Acta Pharm. 56 (2006) 175-188

[ Full paper in PDF ]
Original research paper 
 

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, Universitšt 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
Accepted January 16, 2006

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