4-benzylideneisoquinoline-1,3(2H,4H)-diones as tyrosyl DNA phosphodiesterase 2 (TDP2) inhibitors
Tyrosyl-DNA phosphodiesterase 2 (TDP2) repairs topoisomerase II (Top2) mediated DNA damages, including double-strand breaks (DSBs) that underpin the anticancer mechanism of clinical Top2 poisons such as etoposide (ETP). Inhibition of TDP2 could sensitize
This disclosure describes modular miRNA regulator molecules and methods of using modular miRNA regulator molecules. Generally, the modular miRNA regulator molecules include a recognition module and an inhibition module. Generally, the recognition module includes a polynucleotide in which at least a portion of the polynucleotide recognizes at least a portion of a preselected pre-miRNA. Generally, the inhibition module includes a moiety that inhibits nuclease processing of the preselected pre-RNA to a mature RNA.
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Page/Page column 3
(2018/10/30)
Method for selection of hDIS3 PIN domain inhibitors and use of hDIS3 PIN domain inhibitors for cancer treatment
The present invention relates to a method for selection or screening of hDIS3 PIN domain inhibitors, yeast strain and cell line used in such methods It also relates to new therapeutic agents selected hDIS3 PIN domain inhibitors and uses thereof in the tre
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Paragraph 0163
(2016/04/22)
One-pot cascade synthesis of N-methoxyisoquinolinediones via Rh(iii)-catalyzed carbenoid insertion C-H activation/cyclization
Here a new, mild and versatile method for one-pot cascade synthesis of diverse N-methoxyisoquinolinediones via Rh(iii)-catalyzed regioselective carbenoid insertion C-H activation/cyclization of N-methoxybenzamides with α-diazotized Meldrum's acid has been achieved. Extension of the developed Rh(iii) catalysis for building new analogs of the marketed drug Edaravone has also been demonstrated.
Shi, Jingjing,Zhou, Jie,Yan, Yunnan,Jia, Jinlong,Liu, Xuelei,Song, Huacan,Xu, H. Eric,Yi, Wei
p. 668 - 671
(2015/01/09)
Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain
We report herein the synthesis of a series of 19 2-hydroxyisoquinoline-1, 3(2H,4H)-dione derivatives variously substituted at position 7 aimed at inhibiting selectively two-metal ion catalytic active sites. The compounds were tested against HIV-1 reverse
Billamboz, Muriel,Bailly, Fabrice,Barreca, Maria Letizia,De Luca, Laura,Mouscadet, Jean-Fran?ois,Calmels, Christina,Andréola, Marie-Line,Witvrouw, Myriam,Christ, Frauke,Debyser, Zeger,Cotelle, Philippe
experimental part
p. 7717 - 7730
(2009/12/07)
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