Ngwaahịa

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 bụ ngwakọta nwere ike iji na nyocha ọgwụ na mmepe ọgwụ.Ọdịdị ya dị mgbagwoju anya na otu ndị na-arụ ọrụ na-enye ohere dị iche iche maka nyocha na nyocha nke ngwa ọgwụgwọ ya. Otu ngwa nwere ike ime nke a bụ n'ọhịa nke oncology.Ọnụnọ nke ìgwè bromo na pyrido [2,3-d] pyrimidin moiety na-egosi na ọ nwere ike inwe ọrụ mgbochi ọrịa cancer.A maara otu bromo maka ikike ya igbochi uto cellular na ịkpata apoptosis na mkpụrụ ndụ kansa.Tụkwasị na nke ahụ, pyrido [2,3-d] pyrimidin scaffold ejirila mmetụta mgbochi proliferative na mgbochi tumor.N'ihi ya, a pụrụ ịmụba ogige a maka ikike ya dị ka onye na-ahụ maka ọrịa cancer ọhụrụ. Ọzọkwa, òtù cyclopentyl na methyl dị na nhazi ahụ na-eme ka ogige ahụ lipophilic, nke nwere ike inye aka na ikike ya ịgafe ihe mgbochi ndụ, dị ka ọbara. -ụbụrụ mgbochi.Ihe onwunwe a na-emepe ohere nke iji ya mee ihe na mmepe nke ọgwụ ndị na-elekwasị anya na ọrịa nke usoro nhụjuanya nke etiti, dị ka ọrịa nhụjuanya.Enwere ike gbanwee ogige ahụ iji welie nhọrọ ya na ike ya megide ebumnuche ndị a kapịrị ọnụ na-etinye aka na ọrịa ndị a. Tụkwasị na nke ahụ, ọnụnọ nke piperazine-1-carboxylic acid tert-butyl ester moiety na-egosi na ogige ahụ nwere ike ịba uru dị ka prodrug.Prodrugs bụ ogige na-adịghị arụ ọrụ nke enwere ike ịtụgharị ka ọ bụrụ ụdị arụ ọrụ n'ime ahụ.Otu tert-butyl ester nwere ike ije ozi dị ka otu nchekwa, na-egbochi ịgbalite ọgwụ ahụ n'oge tupu ya erute ebe a chọrọ ime.Ozugbo ọ ruru anụ ahụ ma ọ bụ sel e lekwasịrị anya, ester otu nwere ike ịgbaji enzymatically, na-ahapụ molekul ọgwụ na-arụ ọrụ. Ọzọkwa, pyridine na pyrimidine moieties nke ogige na-egosi ikike ya dị ka pharmacophore maka ịmepụta ndị na-emechi ihe maka ụfọdụ enzymes ma ọ bụ ndị na-anabata ya.Ndị a nwere ike ịdị site na kinase ruo na ndị nnabata protein jikọtara ọnụ, dabere na mgbanwe ndị emere na nhazi isi.Ngwakọta a nwere ike ịbụ mmalite mmalite maka ọmụmụ ihe gbasara mmekọrịta mmekọrịta yana iduzi njikarịcha iji mepụta ndị na-egbochi ike na nhọrọ maka ebumnuche ọgwụgwọ kpọmkwem.Na nchịkọta, 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 na-egosipụta ike na mpaghara dị iche iche nke nyocha ọgwụ.Enwere ike nyochaa usoro ya pụrụ iche na otu ndị na-arụ ọrụ maka ọrụ mgbochi ọrịa cancer, mmepe nke usoro nhụjuanya nke etiti, usoro prodrug, na nhọrọ enzyme ma ọ bụ mgbochi nnabata.Nnyocha na-aga n'ihu na njikarịcha nke ogige a nwere ike iduga n'ịchọpụta nhọrọ ọgwụgwọ ọhụrụ yana arụmọrụ dị mma yana nlebara anya kpọmkwem.