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Molecules 2008, 13(1), 177-189; doi:10.3390/molecules13010177
Article

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

1
,
2
,
3, 4,* , 1
 and
5
1 Department of Organic Chemistry and Biochemistry, Faculty of Chemistry, Al. I. Cuza University, Iasi, 11 B-dul Carol I, 700506, Romania 2 Department of Natural and Synthetic Polymers, Faculty of Chemical Engineering and Environmental Protection, Gh. Asachi Technical University, 71A B-dul Mangeron, Iasi, 700050, Romania 3 IPREM/EPCP, UMR 5254 CNRS, University of Pau et Pays de l’Adour, Hélioparc Pau Pyrénées 2, av. President Angout, 64053 Pau, France 4 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gr. T. Popa Medicine and Pharmacy University, 16 Universitatii Street, 700115, Romania 5 Medical Clinic, Emergency Clinic Hospital, Faculty of Medicine, Gr. T. Popa Medicine and Pharmacy University, 16 Universitatii Street, 700115, Romania
* Author to whom correspondence should be addressed.
Received: 30 December 2007 / Revised: 23 January 2007 / Accepted: 23 January 2007 / Published: 28 January 2008
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Abstract

In order to obtain new compounds with antitumoural action the N-(metaacylaminobenzoyl)-α-acylaminobenzoyl)-α-aminoacids 4-9 were prepared. Thesecompounds 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 toafford the peptide supported N-mustards 16-21, which showed low toxicity and cytostaticactivity similar to that of sarcolisine against the Ehrlich ascite and Walker 253carcinosarcoma.
Keywords: N-(acylaminobenzoyl)-α-aminoacids; Δ2-oxazolin-5-ones; anticancer agents; N-(acylaminobenzoyl)-α-aminoacids; Δ2-oxazolin-5-ones; anticancer agents;
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Sunel, V.; Popa, M.; Desbrières, J.; Profire, L.; Otilia, P.; Catalina, L. New Di-(β-chloroethyl)-α-amides on N-(meta-Acylaminobenzoyl)- D,L-aminoacid Supports with Antitumoral Activity. Molecules 2008, 13, 177-189.

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