Methotrexate α-tert-butyl ester,經(jīng) OtBu 修飾,顯著降低 HT1080 荷瘤小鼠的腫瘤生長。Methotrexate 是一種抗代謝和抗葉葉酸劑,也是一種免疫抑制劑和抗腫瘤藥物。生物活性Methotrexateα-tert-butylester,經(jīng)OtBu修飾,顯著降低HT1080荷瘤小鼠的腫瘤生長。Methotrexate是一種抗代謝和抗葉葉酸劑,也是一種免疫抑制劑和抗腫瘤藥物。體外研究OtBu-MTX-PVGislessHT1080thanMTX-PVGagainstHT1080cells.Itshowsthatprotectionoftheα-carboxylgroupofMTXresultsinreducedinvitroactivity.體內(nèi)研究Lys-MTXcleavable-(OtBu)significantlyreducestumorgrowthinHT1080tumorbearingmice.Theprotectionoftheα-carboxylgroupofmethotrexatemaybeusedtoimprovethecirculatoryhalf-lifeandreducetheliveraccumulationofsimilarMTX-conjugateddendrimers,whilestillretainingantitumoractivityinvivo.AnimalModel:Female,Balb/cnu/nu,6weeks(bearingHT1080cells)Dosage:30mg/kgAdministration:Onceperweekfor2weeksResult:Showedasignificant(63%)reductionintumorsizeonday12.
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