Lihlahisoa

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 ke motsoako o ka sebelisoang lipatlisisong tsa meriana le nts'etsopele ea lithethefatsi.Sebopeho sa eona se rarahaneng le lihlopha tse sebetsang li fana ka menyetla e sa tšoaneng ea lipatlisiso le ho hlahloba mekhoa ea eona ea phekolo.E 'ngoe e ka sebelisoang ea motsoako ona ke tšimong ea oncology.Boteng ba sehlopha sa bromo le karolo ea pyrido[2,3-d] pyrimidin e fana ka maikutlo a hore e ka ba le tšebetso e khahlanong le mofetše.Sehlopha sa bromo se tsebahala ka bokhoni ba sona ba ho thibela kholo ea lisele le ho kenya apoptosis liseleng tsa mofetše.Ho phaella moo, scaffold ea pyrido [2,3-d] pyrimidin e 'nile ea amahanngoa le liphello tse thibelang ho ata le tse khahlanong le hlahala.Ka hona, motsoako ona o ka ithutoa ka ho eketsehileng bakeng sa bokhoni ba oona e le moemeli oa anti-cancer.Ho feta moo, lihlopha tsa cyclopenyl le methyl tse teng mohahong li etsa hore motsoako oa lipophilic, o ka tlatsetsang ho khona ho tšela mekoallo ea likokoana-hloko, tse kang mali. - mokoallo bokong.Thepa ena e bula monyetla oa ho e sebelisa ho nts'etsopele ea lithethefatsi tse lebisang maloetse a tsamaiso ea methapo e bohareng, joalo ka mafu a methapo ea kutlo.Motsoako o ka fetoloa ho ntlafatsa khetho ea oona le matla khahlanong le lipheo tse khethehileng tse amehang maloetseng ana.Ho phaella moo, boteng ba piperazine-1-carboxylic acid tert-butyl ester moiety e fana ka maikutlo a hore motsoako o ka ba le thuso e le prodrug.Lihlahisoa ke metsoako e sa sebetseng e ka fetoloang ho ba mefuta e sebetsang ka hare ho 'mele.Sehlopha sa tert-butyl ester se ka sebetsa e le sehlopha se sireletsang, se thibelang hore moriana o sebelisoe pele ho nako pele o fihla sebakeng seo o se batlang.Hang ha e fihla ho lisele tse lebisitsoeng kapa lisele, sehlopha sa ester se ka phunyeletsoa ka enzymatic, se lokolla molek'hule ea lithethefatsi e sebetsang.Ho feta moo, metsoako ea metsoako ea pyridine le pyrimidine e bontša bokhoni ba eona e le pharmacophore bakeng sa ho etsa li-inhibitors tse khethiloeng bakeng sa li-enzyme kapa li-receptor tse itseng.Tsena li ka tloha ho kinase ho ea ho li-receptor tse kopantsoeng ke protheine ea G, ho latela liphetoho tse entsoeng ho sebopeho sa mantlha.Motsoako ona o ka sebetsa e le qalo ea lithuto tsa likamano tsa sebopeho le ts'ebetso le ho etsa hore ho be le ntlafatso e matla ho nts'etsapele li-inhibitors tse matla le tse khethang bakeng sa lipheo tse khethehileng tsa kalafo. -oxo-7,8-dihydro-pyrido [2,3-d]pyrimidin-2-ylamino) -pyridin-3-yl]-piperazine-1-carboxylic acid tert-butyl ester e bontša bokhoni libakeng tse sa tšoaneng tsa lipatlisiso tsa meriana.Sebopeho sa eona se ikhethang le lihlopha tse sebetsang li ka hlahlojoa ho ea pele bakeng sa ts'ebetso e khahlanong le mofetše, nts'etsopele ea tsamaiso ea methapo ea methapo, maano a prodrug, le ho khetha enzyme kapa thibelo ea li-receptor.Ho tsoela pele ho etsa lipatlisiso le ho ntlafatsa motsoako ona ho ka lebisa ho sibolloeng ha mekhoa e mecha ea phekolo e nang le ts'ebetso e ntlafetseng le sepheo se tobileng.