hydantoin derivatives of l- and d-amino acids synthesis and evaluation of their antiviral and antitumoral activity乙内酰脲衍生物分子的l -氨基酸合成和评估他们的抗病毒和antitumoral活动.pdfVIP

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hydantoin derivatives of l- and d-amino acids synthesis and evaluation of their antiviral and antitumoral activity乙内酰脲衍生物分子的l -氨基酸合成和评估他们的抗病毒和antitumoral活动.pdf

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hydantoin derivatives of l- and d-amino acids synthesis and evaluation of their antiviral and antitumoral activity乙内酰脲衍生物分子的l -氨基酸合成和评估他们的抗病毒和antitumoral活动

Molecules 2006, 11, 837-848 molecules ISSN 1420-3049 Full Paper Hydantoin Derivatives of L- and D-amino acids: Synthesis and Evaluation of Their Antiviral and Antitumoral Activity Zrinka Rajic 1, Branka Zorc 1,*, Silvana Raic-Malic 2, Katja Ester 3, Marijeta Kralj 3, Krešimir Pavelic 3, Jan Balzarini 4, Erik De Clercq 4 and Mladen Mintas 2,* 1 Department of Medicinal Chemistry, Faculty of Pharmacy and Biochemistry, A. Kovačića 1, HR- 10000 Zagreb, Croatia; E-mail: zrajic@pharma.hr 2 Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, Marulićev trg 20, HR-10000 Zagreb, Croatia; E-mail: silvana.raic@fkit.hr 3 Division of Molecular Medicine, Ruđer Bošković Institute, Bijenička cesta 54, HR-10000 Zagreb; E-mails: kester@irb.hr, mhorvat@irb.hr, pavelic@irb.hr 4 Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B- 3000 Leuven, Belgium; E-mail: jan.balzarini@rega.kuleuven.ac.be, erik.declercq@rega.kuleuven.be * Authors to whom correspondence should be addressed; Branka Zorc: bzbz@pharma.hr; Phone: (+385) 1 4856202, Fax: (+385) 1 4856201; Mladen Mintas: mladen.mintas@fkit.hr; Phone: (+385) 1 4597214, Fax: (+385) 1 4597224 Received: 6 October 2006; in revised form: 25 October 2006 / Accepted: 25 October 2006 / Published: 1 November 2006 Abstract: 3,5-Disubstituted hydantoin (1,3-imidazolidinedione) derivatives 5a-h were prepared by base induced cyclization of the corresponding N-(1-benzotriazolecarbonyl)-L- and D-amino acid amides 4a-h. Compounds 5a-h were evaluated for their cytostatic and antiviral activities. Among all the compounds