ABSTRACTIn this article, an improved synthesis strategy of the potent anticancer compound 4,7‐dichloro‐2‐quinolinemethanol (QM) and its acrylate ester 4,7‐dichloro‐2‐quinolinemethylacrylate (AQM) are described. AQM is copolymerized using free‐radical polymerization with N‐vinyl‐2‐pyrrolidone (VP) and the copolymers obtained from different molar ratios of monomers are subjected to nanoprecipitation to produce suspensions of nanoparticles (NPs) in phosphate buffered saline (PBS). The smallest and stable NPs are prepared with the AQM‐VP copolymers 45:55 and 40:60 (118.9 and 128.7 nm in diameter, respectively) at 1 mg mL−1, and along with AQM and QM, are evaluated for their cytotoxic activity on MDA‐MB‐453 breast carcinoma cells using MTT bioassay. AQM and QM are highly cytotoxic (IC50: 19 and 41 μM, respectively); however, the NPs are not cytotoxic in the range of the assayed concentrations. These results contribute to the search for new polymeric NPs with potential application as QM delivery systems for the treatment of cancer or other diseases treatable with QM. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019, 136, 47545.