Zogulitsa

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 ndi gulu lomwe lingagwiritsidwe ntchito pofufuza zamankhwala ndi chitukuko cha mankhwala.Mapangidwe ake ovuta komanso magulu ogwira ntchito amapereka mwayi wosiyanasiyana wofufuza ndi kufufuza ntchito zake zochizira.Mmodzi wotheka kugwiritsa ntchito mankhwalawa ndi gawo la oncology.Kukhalapo kwa gulu la bromo ndi pyrido [2,3-d] pyrimidin moiety kumasonyeza kuti ikhoza kukhala ndi ntchito yotsutsa khansa.Gulu la bromo limadziwika chifukwa cha kuthekera kwake kuletsa kukula kwa ma cell ndikupangitsa apoptosis m'maselo a khansa.Kuonjezera apo, pyrido [2,3-d] pyrimidin scaffold yakhala ikugwirizana ndi zotsutsana ndi zotupa komanso zotsutsana ndi zotupa.Choncho, gululi likhoza kuphunziridwa mowonjezereka chifukwa cha kuthekera kwake monga buku la anti-cancer agent.Komanso, magulu a cyclopenyl ndi methyl omwe alipo mu dongosololi amapanga lipophilic, zomwe zingathandize kuti athe kuwoloka zolepheretsa zamoyo, monga magazi. - chotchinga mu ubongo.Katunduyu amatsegula mwayi wogwiritsa ntchito popanga mankhwala olimbana ndi matenda amitsempha yapakati, monga matenda amisempha.Chophatikizikacho chikhoza kusinthidwa kuti chiwonjezere kusankhidwa kwake ndi potency motsutsana ndi zolinga zenizeni zomwe zimakhudzidwa ndi matendawa.Kuonjezera apo, kukhalapo kwa piperazine-1-carboxylic acid tert-butyl ester moiety kumasonyeza kuti chigawocho chikhoza kukhala chothandizira ngati mankhwala.Mankhwala osokoneza bongo ndi mankhwala osagwira ntchito omwe amatha kusinthidwa kukhala mawonekedwe ogwira ntchito mkati mwa thupi.Gulu la tert-butyl ester litha kugwira ntchito ngati gulu loteteza, kuteteza kuyambika kwamankhwala msanga asanafike pamalo omwe akufuna.Ikafika ku minofu kapena maselo omwe amawunikira, gulu la ester likhoza kudulidwa enzymatically, kutulutsa molecule yogwira ntchito ya mankhwala.Izi zitha kukhala kuchokera ku kinase kupita ku G protein-coupled receptors, kutengera masinthidwe opangidwa pakatikati.Pagululi litha kukhala poyambira maphunziro a ubale-ntchito ndikuwongolera kukhathamiritsa kuti pakhale zoletsa zamphamvu komanso zosankhidwa pazolinga zapadera zamankhwala. -oxo-7,8-dihydro-pyrido [2,3-d]pyrimidin-2-ylamino) -pyridin-3-yl]-piperazine-1-carboxylic acid tert-butyl ester imasonyeza kuthekera m'madera osiyanasiyana a kafukufuku wamankhwala.Mapangidwe ake apadera ndi magulu ogwira ntchito angathe kufufuzidwa mowonjezereka chifukwa cha ntchito zotsutsana ndi khansa, chitukuko chapakati cha mankhwala osokoneza bongo, njira zopangira mankhwala, ndi kuletsa kwa enzyme kapena receptor inhibition.Kupitiliza kufufuza ndi kukhathamiritsa kwa mankhwalawa kungapangitse kuti apeze njira zatsopano zochiritsira zomwe zimakhala zogwira mtima komanso zomwe mukufuna.