7699-83-4Relevant academic research and scientific papers
Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors
Shaldam, Moataz,Eldehna, Wagdy M.,Nocentini, Alessio,Elsayed, Zainab M.,Ibrahim, Tamer M.,Salem, Rofaida,El-Domany, Ramadan A.,Capasso, Clemente,Abdel-Aziz, Hatem A.,Supuran, Claudiu T.
, (2021/03/04)
In the present study, we describe the design of different series of benzofuran-based derivatives as potential carbonic anhydrase inhibitors (CAIs). The adopted design is based on bioisosteric replacement for the p-fluorophenyl SLC-0111 tail with the lipop
Benzofuran-Based Carboxylic Acids as Carbonic Anhydrase Inhibitors and Antiproliferative Agents against Breast Cancer
Abdel-Aziz, Hatem A.,Al-Sanea, Mohammad M.,Al-Warhi, Tarfah,Aljaeed, Nada,Alotaibi, Ohoud J.,Eldehna, Wagdy M.,Elsayed, Zainab M.,Nocentini, Alessio,Supuran, Claudiu T.
, p. 1022 - 1027 (2020/06/27)
Pursuing our effort for developing effective inhibitors of the cancer-related hCA IX isoform, here we describe the synthesis of novel benzofuran-based carboxylic acid derivatives, featuring the benzoic (9a-f) or hippuric (11a,b) acid moieties linked to 2-
New One-Pot Synthesis of Polysubstituted Benzofurans and Benzo-1,4-dioxines
Sakhabutdinova,Raskil’dina,Zlotskii,Sultanova
, p. 233 - 236 (2018/11/21)
It has been revealed that the copper(II) triflate catalyzed reaction of ethyl-2-diazo-3-oxobutanoate with phenols followed by cyclization of the intermediate enol in the presence of polyphosphoric acid is a simple and efficient method of synthesis of polysubstituted benzofurans. The use of pyrocatechol leads to the corresponding substituted 1,4-benzodioxine-2-carboxylates as major products.
Original 2-(3-alkoxy-1 H -pyrazol-1-yl)pyrimidine derivatives as inhibitors of human dihydroorotate dehydrogenase (DHODH)
Munier-Lehmann, Hélène,Lucas-Hourani, Marianne,Guillou, Sandrine,Helynck, Olivier,Zanghi, Gigliola,Noel, Anne,Tangy, Frédéric,Vidalain, Pierre-Olivier,Janin, Yves L.
, p. 860 - 877 (2015/01/30)
From a research program aimed at the design of new chemical entities followed by extensive screening on various models of infectious diseases, an original series of 2-(3-alkoxy-1H-pyrazol-1-yl)pyrimidines endowed with notable antiviral properties were found. Using a whole cell measles virus replication assay, we describe here some aspects of the iterative process that, from 2-(4-benzyl-3-ethoxy-5-methyl-1H-pyrazol-1-yl)pyrimidine, led to 2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine and a 4000-fold improvement of antiviral activity with a subnanomolar level of inhibition. Moreover, recent precedents in the literature describing antiviral derivatives acting at the level of the de novo pyrimidine biosynthetic pathway led us to determine that the mode of action of this series is based on the inhibition of the cellular dihydroorotate dehydrogenase (DHODH), the fourth enzyme of this pathway. Biochemical studies with recombinant human DHODH led us to measure IC50 as low as 13 nM for the best example of this original series when using 2,3-dimethoxy-5-methyl-6-(3-methyl-2-butenyl)-1,4-benzoquinone (coenzyme Q1) as a surrogate for coenzyme Q10, the cofactor of this enzyme.
PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS
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Paragraph 0086; 0088, (2014/03/21)
This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.
PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS
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Page/Page column 17-18, (2012/10/18)
This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.
A novel route to 4-oxy/thio substituted-1H-pyrazol-5(4H)-ones via efficient cross-Claisen condensation
Ragavan, R. Venkat,Vijayakumar
experimental part, p. 323 - 330 (2011/06/19)
α-Oxy/thio substituted β-keto esters were synthesized through an efficient cross-Claisen condensation of oxy/thio substituted acetic acid ethyl esters with acid chlorides, which in turn converted in situ into 4-oxy/thio substituted-1H-pyrazol-5(4H)-ones by the addition of hydrazine and its derivatives. This method has been found to be extremely fast, general, and useful toward the synthesis of inaccessible pyrazolones and synthetically demanding 4-oxy/thio substituted pyrazolones.
Ion exchange resin catalyzed synthesis of substituted-4-methyl-3-(substituted phenoxy)coumarins
Rathnam,Thatte, Chittaranjan S.,Pise, Abhinay C.
body text, p. 6092 - 6098 (2010/12/19)
Various substituted 2//-1-benzopyran-2-one-4-methyl-3-(substi-tuted phenoxy)compounds have been successfully synthesized by the reaction of ethyl-2-(substituted phenoxy)-3-oxobutanoates (Ia-Id) with re-sorcinol, 4-chloro resorcinol and α-naphthol using io
