New Di-(β-chloroethyl)-α-amides on N-(meta-Acylamino-benzoyl)-D,L-aminoacid Supports with Antitumoral Activity

Molecules

Valeriu Sunel³  Marcel Popa¹  Jacques Desbrières²  Lenuta Profire⁴  Pintilie Otilia³ 

[1] Department of Natural and Synthetic Polymers, Faculty of Chemical Engineering and Environmental Protection, Gh. Asachi Technical University, 71A B-dul Mangeron, Iasi, 700050, Romania;;Institut Pluridisciplinaire de Recherche sur l’Environnement et les Matériaux – Equipe de Physique et Chimie des Polymèrs (IPREM/EPCP), UMR 5254 CNRS – Pau et Pays de l’Adour University, Hélioparc Pau Pyrénées 2, av. President Angout, 64053 Pau Cedex 09, FranceDepartment of Organic Chemistry and Biochemistry, Faculty of Chemistry, Al. I. Cuza University, Iasi, 11 B-dul Carol I, 700506, Romania;;Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gr. T. Popa Medicine and Pharmacy University, 16 Universitatii Street, 700115, Romania

关键词: N-(acylaminobenzoyl)-α-aminoacids;    Δ²-oxazolin-5-ones;    anticancer agents;    alkylating activity;    screening;   

DOI  :  10.3390/molecules13010177

来源: mdpi

【 摘 要 】

In order to obtain new compounds with antitumoural action the N-(meta-acylaminobenzoyl)-α-acylaminobenzoyl)-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.

【 授权许可】

Unknown   
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