7597-45-7Relevant academic research and scientific papers
Synthesis and evaluation of thiochroman-4-one derivatives as potential leishmanicidal agents
Vargas, Esteban,Echeverri, Fernando,Vélez, Iván D.,Robledo, Sara M.,Qui?ones, Wiston
, (2018/01/17)
The S-containing heterocyclic compounds benzothiopyrans or thiochromones stand out as having promising biological activities due to their structural relationship with chromones (benzopyrans), which are widely known as privileged scaffolds in medicinal chemistry. In this work, we report the synthesis of 35 thiochromone derivatives and the in vitro antileishmanial and cytotoxic activities. Compounds were tested against intracellular amastigotes of Leishmania panamensis and cytotoxic activity against human monocytes (U-937 ATCC CRL-1593.2). Compounds bearing a vinyl sulfone moiety, 4h, 4i, 4j, 4k, 4l and 4m, displayed the highest antileishmanial activity, with EC50 values lower than 10 μM and an index of selectivity over 100 for compounds 4j and 4l. When the double bond or the sulfone moiety was removed, the activity decreased. Our results show that thiochromones bearing a vinyl sulfone moiety are endowed with high antileishmanial activity and low cytotoxicity.
ROR-GAMMA MODULATORS AND USES THEREOF
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Page/Page column 42; 43, (2016/01/21)
The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ.
Dihydrobenzopyran, thiochroman, tetrahydroquinoleine and tetrahydronaphthalene derivatives and their use in anti-cancer therapy
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Page/Page column 10-11, (2012/08/28)
New dihydrobenzopyran, thiochroman, tetrahydroquinoleine and tetrahydronaphthalene derivatives and their use in anti-cancer therapy with the general formula :
DIHYDROBENZOPYRAN, THIOCHROMAN, TETRAHYDROQUINOLEINE AND TETRAHYDRONAPHTALENE DERIVATIVES AND THEIR USE IN ANTICANCER THERAPY
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Page/Page column 22; 23, (2012/08/28)
New dihydrobenzopyran, thiochroman, tetrahydroquinoleine and tetrahydronaphthalene derivatives and their use in anti-cancer therapy with the general formula (I).
Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L
Song, Jiangli,Jones, Lindsay M.,Kumar, G. D. Kishore,Conner, Elizabeth S.,Bayeh, Liela,Chavarria, Gustavo E.,Charlton-Sevcik, Amanda K.,Chen, Shen-En,Chaplin, David J.,Trawick, Mary Lynn,Pinney, Kevin G.
experimental part, p. 450 - 453 (2012/09/25)
A series of 36 thiosemicarbazone analogues containing the thiochromanone molecular scaffold functionalized primarily at the C-6 position were prepared by chemical synthesis and evaluated as inhibitors of cathepsins L and B. The most promising inhibitors f
TRICYCLIC PYRAZOL AMINE DERIVATIVES
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Page/Page column 126-127, (2011/06/16)
This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.
Fluoride ion-catalyzed conjugate addition for easy synthesis of 3-sulfanylpropionic acid from thiol and α,β-unsaturated carboxylic acid
Gao, Shijay,Tseng, Chi,Tsai, Cheng Hsuan,Yao, Ching-Fa
, p. 1955 - 1961 (2008/09/17)
3-Sulfanylpropionic acids are obtained in excellent yields by proceeding through a simple, mild, and efficient procedure utilizing tetrabutylammonium fluoride (TBAF) as catalyst.
