Iimveliso

4- [6-(6-bromo-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidin-2-ylamino)-pyridin-3-yl]- i-piperazine-1-carboxylic acid tert-butyl ester yikhompawundi enokusetyenziselwa uphando lwamachiza kunye nophuhliso lwamachiza.Isakhiwo sayo esiyinkimbinkimbi kunye namaqela asebenzayo anikezela ngamathuba ahlukeneyo ophando kunye nokuphononongwa kwezicelo zayo zonyango.Enye isicelo esinokwenzeka sale ngqungquthela kwintsimi ye-oncology.Ubukho beqela le-bromo kunye ne-pyrido [2,3-d] pyrimidin moiety ibonisa ukuba ingaba nomsebenzi wokuchasana nomhlaza.Iqela le-bromo laziwa ngokubanakho ukuthintela ukukhula kweeseli kunye nokwenza i-apoptosis kwiiseli zomhlaza.Ukongezelela, i-pyrido [2,3-d] i-scaffold ye-pyrimidin iye yadibaniswa ne-anti-proliferative and anti-tumor effects.Ngaloo ndlela, le ngqungquthela ingaqhutyelwa phambili ngokuqhutyelwa phambili njenge-agent anti-cancer inoveli.Ngaphezu koko, i-cyclopenyl kunye namaqela e-methyl akhoyo kwisakhiwo senza i-lipophilic edibeneyo, enokuthi ibe negalelo ekukwazini ukuwela imiqobo yezinto eziphilayo, njengegazi. -umqobo wengqondo.Le propati ivula ithuba lokuyisebenzisa ekuphuhliseni iziyobisi ezijoliswe kwizifo zenkqubo ye-nervous central, ezifana ne-neurological disorders.I-compound inokuguqulwa ukuze ikhulise ukukhetha kwayo kunye namandla ngokuchasene neenjongo ezithile ezibandakanyekayo kwezi zifo.Ukongezelela, ubukho be-piperazine-1-carboxylic acid tert-butyl ester moiety ibonisa ukuba i-compound ingaba ne-utility njenge-prodrug.Iimveliso zizixhobo ezingasebenziyo ezinokuguqulwa zibe ziifom ezisebenzayo ngaphakathi emzimbeni.Iqela le-tert-butyl ester linokusebenza njengeqela elikhuselayo, lithintele ukusebenza kwangaphambili kwechiza ngaphambi kokuba lifike kwindawo efunekayo yesenzo.Emva kokuba ifikelele kwi-tissue okanye iiseli ezijoliswe kuyo, iqela le-ester linokuthi lihlulwe nge-enzymatic, likhuphe i-molecule yeziyobisi ezisebenzayo.Ngaphezu koko, i-compound's pyridine kunye ne-pyrimidine moieties ibonisa amandla ayo njenge-pharmacophore yokuyila i-inhibitors ekhethiweyo kwi-enzymes okanye i-receptors ethile.Ezi zinokuthi zisuse kwi-kinases ukuya kwi-G protein-coupled receptors, kuxhomekeke kwiinguqulelo ezenziwe kwi-core structure.Le khompawundi inokusebenza njengesiqalo sezifundo zobudlelwane bomsebenzi kunye nokukhokelela ekuphuhliseni i-inhibitors ezinamandla kunye nezikhethiweyo kwiithagethi ezithile zonyango.Ngokufutshane, 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 ibonisa amandla kwiindawo ezahlukeneyo zophando lwamachiza.Ulwakhiwo lwalo olukhethekileyo kunye namaqela asebenzayo angaphononongwa ngakumbi ngomsebenzi wokuchasana nomhlaza, inkqubo ye-nervous central development drug, izicwangciso zeprodrug, kunye ne-enzyme ekhethiweyo okanye inhibition ye-receptor.Uphando oluqhubekayo kunye nokuphucula le khompawundi kunokukhokelela ekufunyanweni kokhetho olutsha lonyango oluphuculweyo olusebenzayo kunye neenkcukacha ezijoliswe kuzo.