title: Regioselective synthesis of folate receptor-targeted agents derived from epothilone analogs and folic acid.
abstract: Efficient regioselective syntheses of conjugates of folic acid and cytotoxic agents derived from natural epothilones are described. These folate receptor (FR) targeting compounds are water soluble and incorporate a hydrophilic peptide-based spacer unit and a reducible self-immolative disulfide-based linker system between the FR-targeting ligand and the parent drug.
authors.affiliation: Endocyte Inc., West Lafayette, IN 47906, USA. ivlahov@endocyte.com
authors.forename: Iontcho R
authors.initials: IR
authors.lastname: Vlahov
authors.forename: Gregory D
authors.initials: GD
authors.lastname: Vite
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Kleindl
authors.forename: Yu
authors.initials: Y
authors.lastname: Wang
authors.forename: Hari Krishna R
authors.initials: HK
authors.lastname: Santhapuram
authors.forename: Fei
authors.initials: F
authors.lastname: You
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: Howard
authors.forename: Soong-Hoon
authors.initials: SH
authors.lastname: Kim
authors.forename: Francis F Y
authors.initials: FF
authors.lastname: Lee
authors.forename: Christopher P
authors.initials: CP
authors.lastname: Leamon
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004220:Disulfides / Q000737:chemistry; D034261:Epothilones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D058973:Folate Receptors, GPI-Anchored / Q000037:antagonists & inhibitors* / Q000378:metabolism; D005492:Folic Acid / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D004220:Disulfides; D034261:Epothilones; D058973:Folate Receptors, GPI-Anchored; D005492:Folic Acid