Preparation of amino acid conjugates of betulinic acid with activity against human melanoma

Betulinic acid has been coupled with a series of amino acids at C-28 carbox ylic acid position and the toxicity of the derivatives has been evaluated a gainst cultured human melanoma (MEL-2) and human epidermoid carcinoma of th e mouth (KB) cell lines. A number of amino acid conjugates of betulinic aci d showed improved water solubility as well as selective cytotoxicity. This investigation demonstrates that amino acid conjugates of betulinic acid can produce potentially important derivatives, which may be developed as antit umor agents. (C) 1999 Elsevier Science Ltd. All rights reserved.