Literature DB >> 16870437

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

Iontcho R Vlahov1, Hari Krishna R Santhapuram, Paul J Kleindl, Stephen J Howard, Katheryn M Stanford, Christopher P Leamon.   

Abstract

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.

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Year:  2006        PMID: 16870437     DOI: 10.1016/j.bmcl.2006.07.030

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  30 in total

1.  Fluorine-Containing Taxoid Anticancer Agents and Their Tumor-Targeted Drug Delivery.

Authors:  Joshua Seitz; Jacob G Vineberg; Edison S Zuniga; Iwao Ojima
Journal:  J Fluor Chem       Date:  2013-08-01       Impact factor: 2.050

Review 2.  Plant-derived natural product research aimed at new drug discovery.

Authors:  Hideji Itokawa; Susan L Morris-Natschke; Toshiyuki Akiyama; Kuo-Hsiung Lee
Journal:  J Nat Med       Date:  2008-04-22       Impact factor: 2.343

3.  Cell-specific, activatable, and theranostic prodrug for dual-targeted cancer imaging and therapy.

Authors:  Santimukul Santra; Charalambos Kaittanis; Oscar J Santiesteban; J Manuel Perez
Journal:  J Am Chem Soc       Date:  2011-09-27       Impact factor: 15.419

4.  Determinants of the activities of antifolates delivered into cells by folate-receptor-mediated endocytosis.

Authors:  Rongbao Zhao; Michele Visentin; I David Goldman
Journal:  Cancer Chemother Pharmacol       Date:  2015-04-07       Impact factor: 3.333

Review 5.  Precision targeted therapy of ovarian cancer.

Authors:  Justin Sapiezynski; Oleh Taratula; Lorna Rodriguez-Rodriguez; Tamara Minko
Journal:  J Control Release       Date:  2016-10-14       Impact factor: 9.776

6.  Strategic Incorporation of Fluorine into Taxoid Anticancer Agents for Medicinal Chemistry and Chemical Biology Studies.

Authors:  Iwao Ojima
Journal:  J Fluor Chem       Date:  2017-01-03       Impact factor: 2.050

7.  Phase I study of folate conjugate EC145 (Vintafolide) in patients with refractory solid tumors.

Authors:  Patricia M Lorusso; Martin J Edelman; Susan L Bever; Karen M Forman; Maryjo Pilat; Mary F Quinn; Jing Li; Elisabeth I Heath; Lisa M Malburg; Patrick J Klein; Christopher P Leamon; Richard A Messmann; Edward A Sausville
Journal:  J Clin Oncol       Date:  2012-10-01       Impact factor: 44.544

8.  Clinical pharmacokinetics and exposure-toxicity relationship of a folate-Vinca alkaloid conjugate EC145 in cancer patients.

Authors:  Jing Li; Edward A Sausville; Patrick J Klein; David Morgenstern; Christopher P Leamon; Richard A Messmann; Patricia LoRusso
Journal:  J Clin Pharmacol       Date:  2009-10-16       Impact factor: 3.126

9.  Properties influencing the relative binding affinity of pteroate derivatives and drug conjugates thereof to the folate receptor.

Authors:  Christopher P Leamon; Fei You; Hari Krishna Santhapuram; Mingjin Fan; Iontcho R Vlahov
Journal:  Pharm Res       Date:  2009-02-03       Impact factor: 4.200

Review 10.  Recent trends in targeted anticancer prodrug and conjugate design.

Authors:  Yashveer Singh; Matthew Palombo; Patrick J Sinko
Journal:  Curr Med Chem       Date:  2008       Impact factor: 4.530

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