4.6 Article

Synthesis and anticancer activity of geldanamycin derivatives derived from biosynthetically generated metabolites

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 6, Issue 2, Pages 340-348

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/b713407j

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A new series of geldanamycin derivatives were synthesized using a semi-synthetic approach involving genetically engineered biosynthetic intermediates. These analogues were then evaluated for anti-proliferation activity in human cancer cell lines, SK-Br3 and SK-Ov3. Most of the synthesized compounds exhibited potent in vitro anti-proliferation activity toward both cell lines. Such compounds potently inhibited the expression of the Hsp90 client protein ErbB2.

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