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

Kyeong Lee, Jung S Ryu, Yinglan Jin, Woncheol Kim, Navneet Kaur, Sang J Chung, Yong-Jin Jeon, Joon-Tae Park, Ji S Bang, Hong S Lee, Tae Y Kim, Jung J Lee, Young-Soo Hong
Organic & Biomolecular Chemistry 2008 January 21, 6 (2): 340-8
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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