Acta Pharm. 56 (2006) 175-188

Amino acid derivarives Part I. Synthesis, antiviral and antitumor evaluation of new alpha-amino acid esters
bearing coumarin side chain

NAJIM A. AL-MASOUDI,^1* IMAN A. AL-MASOUDI,²  IBRAHIM A. I. ALI,³  YASEEN A. AL-SOUD,⁴  BAHJAT SAEED,² 
and PAOLO LA COLLA⁵

najim.al-masoudi@gmx.de

¹ Fachbereich Chemie, Universität Konstanz, Postfach 5560, D-78457 Konstanz, Germany
² College of Veterinary Medicine, University of Basrah, Basrah, Iraq
³ Department of Chemistry, Faculty of Science, Suez Canal University, Ismailia, Egypt
⁴ Department of Chemistry, College of Science, University of Al al-Bayt, Jordan
⁵ Universita di Cagliari, Departimento di Biologia Sperimentale Sezione di Microbiologia, 09042 Cagliari, Italy

A series of amino acid esters bearing coumarin (3-15) were synthesized and evaluated, in vitro, against HIV-1, and bovine viral diarrhea virus (BVDV). The in vitro cytotoxicity of 3-10 and 12 were assyed against a panel of tumor cell lines consisting of CD4 human T-cells. Compound 14 showed inhibition of HIV-1 with EC₅₀ > 1.6 microg mL^-1, meanwhile compound 9 exhibited activity against leukaemia (MT4) with CC₅₀ = 24 micromol L^-1).

Keywords: amino acids, antitumor activity, antiviral activity, coumarin