New Di-(β-chloroethyl)-α-amides on N-(meta-Acylaminobenzoyl)- D,L-aminoacid Supports with Antitumoral Activity
作者:Valeriu Sunel、Marcel Popa、Jacques Desbrières、Lenuta Profire、Pintilie Otilia、Lionte Catalina
DOI:10.3390/molecules13010177
日期:——
oyl)-α-aminoacids 4-9 were prepared. These compounds were subsequently converted into the corresponding Δ2-oxazolin-5-ones 10-15, which in turn were submitted to a ring opening reaction with di-(β-chloroethyl)amine to afford the peptide supported N-mustards 16-21, which showed low toxicity and cytostatic activity similar to that of sarcolisine against the Ehrlich ascite and Walker 253 carcinosarcoma
为了获得具有抗肿瘤作用的新化合物,制备了N-(间酰基氨基苯甲酰基)-α-酰基氨基苯甲酰基)-α-氨基酸4-9。这些化合物随后被转化为相应的 Δ2-恶唑啉-5-酮 10-15,进而与二-(β-氯乙基)胺进行开环反应,得到肽支持的 N-芥末 16-21,其对艾氏腹水和 Walker 253 癌肉瘤显示出与肌氨酸类似的低毒性和细胞抑制活性。