1245654-95-8

Upstream product

• 1245654-44-7 10-amino-1,2,3,4-tetrahydropyrido[2,1-a]isoindol-6(10bH)-one 
• 103-71-9 phenyl isocyanate 
• 582-61-6 benzoyl azide 
• 98-88-4 benzoyl chloride 
• 65-85-0 benzoic acid 
• 1245654-43-6 10-amino-1,3,4,10b-tetrahydropyrido[2,1-a]isoindole-2,6-dione 
• 325851-19-2 4-nitro-2-(3-oxobutyl)isoindoline-1,3-dione 
• 603-62-3 4-nitro-1H-isoindole-1,3(2H)-dione 

Relevant academic research and scientific papers

Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): Potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts

The development of CDK and GSK3 inhibitors has been regarded as a potential therapeutic approach, and a substantial number of diverse structures have been reported to inhibit CDKs and GSK-3β in recent years. Only a few molecules have gone through or are currently undergoing clinical trials as CDK and GSK inhibitors. In this paper, we prepared valmerins, a new family containing the tetrahydropyrido[1,2-a]isoindone core. The fused heterocycle was prepared with a straightforward synthesis that was functionalized by a (het)arylurea. Twelve valmerins inhibited the CDK5 and GSK3 with an IC50 100 nM. A semiquantitative kinase scoring was realized, and a cellular screening was done. At the end of our study, we investigated the in vivo potency of one valmerin. Mice exhibited good tolerance to our lead, which proved its efficacy and clearly blocked tumor growth. Valmerins appear also as good candidates for further development as anticancer agents.

DERIVATIVES OF 10-AMINO-1,2,3,4-TETRAHYDROPYRIDO[2,1-A]ISOINDOL-6(10BH)-ONES, METHOD FOR PREPARATION THEREOF AND THERAPEUTIC USES THEREOF

The present invention relates to compounds having the following general formula (I): wherein: A represents a SO2 or CX group, X representing O or S;R1, R2, R″, R4 represent in particular H,R represents in particular an alkyl group or an aryl group, as well as to the pharmaceutically acceptable salts thereof, the compound of formula (I) taking the form of a pure stereoisomer or an enantiomer and/or diastereoisomer mixture, including racemic mixtures.