21168-41-2Relevant articles and documents
Interaction of a Triantennary Quinoline Glycoconjugate with the Asialoglycoprotein Receptor
Palit, Subhadeep,Banerjee, Sayanika,Mahata, Tridib,Niyogi, Sougata,Das, Tanusree,Sova Mandi, Chandra,Chakrabarti, Partha,Dutta, Sanjay
, p. 2211 - 2216 (2021/05/10)
Targeted intracellular delivery is an efficient strategy for developing therapeutics against cancer and other intracellular infections. Nonspecific drug delivery shows limited clinical applications owing to high dosage, cytotoxicity, nonspecific action, h
COMPOUNDS FOR THE DEGRADATION OF BRD9 OR MTH1
-
Page/Page column 267-268, (2020/03/29)
Compounds that degrade BRD9 or MTH1 via the ubiquitin proteasome pathway in a subject in need thereof for therapeutic applications are provided. The compounds provided have an E3 Ubiquitin Ligase targeting moiety (Degron) that is linked to a Targeting Ligand for BRD9 or MTH1.
Synthesis and preliminary structure-activity relationship study of 2-aryl-2H-pyrazolo[4,3-c]quinolin-3-ones as potential checkpoint kinase 1 (Chk1) inhibitors
Malvacio, Ivana,Cuzzolin, Alberto,Sturlese, Mattia,Vera, D. Mariano A.,Moyano, E. Laura,Moro, Stefano
, p. 171 - 183 (2017/12/26)
The serine-threonine checkpoint kinase 1 (Chk1) plays a critical role in the cell cycle arrest in response to DNA damage. In the last decade, Chk1 inhibitors have emerged as a novel therapeutic strategy to potentiate the anti-tumour efficacy of cytotoxic chemotherapeutic agents. In the search for new Chk1 inhibitors, a congeneric series of 2-aryl-2 H-pyrazolo[4,3-c]quinolin-3-one (PQ) was evaluated by in-vitro and in-silico approaches for the first time. A total of 30 PQ structures were synthesised in good to excellent yields using conventional or microwave heating, highlighting that 14 of them are new chemical entities. Noteworthy, in this preliminary study two compounds 4e2 and 4h2 have shown a modest but significant reduction in the basal activity of the Chk1 kinase. Starting from these preliminary results, we have designed the second generation of analogous in this class and further studies are in progress in our laboratories.