Synthesis and structure-activity relationship of furoquinolinediones as inhibitors of Tyrosyl-DNA phosphodiesterase 2 (TDP2)
作者:Le-Mao Yu、Zhu Hu、Yu Chen、Azhar Ravji、Sophia Lopez、Caroline B. Plescia、Qian Yu、Hui Yang、Monica Abdelmalak、Sourav Saha、Keli Agama、Evgeny Kiselev、Christophe Marchand、Yves Pommier、Lin-Kun An
DOI:10.1016/j.ejmech.2018.04.024
日期:2018.5
Tyrosyl-DNA phosphodiesterase 2 (TDP2) is a recently discovered enzyme specifically repairing topoisomerase II (TOP2)-mediated DNA damage. It has been shown that inhibition of TDP2 synergize with TOP2 inhibitors. Herein, we report the discovery of the furoquinolinedione chemotype as a suitable skeleton for the development of selective TDP2 inhibitors. Compound 1 was identified as a TDP2 inhibitor as a result
increasingly investigated for a range of applications spanning from healthcare to advanced functional materials. Synthetic glycopolymers are particularly attractive as they possess low toxicity and immunogenicity and can be used as multivalent ligands to target sugar-binding proteins (lectins). Here, we utilised RAFT polymerisation to synthesize two families of novel diblock copolymers consisting of a
The present invention provides compounds, compositions thereof, and methods of using the same.
本发明提供了化合物、其组合物以及使用相同的方法。
LIQUID BISACYLPHOSPHINE OXIDE PHOTOINITIATOR
申请人:BASF SE
公开号:US20160168177A1
公开(公告)日:2016-06-16
A photoinitiator mixture comprising the components
(a) a compound of the formula (I)
wherein
Ar and Ar
2
independently of each other are
or naphthyl which is unsubstituted or substituted one or more times by R
1
, R
2
, R
3
or R′; R
1
and R
3
in-dependently of each other are C
1
-C
4
alkyl, C
1
-C
4
alkoxy or halogen; R
2
is hydrogen, C
1
-C
4
alkyl, halogen, C
1
-C
4
alkoxy or C
2
-C
20
alkoxy which is interrupted by one or more O; Q is C
1
-C
4
alkylene; R
4
is methyl or ethyl; R′ and R″ independently of each other are hydrogen or PG-Y-R′″—X—; PG is a polymerizable group or methyl or ethyl; Y is a direct bond, O or S; X is a direct bond, O or S; R′″ is a direct bond, C
1
-C
20
alkylene or C
2
-C
20
alkylene which is interrupted by one or more O;
(b) one or more compounds of the formula (II)
wherein
Ar
1
, Ar
2
and Q are as defined above, and R
5
is for example C
3
-C
30
alkyl which is unsubstituted or substituted and
(c) optionally a compound of the formula (III)
R
5
—OH (III), wherein
R
5
is as defined above; provides a liquid photointiator.
[EN] NOVEL PHOTO-INITIATORS AND THEIR APPLICATION<br/>[FR] NOUVEAUX PHOTO-INITIATEURS ET LEUR UTILISATION
申请人:ETH ZUERICH
公开号:WO2019175112A1
公开(公告)日:2019-09-19
The present invention relates to novel bisacylphosphinic acids, salts and derivatives thereof as well as their use as photo-initiators with superior water solubility and photo-activity. The invention further encompasses versatile processes for the preparation of the aforementioned compounds.