2. Academic Validation
  3. Amino(oxo)acetate moiety: A new functional group to improve the cytotoxicity of betulin derived carbamates

Amino(oxo)acetate moiety: A new functional group to improve the cytotoxicity of betulin derived carbamates

  • Bioorg Med Chem Lett. 2016 Jun 15;26(12):2852-2854. doi: 10.1016/j.bmcl.2016.04.055.
Lucie Heller 1,  Vincent Perl 1,  Jana Wiemann 1,  Ahmed Al-Harrasi 2,  René Csuk 1
Affiliations

Affiliations

  • 1 Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany.
  • 2 University of Nizwa, Chair of Oman's Medicinal Plants and Marine Natural Products, PO Box 33, Birkat Al-Mauz, Nizwa, Oman.
PMID: 27142753 DOI: 10.1016/j.bmcl.2016.04.055
Abstract

While 3-O-acetylated betulin derivatives carrying a carbamate moiety at position C-28 are of rather low cytotoxicity for human tumor cell lines, the corresponding C-3 amino(oxo) acetates show good cytotoxicity. For example, an EC50 as low as 2.0μM was found for (3β) 28-{[(hexylamino)carbonyl]oxy}lup-20(29)-en-3-yl amino(oxo)acetate (16) employing the ovarian Cancer cell line A2780.

Keywords

Betulin; Cytotoxicity; Triterpene.

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