Micro-RNAs are able to negatively regulate transcription by coupling with the 3’ UnTranslated Region of messenger RNAs. Several Micro-RNAs recognize the same 3’ UnTranslated Region and each Micr…
Complessi di Platinum(II): sintesi, studi di DNA-binding e loro attività antitumorale in vitro
2013
Con lo scopo di trovare nuovi analoghi del Cis-DDP (cis-diammino dicloro platino(II)) nuovi complessi del platino sono stati sintetizzati, caratterizzati e ne è stata studiata l’attività antitumorale in vitro [1]. Recentemente sono stati preparati complessi con metalli del quarto periodo di transizione con entrambi i leganti, dipirido[3,2-a:2’,3’-c]fenazina (dppz) e glicinato (gly) [2]. I composti di nuova sintesi vengono generalmente caratterizzati attraverso parecchie tecniche analitiche incluso la cristallografia a raggi-X e la loro attività antitumorale viene testata su un vasto pannello di linee cellulari umane [1,2]. Le proprietà biologiche spesso sono correlate alla loro interazione …