Synthesis of betulinic acid derivatives with activity against human melanoma

D S Kim; J M Pezzuto; E Pisha

doi:10.1016/s0960-894x(98)00295-9

Synthesis of betulinic acid derivatives with activity against human melanoma

Bioorg Med Chem Lett. 1998 Jul 7;8(13):1707-12. doi: 10.1016/s0960-894x(98)00295-9.

Authors

D S Kim¹, J M Pezzuto, E Pisha

Affiliation

¹ Department of Medicinal Chemistry and Pharmacognosy (m/c 833), College of Pharmacy, University of Illinois at Chicago 60612-7231, USA.

PMID: 9873420
DOI: 10.1016/s0960-894x(98)00295-9

Abstract

Betulinic acid has been modified at C-3, C-20, and C-28 positions and the toxicity of the derivatives has been evaluated against cultured human melanoma (MEL-2) and human epidermoid carcinoma of the mouth (KB) cell lines. This preliminary investigation demonstrates that simple modifications of the parent structure of betulinic acid can produce potentially important derivatives, which may be developed as antitumor drugs.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Betulinic Acid
Carcinoma, Squamous Cell / pathology
Drug Screening Assays, Antitumor
Humans
Hydrogen Bonding
Melanoma / pathology*
Mouth Neoplasms / pathology
Pentacyclic Triterpenes
Triterpenes / chemical synthesis*
Triterpenes / chemistry
Triterpenes / pharmacology*

Substances

Antineoplastic Agents
Pentacyclic Triterpenes
Triterpenes
Betulinic Acid