Sunel Valeriu, Popa Marcel, Desbrières Jacques, Profire Lenuta, Otilia Pintilie, Catalina Lionte
Department of Organic Chemistry and Biochemistry, Faculty of Chemistry, Al. I. Cuza University, Iasi, 11 B-dul Carol I, 700506, Romania.
Molecules. 2008 Jan 28;13(1):177-89. doi: 10.3390/molecules13010177.
In order to obtain new compounds with antitumoural action the N-(meta-acylaminobenzoyl)-alpha-acylaminobenzoyl)-alpha-aminoacids 4-9 were prepared. These compounds were subsequently converted into the corresponding Delta(2)-oxazolin-5-ones 10-15, which in turn were submitted to a ring opening reaction with di-(beta-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-（间酰氨基苯甲酰基）-α-酰氨基苯甲酰基-α-氨基酸4-9。这些化合物随后被转化为相应的Δ(2)-恶唑啉-5-酮10-15，进而使其与二（β-氯乙基）胺发生开环反应，得到肽负载的N-芥子气16-21，其毒性较低，对艾氏腹水癌和沃克253癌肉瘤的细胞生长抑制活性与肌氨酸相似。
