Basic Information
ID: ALA4130434
Journal: J Nat Prod
Title: Antineoplastic Agents. 604. The Path of Quinstatin Derivatives to Antibody Drug Conjugates.
Authors: Pettit GR, Melody N, Chapuis JC.
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.
CiteXplore: 28895394
DOI: 10.1021/acs.jnatprod.7b00237
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets