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Synthesis and anticancer activity of poly(ester) acemetacin conjugates

  • Israel Barajas-Mendoza
  • , Alberto Espinosa-Hernández
  • , Elena Martinez-Klimova
  • , Teresa Ramirez-Ápan
  • , Marcos Martínez-García*
  • *Corresponding author for this work

Research output: Contribution to journalArticleScientificpeer-review

Abstract

Acemetacin (ACM), a carboxymethyl ester of indomethacin, is a potent anti-inflammatory drug. However, the low solubility and is easily degraded in the stomach causes gastric mucosal dysfunction. This study. Aimed to synthetize a Janus dendrimer with polyesters, which are strong protection of the acemetacin for an efficient delivery in the targets. The dendrons with two or four acemetacin molecules were attached via azido-alkyne Click reaction to obtain the Janus dendrimers. The rates of hydrolysis at stomach conditions pH 1.4 at 37 °C showed that dendrons and Janus dendrimers are constant at different times. Janus dendrimers showed good activity against three human cells: Chronic myelogenous leukemia, mammary adenocarcinoma and lung adenocarcinoma cancer cells. The dendrons and dendrimers do not show activity against normal cells. Our study comprehensively demonstrates the advantages of polyester Janus dendrimers acemetacin delivery platform and that acemetacin conjugated with polyesters can act as anticancer agent.

Original languageEnglish
Pages (from-to)3160-3170
Number of pages11
JournalJournal of Materials Research
Volume40
Issue number22
DOIs
Publication statusPublished - 28 Nov 2025
MoE publication typeA1 Journal article-refereed

Funding

This research was funded by DGAPA, grant number IN205123 and IBM and AEH were supported by a doctoral and master fellowship from CONAHCyT. We would like to thank Huerta S. E., Peña González M. A., Rios Ruiz L. M., García Rios., Orta-Pérez Ma. E., Romo Pérez A., Quiroz García B., and Márquez Alonso M. del C., for technical assistance.

Keywords

  • Acemetacin
  • Anticancer activity
  • Click reaction
  • Poli(ester)

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