Search results for "IPR"

Synthesis, characterization, crystal structures and biological screening of 4-amino quinazoline sulfonamide derivatives

2019

Three quinazolin-4-ylamino derivatives containing phenylbenzenesulfonamides (7a-7c) were synthesized by reacting (E)-N'-(2-cyanophenyl)-N,N-dimethyl formamidine (6) with different 4- amino-N-(phenyl)benzenesulfonamides (4a-4c) and characterized by different techniques such as HRMS, IR, 1H NMR and 13C NMR spectroscopy. The structural properties were further examined by single crystal X-ray diffraction method. The X-ray data shows that compounds 7a and 7c contain two molecules and 7b contains one molecule in the asymmetric unit. Comparison of conformation of two distinct molecules, “A” and “B”, in the asymmetric unit of 7a and 7c were studied with the aid of reported literature. The in vitro …

Synthesis of the New Ring System Bispyrido[4',3':4,5]pyrrolo [1,2-a:1',2'-d]pyrazine and Its Deaza Analogue

2014

Derivatives of the new ring systems bispyrido[4',3':4,5]pyrrolo[1,2-a:1',2'-d] pyrazine-6,13-dione and its deaza analogue pyrido[4'',3'':4',5']pyrrolo-[1',2':4,5]pyrazino [1,2-a]indole-6,13-dione were conveniently synthesized through a four-step sequence. Symmetrical derivatives of the former ring system were obtained through self condensation. On the other hand, condensation of 6-azaindole carboxylic acid with indole 2-carboxylic acid afforded the deaza analogue ring system. Derivatives of the title ring system were tested by the National Cancer Institute (Bethesda, MD, USA) and four of them exhibited modest activity against MCF7 (a breast cancer cell line) and/or UO-31 (a renal cancer cel…

Enzyme-assisted extraction of anthocyanins and other phenolic compounds from blackcurrant (Ribes nigrum L.) press cake: From processing to bioactivit…

2022

The effects of commercial enzymes (pectinases, cellulases, beta-1-3-glucanases, and pectin lyases) on the recovery of anthocyanins and polyphenols from blackcurrant press cake were studied considering two solid:solvent ratios (1:10 and 1:4 w/v). β-glucanase enabled the recovery of the highest total phenolic content – 1142 mg/100 g, and the extraction of anthocyanins was similar using all enzymes (∼400 mg/100 g). The use of cellulases and pectinases enhanced the extraction of antioxidants (DPPH − 1080 mg/100 g; CUPRAC – 3697 mg/100 g). The freeze-dried extracts presented antioxidant potential (CUPRAC, DPPH), which was associated with their biological effects in different systems: antiviral a…

Chamazulene-Rich Artemisia arborescens Essential Oils Affect the Cell Growth of Human Melanoma Cells

2020

Artemisia arborescens is an aromatic shrub whose essential oils are considered a potential source of molecules with industrial and pharmaceutical interest. The chemical profile of A. arborescens essential oils (EOs) was shown to be quite variable and various chemotypes have been identified. In this study, we compared the EOs composition of A. arborescens leaves and flowers collected from four different locations in Sicily. The EOs were assayed for their antiproliferative activity against A375 human malignant melanoma cells, also testing cell viability and cell membrane integrity. The evaluation of DNA fragmentation and caspase-3 activity assay was employed for the detection of apoptosis. Th…

3-(6-Phenylimidazo [2,1-

2019

A new series of imidazo[2,1-b][1,3,4]thiadiazole derivatives was efficiently synthesized and screened for their in vitro antiproliferative activity on a panel of pancreatic ductal adenocarcinoma (PDAC) cells, including SUIT-2, Capan-1 and Panc-1. Compounds 9c and 9l, showed relevant in vitro antiproliferative activity on all three pre-clinical models with half maximal inhibitory concentration (IC50) ranging from 5.11 to 10.8 µM, while the compounds 9e and 9n were active in at least one cell line. In addition, compound 9c significantly inhibited the migration rate of SUIT-2 and Capan-1 cells in the scratch wound-healing assay. In conclusion, our results will support further studies to increa…

Photochemotherapeutic haterocyclic agents having antiproliferative and antineoplastic activity

2011

Phytochemical investigation and antitumor activity of coumarins from Sicilian accession of Ferulago nodosa (L.) Boiss. roots

2023

Ferulago nodosa (L.) Boiss. (Apiaceae) is a species occurring in the Balkan-Tyrrhenian area being present in Crete, Greece, Albania, and probably in Macedonia. From the roots of this accession of species, not previously investigated, four coumarins, grandivittin, aegelinol benzoate, felamidin and aegelinol, and two terpenoids, (2E)-3-methyl-4-[(3-methyl-1-oxo-2-buten-1yl)oxy]-2-butenoic acid and pressafonin-A, were isolated and spectroscopically characterized. The last one was never detected in Ferulago species. The evaluation of the anti-tumor effects of F. nodosa coumarins on colon cancer HCT116 cells showed only a modest effect on reduction of tumor cell viability. For aegelinol, the red…

Antiproliferative activity of Pyrrolo[3,2-c]quinoline derivatives

2012

The pyrrolo[3,2-c]quinoline scaffold has been known as a core structure of a wide number of bioactive molecules. Several derivatives of such a tricyclic angular heterocycle have shown a wide spectrum of biological activities, such as hypotensive, anti-inflammatory properties, gastric (H)ATPase inhibition effect, and remarkable antitumor activity (1). The high therapeutic potentiality of such a skeleton along with our interest in targets featuring aza-polycondensed aromatic structures, attracted us to develop an alternative synthetic strategy, in order to reach a series of pyrrolo[3,2-c]quinolines in quantitative yields (2). The reaction of 3-acetyl-1,4-dione 1 with selected amines allowed th…

1988 06. Documentos del Vº Congreso del PSPV-PSOE. El proyecto de la mayoría. Valencia, 3-5 de junio 1988

2014

1988 06. Documentos del Vº Congreso del PSPV-PSOE. El proyecto de la mayoría. Valencia, 3-5 de junio 1988. Los documentos del 5º congreso del PSPV-PSOE que se recogen son: Informe sobre modificación del artículo 14 de los estatutos del PSPV-PSOE aprobados en el 4º congreso. Propuesta de reducir las 36 comarcas actuales a 21 en las Resoluciones del 5º Congreso. Estatutos. Guía orgánica del PSPV-PSOE, y las resoluciones del congreso. Censo de militantes. Dossier de prensa del congreso.

Appunti sui rapporti tra appello incidentale e mera riproposizione

2018

L’a. affronta il discusso problema dei rapporti tra appello incidentale e mera riproposizione ex art. 346 c.p.c., soffermandosi sulle diverse soluzioni offerte in argomento dalla più recente giurisprudenza di legittimità. In particolare, l’analisi si concentra su Cass., Sez. Un., n. 1179/2017, che tratta prevalentemente del meccanismo di devoluzione in appello sia delle eccezioni respinte sia di quelle assorbite in prime cure, prospettando soluzioni – ad avviso dell’a. – non sempre condivisibili e coerenti.