Cov khoom

4-[6-(6-bromo-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidin-2-ylamino)-pyridin-3-yl]- piperazine-1-carboxylic acid tert-butyl ester yog ib qho kev sib xyaw nrog kev siv hauv kev tshawb fawb tshuaj thiab kev tsim tshuaj.Nws cov txheej txheem nyuaj thiab cov pab pawg ua haujlwm muaj ntau lub sijhawm rau kev tshawb nrhiav thiab kev tshawb nrhiav ntawm nws cov kev siv tshuaj kho mob.Ib daim ntawv thov ntawm cov tshuaj no yog nyob rau hauv thaj chaw ntawm oncology.Lub xub ntiag ntawm pawg bromo thiab pyrido [2,3-d] pyrimidin moiety qhia tias nws yuav muaj kev tiv thaiv kab mob cancer.Cov pab pawg bromo paub txog nws lub peev xwm los tiv thaiv kev loj hlob ntawm tes thiab ua rau apoptosis hauv cov qog nqaij hlav cancer.Tsis tas li ntawd, pyrido [2,3-d] pyrimidin scaffold tau cuam tshuam nrog kev tiv thaiv kev loj hlob thiab tiv thaiv qog.Yog li, qhov sib xyaw no tuaj yeem kawm ntxiv rau nws lub peev xwm los ua cov tshuaj tiv thaiv kab mob tshiab.Ntxiv mus, cov pawg cyclopentyl thiab methyl tam sim no nyob rau hauv cov qauv ua rau cov lipophilic compound, uas yuav ua rau nws muaj peev xwm hla cov kab mob lom, xws li cov ntshav. - lub hlwb barrier.Cov cuab yeej no qhib qhov muaj peev xwm ntawm kev siv nws hauv kev txhim kho cov tshuaj tiv thaiv kab mob ntawm lub hauv nruab nrab paj hlwb, xws li cov kab mob neurological.Cov compound tuaj yeem hloov kho los txhim kho nws cov kev xaiv thiab muaj zog tiv thaiv cov hom phiaj tshwj xeeb cuam tshuam nrog cov kab mob no.Ntxiv rau qhov muaj cov piperazine-1-carboxylic acid tert-butyl ester moiety qhia tau hais tias cov compound tej zaum yuav muaj kev siv hluav taws xob raws li kev siv tshuaj.Prodrugs yog cov tshuaj tsis muaj zog uas tuaj yeem hloov mus rau hauv cov ntaub ntawv nquag hauv lub cev.Cov pab pawg tert-butyl ester tuaj yeem ua pab pawg tiv thaiv, tiv thaiv kev ua kom ntxov ntxov ntawm cov tshuaj ua ntej nws mus txog qhov chaw xav tau ntawm kev ua.Thaum nws ncav cuag lub hom phiaj cov ntaub so ntswg los yog cov hlwb, cov ester pawg tuaj yeem ua rau cov enzymes cleaved, tso cov tshuaj active tshuaj molecule. Tsis tas li ntawd, cov compounds pyridine thiab pyrimidine moieties qhia nws lub peev xwm raws li ib tug pharmacophore rau kev xaiv inhibitors rau tej enzymes los yog receptors.Cov no tuaj yeem sib txawv ntawm kinases mus rau G protein-coupled receptors, nyob ntawm kev hloov kho rau cov qauv tseem ceeb.Qhov kev sib xyaw no tuaj yeem ua lub luag haujlwm pib rau kev tshawb fawb txog kev sib raug zoo ntawm cov qauv-kev sib raug zoo thiab ua rau kev txhim kho kom muaj zog thiab xaiv cov inhibitors rau cov hom phiaj kho mob tshwj xeeb. -oxo-7,8-dihydro-pyrido[2,3-d]pyrimidin-2-ylamino)-pyridin-3-yl]-piperazine-1-carboxylic acid tert-butyl ester qhia tau tias muaj peev xwm hauv ntau qhov chaw ntawm kev tshawb fawb tshuaj.Nws cov qauv tshwj xeeb thiab cov pab pawg ua haujlwm tuaj yeem tshawb nrhiav ntxiv rau kev tiv thaiv kab mob qog noj ntshav, kev txhim kho hauv nruab nrab paj hlwb, cov tswv yim prodrug, thiab xaiv enzyme lossis receptor inhibition.Kev tshawb nrhiav txuas ntxiv thiab kev ua kom zoo ntawm qhov sib xyaw no tuaj yeem ua rau kev tshawb pom ntawm cov kev kho mob tshiab nrog kev txhim kho kev ua tau zoo thiab lub hom phiaj tshwj xeeb.