Antineoplastic Agents. 604. the Path of Quinstatin Derivatives to Antibody Drug Conjugates

George Pettit, Noeleen Melody, Jean Chapuis

Research output: Contribution to journalArticle

1 Scopus citations

Abstract

To further evaluate the exceptional cancer cell growth inhibition by the quinstatins, of which one of the series, quinstatin 8, approaches the exceptional cytotoxic activity of the parent dolastatin 10 (1), four of the quinstatins have been converted to desmethyl derivatives. Three of the four (4, 5, and 8 [7b-d]) were next bonded to the linker (8) employed in the synthesis of the very successful and structurally related anticancer drug Adcetris (3). Owing to these structural modifications, a next step could be taken by bonding to a monoclonal antibody, thereby producing an antibody drug conjugate (ADC) related to Adcetris structurally but with the possibility of a wider spectrum of activity and utility.

Original languageEnglish (US)
Pages (from-to)2447-2452
Number of pages6
JournalJournal of Natural Products
Volume80
Issue number9
DOIs
StatePublished - Jan 1 2017

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ASJC Scopus subject areas

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

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