scholarly journals Induction of arginosuccinate synthetase (ASS) expression affects the antiproliferative activity of arginine deiminase (ADI) in melanoma cells

Author(s):  
Giuseppe Palmieri
Synthesis ◽  
2020 ◽  
Author(s):  
Ghenia Bentabed-Ababsa ◽  
Laurent Picot ◽  
Florence Mongin ◽  
Salima Bouarfa ◽  
William Erb ◽  
...  

Abstract N-Arylation of various 2-acylated anilines with different electron-rich heteroaryl iodides (2- and 3-iodothiophenes, 2- and 3-iodobenzothiophenes­, 2-iodobenzofuran) was achieved by using activated copper and potassium carbonate in dibutyl ether at reflux. The reactivity of the different heteroaryl iodides and anilines employed was discussed and rationalized on the basis of their electronic features. Subsequent cyclization by aromatic electrophilic substitution easily took place in the case of C2-free (benzo)thienyl or C3-free (benzo)furyl derivatives­, affording original tri- and tetracycles. The antiproliferative activity of most of them was evaluated in A2058 melanoma cells and revealed four chlorinated tetracycles as effective growth inhibitors.


2017 ◽  
Vol 125 ◽  
pp. 1225-1234 ◽  
Author(s):  
Virginie Bellet ◽  
Laure Lichon ◽  
Dominique P. Arama ◽  
Audrey Gallud ◽  
Vincent Lisowski ◽  
...  

2020 ◽  
Vol 13 (4) ◽  
pp. 68
Author(s):  
Anna Baldisserotto ◽  
Monica Demurtas ◽  
Ilaria Lampronti ◽  
Massimo Tacchini ◽  
Davide Moi ◽  
...  

In the search of multifunctional compounds we designed benzimidazole derivatives endowed with phenolic hydroxy groups and a hydrazone moiety as potential radical-scavenger and the antioxidant agents. The target molecules have been prepared by a simple synthetic procedure and tested for their antioxidant activity by DPPH, FRAP, and ORAC test, for photoprotective activity against UV rays and for antiproliferative activity against Colo-38 melanoma cells. Furthermore, two different dermocosmetic formulations were prepared with the compounds endowed with the best antioxidant and photoprotective profile and their release from formulation evaluated using Franz Cells system. High antioxidant activity is related to the presence of at least two hydroxy groups on arylidene moiety of benzimidazoles. Structure activity analysis revealed that the position of hydroxy groups is crucial for antioxidant activity as well as the presence of a 2-hydroxy-4-(diethylamino)arylidene group. The same correlation pattern was found to be related to photoprotective activity resulting in an UVA Protection Factor better than the commercial solar filter PBSA and antiproliferative activity against melanoma cells without producing cytotoxicity on normal keratinocytes. The release analysis indicated that high antioxidant activities are achieved with limited release at concentration compatible with the use as UV sunscreen filter.


2006 ◽  
Vol 2 (2) ◽  
pp. 123-132
Author(s):  
D. Fairlie ◽  
P. Parsons ◽  
A. Lucke ◽  
G. Boyle

Phytomedicine ◽  
2008 ◽  
Vol 15 (6-7) ◽  
pp. 528-532 ◽  
Author(s):  
C.R. Vieira ◽  
M.F. Marques ◽  
P.R. Soares ◽  
L. Matuda ◽  
C.M.A. de Oliveira ◽  
...  

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2961 ◽  
Author(s):  
Frédéric Lassagne ◽  
Timothy Langlais ◽  
Elsa Caytan ◽  
Emmanuelle Limanton ◽  
Ludovic Paquin ◽  
...  

2,3-Diphenylated quinoxaline, pyrido[2,3-b]pyrazine and 8-bromopyrido[3,4-b]pyrazine were halogenated in deprotometalation-trapping reactions using mixed 2,2,6,6-tetramethyl piperidino-based lithium-zinc combinations in tetrahydrofuran. The 2,3-diphenylated 5-iodo- quinoxaline, 8-iodopyrido[2,3-b]pyrazine and 8-bromo-7-iodopyrido[3,4-b]pyrazine thus obtained were subjected to palladium-catalyzed couplings with arylboronic acids or anilines, and possible subsequent cyclizations to afford the corresponding pyrazino[2,3-a]carbazole, pyrazino[2′,3′:5,6] pyrido[4,3-b]indole and pyrazino[2′,3′:4,5]pyrido[2,3-d]indole, respectively. 8-Iodopyrido[2,3-b] pyrazine was subjected either to a copper-catalyzed C-N bond formation with azoles, or to direct substitution to introduce alkylamino, benzylamino, hydrazine and aryloxy groups at the 8 position. The 8-hydrazino product was converted into aryl hydrazones. Most of the compounds were evaluated for their biological properties (antiproliferative activity in A2058 melanoma cells and disease-relevant kinase inhibition).


2014 ◽  
Vol 22 (13) ◽  
pp. 3498-3507 ◽  
Author(s):  
Madani Hedidi ◽  
Ghenia Bentabed-Ababsa ◽  
Aïcha Derdour ◽  
Thierry Roisnel ◽  
Vincent Dorcet ◽  
...  

2013 ◽  
Vol 12 (11) ◽  
pp. 2581-2590 ◽  
Author(s):  
Yan Long ◽  
Wen-Bin Tsai ◽  
Medhi Wangpaichitr ◽  
Takashi Tsukamoto ◽  
Niramol Savaraj ◽  
...  

2016 ◽  
Vol 83 ◽  
pp. 492-499 ◽  
Author(s):  
Alessandra Russo ◽  
Carmen Formisano ◽  
Daniela Rigano ◽  
Venera Cardile ◽  
Nelly Apostolides Arnold ◽  
...  

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