Design and regioselective synthesis of a new generation of targeted chemotherapeutics. Part 1: EC145, a folic acid conjugate of desacetylvinblastine monohydrazide

An efficient synthesis of the folate receptor (FR) targeting conjugate EC145 is described. EC145 is a water soluble derivative of the vitamin folic acid and the potent cytotoxic agent, desacetylvinblastine monohydrazide. Both molecules are connected in regioselective manner via a hydrophilic peptide...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-10, Vol.16 (19), p.5093-5096
Hauptverfasser:	Vlahov, Iontcho R., Santhapuram, Hari Krishna R., Kleindl, Paul J., Howard, Stephen J., Stanford, Katheryn M., Leamon, Christopher P.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-cancer Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - toxicity Biological and medical sciences Chemistry Desacetylvinblastine Disulfide Disulfides - chemistry Drug Delivery Systems Drug Design Exact sciences and technology Folate Folic Acid - chemical synthesis Folic Acid - pharmacology General aspects Heterocyclic compounds Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings Medical sciences Organic chemistry Pharmacology. Drug treatments Preparations and properties Solubility Structure-Activity Relationship Targeted therapeutics Vinblastine - analogs & derivatives Vinblastine - chemical synthesis Vinblastine - pharmacology
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Zusammenfassung:	An efficient synthesis of the folate receptor (FR) targeting conjugate EC145 is described. EC145 is a water soluble derivative of the vitamin folic acid and the potent cytotoxic agent, desacetylvinblastine monohydrazide. Both molecules are connected in regioselective manner via a hydrophilic peptide spacer and a reductively labile disulfide linker.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.07.030