75152-19-1Relevant articles and documents
Synthesis, cytotoxicity, and docking study of novel 1-naphthyl-5-aryl-1H-1,2,4-triazole-3-carboxamides
Zaki, Islam,Ramadan, Mohamed,Abdelrahman, Mostafa H.,Aly, Omar M.
, p. 1483 - 1496 (2017/07/18)
A new series of 1-naphthyl-5-aryl-1H-1,2,4-triazole-3-carboxamide derivatives were synthesized and structurally proved by 1H and 13C NMR along with high-resolution mass spectrometry. The cytotoxic activity of the newly synthesized compounds was evaluated. Compounds showed a pronounced inhibitory effect against cellular localization of tubulin. Flow cytometric analysis showed that Hep-G2 cells treated indicated a predominated growth arrest at the G2/M-phase compared to that of S-phase. Molecular modeling study using MOE program indicated that most of the target compounds showed good binding with the colchicine-binding site of β-subunit of tubulin with the binding free energy (?G) values of about 42?kJ/mol. Graphical abstract: [Figure not available: see fulltext.].
Synthesis of di- and tri-substituted imidazole-4-carboxylates via PBu3-mediated [3+2] cycloaddition
Hsu, Mei-Yuan,Dietrich, Justin,Hulme, Christopher,Shaw, Arthur Y.
, p. 1538 - 1542 (2013/05/21)
Some new di- and trisubstituted imidazole-4-carboxylates were prepared from amidoacetic acids 3 in the present report. The key step to establish such imidazole- 4-carboxylates stemmed from the PBu3-mediated [3+2] cycloaddition between in situ-generated Δ2-oxazolinone 4 and ethyl cyanoformate6. Our results indicated that trisubstituted imidazoles 7-20 were afforded in better yields than those of disubstituted imidazoles 21-27. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications1 to view the free supplemental file. Copyright Taylor & Francis Group, LLC.
A kinetic study of the base-catalyzed dimerization of 5(4H)-oxazolones
Mazurkiewicz,Pierwocha,Fryczkowska
, p. 113 - 121 (2007/10/03)
The effects of the substituent at position-2 and kind of the base on the rate of the base-catalyzed dimerization of 5(4H)-oxazolones have been investigated. The electrondonating and strong steric effect of the substituent at position-2 reduce markedly the proclivity of 5(4H)-oxazolones to dimerization. The following catalytic activity sequence of the bases has been found: DBU >> Et3N > (i-Pr)2EtN.