Methotrexate α-tert-Butyl Ester

Methotrexate α-tert-butyl ester，经 OtBu 修饰，显著降低 HT1080 荷瘤小鼠的肿瘤生长。Methotrexate 是一种抗代谢和抗叶叶酸剂，也是一种免疫抑制剂和抗肿瘤药物。生物活性Methotrexateα-tert-butylester，经OtBu修饰，显著降低HT1080荷瘤小鼠的肿瘤生长。Methotrexate是一种抗代谢和抗叶叶酸剂，也是一种免疫抑制剂和抗肿瘤药物。体外研究OtBu-MTX-PVGislessHT1080thanMTX-PVGagainstHT1080cells.Itshowsthatprotectionoftheα-carboxylgroupofMTXresultsinreducedinvitroactivity.体内研究Lys-MTXcleavable-(OtBu)significantlyreducestumorgrowthinHT1080tumorbearingmice.Theprotectionoftheα-carboxylgroupofmethotrexatemaybeusedtoimprovethecirculatoryhalf-lifeandreducetheliveraccumulationofsimilarMTX-conjugateddendrimers,whilestillretainingantitumoractivityinvivo.AnimalModel:Female,Balb/cnu/nu,6weeks(bearingHT1080cells)Dosage:30mg/kgAdministration:Onceperweekfor2weeksResult:Showedasignificant(63%)reductionintumorsizeonday12.