52188-11-1Relevant articles and documents
Structural investigation on thiazolo[5,4-d]pyrimidines to obtain dual-acting blockers of CD73 and adenosine A2A receptor as potential antitumor agents
Catarzi, Daniela,Colotta, Vittoria,Espindola Gelsleichter, Nicolly,Guilbaud, Audrey,Lopes Rangel Fietto, Juliana,Pasquini, Silvia,Pelletier, Julie,Sévigny, Jean,Sarlandie, Marine,Varani, Katia,Varano, Flavia,Vincenzi, Fabrizio
, (2020)
Adenosine pathway, including its generating enzyme (CD73) and its receptors represents a key target for cancer immunotherapy. Here we aimed to search for novel compounds able to co-target the CD73 and the A2A adenosine receptor (A2A
Design, synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel histone deacetylase inhibitors
Han, Leiqiang,Wang, Lei,Hou, Xuben,Fu, Huansheng,Song, Weiguo,Tang, Weiping,Fang, Hao
, p. 1529 - 1538 (2014/03/21)
Histone deacetylase (HDAC) is a clinically validated target for antitumor therapy. In order to increase HDAC inhibition and efficiency, we developed a novel series of saccharin hydroxamic acids as potent HDAC inhibitors. Among them, compounds 11e, 11m, 11
A facile and green synthesis of novel imide and amidic acid derivatives of phenacetin as potential analgesic and anti-pyretic agents
Reddy, Yervala D.,Kumar, Padam P.,Devi, Bhoomireddy R.,Dubey, Pramod K.,Kumari, Yalamanchili B.
, p. 70 - 76 (2013/07/26)
Facile and green syntheses of potential analgesic and antipyretic compounds, N-(4-ethoxy-phenyl)-2-(1,3- dioxo-1,3-dihydroisoindol-2-yl)acetamide derivatives 6a-g and N-[(4-ethoxy-phenylcarbamoyl)methyl]phthalamic acid derivatives 10a-g have been developed. Two synthetic routes (A and B) have been established for the preparation of 6a-g. In the route-A, 4-ethoxyaniline 2 was reacted with chloroacetyl chloride 3 in a solution of potassium acetate and acetic acid to yield N-(4-ethoxyphenyl)-2-chloroacetamide 4. The latter was reacted with imide compounds 5a-g either in triethanolamine as a green solvent or in solid phase in the presence of TEBAC and KI to yield 6a-g. Alternatively, in the route-B, reaction of anhydrides 7a-g with glycine 8 yielded the (1, 3-dioxo-1, 3-dihydroisoindol-2-yl)acetic acid derivatives 9a-g which on reaction with 2 either in triethnolamine and DCC as a dehydrating agent or in solid phase in the presence of DCC gave 6a-g. The latter were hydrolyzed in 0.5N ethanolic KOH to afford 10a-g.