Abstract
The 17-methoxy group of geldanamycin was substituted with 1,3-diaminopropane and 1,3-diamino-2-hydroxypropane to introduce a primary amino group useful for conjugation with targeting moieties and drug carriers. We have developed a procedure that has provided improved yield and reproducibility of the syntheses. Both geldanamycin derivatives demonstrated antiproliferative activity towards the human ovarian carcinoma cell line, A2780.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Antibiotics, Antineoplastic / chemical synthesis*
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Antibiotics, Antineoplastic / chemistry
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Antibiotics, Antineoplastic / pharmacology
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Benzoquinones
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Diamines / chemistry
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Drug Carriers / chemistry
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Drug Delivery Systems
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Drug Screening Assays, Antitumor
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Humans
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Lactams, Macrocyclic
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Quinones / chemical synthesis*
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Quinones / chemistry
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Quinones / pharmacology
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Tumor Cells, Cultured
Substances
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Antibiotics, Antineoplastic
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Benzoquinones
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Diamines
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Drug Carriers
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Lactams, Macrocyclic
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Quinones
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trimethylenediamine
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geldanamycin