Description
NMS-1286937isaninhibitorofpolo-likekinase1(PLK1)thatiscurrentlyinclinicaltrialsasapotentialtreatmentforvariouscancers;itexhibitsanticancerchemotherapeuticactivity.Inosteosarcomacells,NMS-1286937inducescellcyclearrestandapoptosisandinhibitscellgrowth.Inanimalmodelsofacutemyelogenousleukemia(AML),thiscompoundincreasessurvivaltimeanddecreasestumorcellinfiltration.Additionally,NMS-1286937inhibitscellproliferationandinducesapoptosis,cellcyclearrest,andtumorregressionincellularandanimalmodelsofcoloncancer.
References
SEROV,TAvantiE,VellaS,etal.Targetingpolo-likekinase1byNMS-P937inosteosarcomacelllinesinhibitstumorcellgrowthandpartiallyovercomesdrugresistance.InvestNewDrugs.2014Dec;32(6):1167-80.PMID:25193492.
CasolaroA,GolayJ,AlbaneseC,etal.ThePolo-LikeKinase1(PLK1)inhibitorNMS-P937iseffectiveinanewmodelofdisseminatedprimaryCD56+acutemonoblasticleukaemia.PLoSOne.2013;8(3):e58424.PMID:23520509.
ValsasinaB,BeriaI,AlliC,etal.NMS-P937,anorallyavailable,specificsmall-moleculepolo-likekinase1inhibitorwithantitumoractivityinsolidandhematologicmalignancies.MolCancerTher.2012Apr;11(4):1006-16.PMID:22319201.
BeriaI,BossiRT,BrascaMG,etal.NMS-P937,a4,5-dihydro-1H-pyrazolo[4,3-h]quinazolinederivativeaspotentandselectivePolo-likekinase1inhibitor.BioorgMedChemLett.2011May15;21(10):2969-74.PMID:21470862.
