New cysteine derivatives with antiproliferative activity on melanoma cells.

New cysteine derivatives with antiproliferative activity on melanoma cells. Research Abstract Details 

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New cysteine derivatives with antiproliferative activity on melanoma cells. Abstract Text:

Here we describe the rational design, computer-aided virtual ligand docking and synthesis of 19 nonpeptidic compounds designed to inhibit histone deacetylases and kill melanoma cells. Compounds were derived from cysteine, fused at the S-terminus to 4-butanoyl hydroxamate, and at the N-terminus to 4-(dimethylamino)benzoic acid. The latter was extended by coupling to amines to form a small library of prospective anti-cancer compounds. Four compounds were cytotoxic at sub-micromolar concentrations against cells of a particularly aggressive human melanoma (MM96L), and nine compounds showed selectivities of >or=5:1 for killing human melanoma instead of normal human fibroblast cells. The most active compounds were shown to cause hyperacetylation of histones due to inhibition of histone deacetylases. Further refinement of these compounds may produce an anti-tumor drug suitable for treating melanoma.

New cysteine derivatives with antiproliferative activity on melanoma cells. Publishing Authors By Initials

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New cysteine derivatives with antiproliferative activity on melanoma cells. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Medicinal chemistry (Sh?riqah (United Arab Emirate

VOLUME: 2

Page Numbers: 123-32

Journal Abbreviation:

ISSN: 1573-4064

DAY: 26

MONTH: Mar

YEAR: 2006

New cysteine derivatives with antiproliferative activity on melanoma cells. Information

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LANGUAGE: eng

NlmUniqueID: 101240303

New cysteine derivatives with antiproliferative activity on melanoma cells. Keywords Mesh Terms:

KEYWORDS: Models, Chemical

MESH TERMS: pathology

Chemical & Substance for Abstract: New cysteine derivatives with antiproliferative activity on melanoma cells. Information

Substance Name: Histone Deacetylases

Registry Number: EC 3.5.1.-

Grant and Affiliation Information for New cysteine derivatives with antiproliferative activity on melanoma cells.

AFFILIATION: Centre for Drug Design and Development, Institute for Molecular Bioscience, University of Queensland, Brisbane, Queensland 4072, Australia.

Country: United Arab Emirates

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MEDLINETA: Med Chem

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