117971-50-3Relevant academic research and scientific papers
Antiproliferative 1,2,3-thiadiazole compounds
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, (2008/06/13)
Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are 1,2,3-thiadiazoles having the structure: and including stereoisomers, solvates, and pharmaceutically acceptable salts thereof, wherein each of R1, R2, R3 and R4 is independently selected from hydrogen, R5, R6, and R7; R5 is selected from alkyl, heteroalkyl, aryl and heteroaryl; R6 is selected from (R5)n-alkylene, (R5)n-heteroalkylene, (R5)n-arylene and (R5)n-heteroarylene; R7 is selected from (R6)n-alkylene, (R6)n-heteroalkylene, (R6)n-arylene, and (R6)n-heteroarylene; and n is selected from 0, 1, 2, 3, 4 and 5, where R1 and R2 may together form a heterocyclic structure including the nitrogen to which they are both attached, and R3 and R4 may together form a heterocyclic structure including the nitrogen to which they are both attached; and each of L1 and L2 is independently selected from -A1-A2-A3- where each of A1, A2, and A3 is independently selected from a direct bond, alkylene, heteroalkylene, arylene and heteroarylene.
STUDY OF THE CHARACTERISTICS OF REARRANGEMENTS OF 5-AMINO-1,2,3-THIADIAZOLE-4-CARBOTHIOAMIDES
Morzherin, Yu. Yu.,Bakulev, V. A.,Dankova, E. F.,Mokrushin, V. S.
, p. 483 - 488 (2007/10/02)
Using NMR spectroscopy, we have determined the relative stability and the effect of the solvent on the ratio of isomeric N,N-disubstituted 5-amino-1,2,3-thiadiazole-4-carbothioamides in a mixture.We carried out chromatographic separation of a mixture of 5
TWO DIRECTIONS OF CYCLISATION OF α-DIAZO-β-DITHIOAMIDES. NEW REARRANGEMENTS OF 1,2,3-TRIAZOLE-4-CARBOTHIAMIDES.
Bakulev, V. A.,Lebedev, A. T.,Dankova, E. F.,Mokrushin, V. S.,Petrosyan, V. S.
, p. 7329 - 7340 (2007/10/02)
The cyclization processes of 2-diazomalondithioamides, generated by five different methods, have been studied.The ambient character of the derivatives of 2-diazomalondithioamide is the cause of previously unknown rearrangements of 5-mercapto-1,2,3-triazole- and 5-amino-1,2,3-thiadiazole-4-N-R-carbothioamides to 5-N-R-amino-1,2,3-thiadiazole-4-carbothioamides.NMR 1H and 13C spectra and mass-spectra are presented for the series of 5-amino-1,2,3-thiadiazole derivatives.
Reaction of 5-mercapto-1,2,3-triazole-4-carboxamides with phosphorus decasulfide
Dankova,Bakulev,Kolobov,Andosova,Mokrushin
, p. 688 - 690 (2007/10/02)
The reaction of 5-mercapto-1,2,3-triazole-4-carboxamide with P4S10 was studied; the mechanism of this reaction is discussed. The effect of the donor-acceptor properties of the substituents on the direction of cyclization of the intermediate malonic acid α-diazodithioamide was investigated. A new rearrangement in the 5-mercapto-1,2,3-triazole series was observed.
SYNTHESIS AND PROPERTIES OF 5-AMINO-1,2,3-THIADIAZOLE-4-CARBOTHIOAMIDES
Dankova, E. F.,Bakulev, V. A.,Kolobov, M. Yu.,Shishkina, V. I.,Yasman, Ya. B.,Lebedev, A. T.
, p. 1051 - 1055 (2007/10/02)
5-Amino-1,2,3-thiadiazole-4NR-carboxamides were reacted with P4S10, and 5-NR-amino-1,2,3-thiadiazole-4-carbonitriles with H2S.The reversible rearrangement of 5-amino-1,2,3-thiadiazole-4-NR-carbothioamides to 5-NR-amino-1,2,3-thiadiazole-4-carbothioamides
