NQO1-responsive Prodrug for in Cellulo Release of Cytochalasin B as Cancer Cell-targeted Migrastatic

01 July 2024, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


Migrastatic drugs targeting cell motility and thereby suppress invasiveness of solid cancer cells, including their ability to metastasize and establish secondary tumors, are of high interest and have the potential to bring about a paradigm shift in the treatment of solid cancer. Cytochalasans, such as cytochalasin B, are known to disrupt cytoskeletal dynamics by inhibiting actin polymerization and have attracted considerable attention as potential migrastatics over the last decades, but are limited by selectivity issues so far. We herein report on the design, synthesis and evaluation of a bioresponsive prodrug BQTML-CB cleavable by the quinone-oxidoreductase NQO1, discussed as therapeutic target for the treatment of cancer.


Cytochalasin B
NQO1-responsive prodrug

Supplementary materials

Supplementary Information
Experimental protocols and analytical spectra


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Comment number 1, Pavla Perlikova: Jul 08, 2024, 11:14

Congratulations on your excellent work. I agree that the migrastatic activity of cytochalasins holds significant promise for cancer therapy. It would be fantastic if you could also include data on the effect of the newly developed prodrug on cell migration. Additionally, please note that the correct citation for reference 24 is: B. Formánek, D. Dupommier, T. Volfová, S. Rimpelová, A. Škarková, J. Herciková, D. Rösel, J. Brábek, P. Perlíková, RSC Med. Chem. 2024, 15, 322–343.