【摘 要】
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Geldanamycin (GDM) is a benzoquinone ansamycin produced by Streptomyces hygroscopicus.It is an important anticancer agent that inhibits specifically heat shock
【机 构】
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KeyLaboratoryofBiotechnologyofAntibiotics,MinistryofHealth,InstituteofMedicinalBiotechnology,CAMS&PU
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Geldanamycin (GDM) is a benzoquinone ansamycin produced by Streptomyces hygroscopicus.It is an important anticancer agent that inhibits specifically heat shock protein 90 (Hsp90), but shows severe hepatotoxicity and poor water solubility.We are interested in obtaining novel natural GDM analogues with improved water solubility and potent antitumor cell activity.We explored the potential of Streptomyces hygroscopicus 17997, a GDM producer, for natural GDM analogue(s) production, which resulted in the discovery of thiazinogeldanamycin, 19-S-methylgeldanamycin and 4,5-dihydro-4-hydroxygeldanamycins.Compared to GDM, all these natural GDM analogues showed much improved water solubility.Compounds 19-S-methylgeldanamycin and 4,5-dihydro-4-hydroxygeldanamycins exhibited still strong antitumor cell activity, and thiazinogeldanamycin displayed moderate antitumor cell activity.
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