64220-26-4Relevant academic research and scientific papers
Synthesis and biological evaluation of 4β-(thiazol-2-yl)amino-4′-O-demethyl-4-deoxypodophyllotoxins as topoisomerase-II inhibitors
Sang, Chun-Yan,Tian, Heng-Zhi,Chen, Yue,Liu, Jian-Fei,Chen, Shi-Wu,Hui, Ling
, p. 71 - 76 (2017/12/28)
A series of 4β-(thiazol-2-yl)amino-4′-O-demethyl-4-deoxypodophyllotoxins were synthesized, and their cytotoxicities were evaluated against four human cancer cell lines (A549, HepG2, HeLa, and LOVO cells) and normal human diploid fibroblast line WI-38. Som
Thiazole- and imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase
Bolchi, Cristiano,Pallavicini, Marco,Bernini, Sergio K.,Chiodini, Giuseppe,Corsini, Alberto,Ferri, Nicola,Fumagalli, Laura,Straniero, Valentina,Valoti, Ermanno
, p. 5408 - 5412 (2011/10/12)
Mimetics of the C-terminal CAAX tetrapeptide of Ras protein were designed replacing internal dipeptide AA with 4-amino-2-phenylbenzoic acid and cysteine (C) with 2-amino-4-thiazolyl-, 2-mercapto-4-thiazolyl-, 2-mercapto-4-imidazolyl- and 2-methylmercapto-4-thiazolyl-acetic or propionic acid. The compound in which C is replaced by 2-amino-4-thiazolylacetic acid inhibited FTase activity in the low nanomolar range and showed antiproliferative effect on rat aortic smooth muscle cells interfering with Ras farnesylation. On the basis of these results, 2-aminothiazole can be considered as an alternative to heterocycles, such as pyridine and imidazole, normally used in FTase inhibitors designed as non-thiol CAAX mimetics.
3-Carbamoyloxymethyl-7-(amino-4-thiazolyl-acetamido)-cephalosporanic acid derivatives
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, (2008/06/13)
A compound of the formula STR1 wherein R is selected from the group consisting of hydrogen and a group easily removable by acid hydrolysis or hydrogenolysis, R1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms
7-Amino-thiazolyl acetamido cephalosporanic acids
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, (2008/06/13)
Novel 7-amino-thiazolyl-acetamido-cephalosporanic acid compounds of the formula STR1 wherein R is selected from the group consisting of hydrogen and a group easily removable by acid hydrolysis or hydrogenolysis, R1 is selected from the group consisting of alkyl of 1 to 4 carbon atoms, a 5 member heterocyclic ring and a 5 member heterocyclic ring containing a ketone group and A is selected from the group consisting of hydrogen, alkali metal and equivalents of alkaline earth metals, magnesium and organic amine having antibiotic activity against gram negative and gram positive bacteria and their preparation and novel intermediates therefore. STATE OF THE ART French Pat. No. 2,255,077 of Takeda describes antibacterial cephalosporins having a different substitutent in the 3-position.
