Iimveliso

I-6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-enye i-hydrochloride yi-compound. kunye nezicelo ezinokwenzeka kuphando lwamachiza kunye nophuhliso lwamachiza.Ubume bayo obukhethekileyo bemolekyuli bubonelela ngamathuba ophando malunga nokusetyenziswa kwayo kwezonyango.Le khompawundi yeyosapho lwepyrido [2,3-d] pyrimidinone, oluye lwafundwa ngokubanzi kwimisebenzi yalo ye-pharmacological.Ubukho beqela le-acetyl libonisa ukusebenzisana okunokwenzeka kunye nama-enzyme abandakanyekayo kwiinkqubo zeselula.Inokuba nemiphumo yokuthintela kwi-enzymes efana ne-kinases okanye i-proteases, iyenza ibe ngumviwa othembisayo wokuphuhliswa kwe-enzyme-specific inhibitors.I-cyclopentyl kunye namaqela e-methyl kwisakhiwo negalelo kwindalo ye-lipophilic ye-compound.Le propati ivumela ukuba inqumle ngokulula imiqobo yebhayoloji, inyusa amandla ayo njengomgqatswa weziyobisi.Inokuthi iphucule i-permeability kunye ne-bioavailability, eyenza ukuba ilungele ukulawulwa komlomo kunye nokuhanjiswa kwenkqubo.I-1-piperazinyl kunye ne-2-pyridinyl amaqela akhoyo kwi-compound ibonelela ngeendlela ezahlukeneyo zokusetyenziswa kwayo ekuyilweni kweziyobisi.I-Piperazine derivatives ibonwa ngokubanzi kwi-chemistry yamayeza kwimisebenzi yabo ye-biological.Iqela le-piperazine linokufaka isandla ekubopheni i-receptor kunye nokulungelelanisa iimpawu ze-pharmacokinetic.Ngaphezu koko, iqela le-pyridine lihlala libandakanyeka ekusebenzisaneni kwe-ligand-receptor, njengoko iinkqubo zeringi ze-pyridine zingenza iibhondi ze-hydrogen kunye neendawo ezithile ze-receptor.Ezi zakhiwo zenza le ngqungquthela ibe yi-ligand enokubakho kwii-receptors ezahlukeneyo, kubandakanywa i-G protein-coupled receptors. Ukuqwalasela i-pyrido [2,3-d] i-pyrimidinone scaffold kunye nobukho beqela le-piperazine, i-compound inokuphononongwa njenge-agent anti-cancer. .Inokubonisa iziphumo ze-cytotoxic ngokuchasene neeseli zomhlaza ngokuthintelwa kweendlela ezithile zomqondiso ezinxulumene nokwanda kweeseli.Uphononongo olongezelelweyo olubandakanya i-in vitro kunye ne-vivo imodeli inokuvavanya amandla ayo njenge-agent anti-tumor.Ukongezelela, i-pyrido ye-compounds [2,3-d] i-pyrimidinone core inokuguqulwa ukuba ijolise kwizifo ezithile okanye iimeko.Ngokuzisa amaqela asebenzayo afanelekileyo okanye abathathi-nxaxheba, ukukhethwa kwayo kunye namandla kunokuphuculwa, okuvumela ukuphuhliswa kwee-agent ezikhethekileyo zonyango. i-piperazinyl) -2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-enye i-hydrochloride ibambe amandla kwiindawo ezininzi zophando lwamachiza.Iimpawu zayo zesakhiwo zivumela uphando kwi-enzyme inhibition, i-receptor binding, kunye nomsebenzi wokuchasana nomhlaza.Uphononongo olongezelelekileyo kunye nokwandisa ubume bayo obungundoqo kunokuvelisa abaviwa amayeza akwinoveli ngobuchule obuphuculweyo kunye neenkcukacha ezithile kwiithagethi ezahlukeneyo zonyango.