Amino acid derivatives. Part I. Synthesis, antiviral and antitumor evaluation of new alpha-amino acid esters bearing coumarin side chain.
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 was assayed 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).
Al-Masoudi
Najim A
NA
Fachbereich Chemie, Universität Konstanz, Postfach 5560, D-78457 Konstanz, Germany. najim.al-masoudi@gmx.de
Al-Masoudi
Iman A
IA
Ali
Ibrahim A I
IA
Al-Soud
Yaseen A
YA
Saeed
Bahjat
B
La Colla
Paolo
P
D000596:Amino Acids / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003374:Coumarins / Q000138:chemical synthesis / Q000494:pharmacology*; D001908:Diarrhea Viruses, Bovine Viral / Q000187:drug effects* / Q000254:growth & development; D004952:Esters; D015497:HIV-1 / Q000187:drug effects* / Q000254:growth & development; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000596:Amino Acids; D000970:Antineoplastic Agents; D000998:Antiviral Agents; D003374:Coumarins; D004952:Esters