Exploring BenzylethoxyAryl Urea Scaffolds for Multitarget Immunomodulation Therapies

Raquel Gil-Edo, German Hernández-Ribelles, Santiago Royo, Natasha Thawait, Alan Serrels, Miguel Carda, Eva Falomir

Research output: Contribution to journalArticlepeer-review

Abstract / Description of output

Thirteen benzylethoxyaryl ureas have been synthesized and biologically evaluated as multitarget inhibitors of VEGFR-2 and PD-L1 proteins to overcome resistance phenomena offered by cancer. The antiproliferative activity of these molecules on several tumor cell lines (HT-29 and A549), on the endothelial cell line HMEC-1, on immune cells (Jurkat T) and on the non-tumor cell line HEK-293 has been determined. Selective indexes (SI) have been also determined and compounds bearing p-substituted phenyl urea unit together with a diaryl carbamate exhibited high SI values. Further studies on these selected compounds to determine their potential as small molecule immune potentiators (SMIPs) and as antitumor agents have been performed. From these studies, we have concluded that the designed ureas have good tumor antiangiogenic properties, exhibit good inhibition of CD11b expression, and regulate pathways involved in CD8 T-cell activity. These properties suggest that these compounds could be potentially useful in the development of new cancer immune treatments
Original languageEnglish
Pages (from-to)8582
JournalInternational Journal of Molecular Sciences
Issue number10
Early online date11 May 2023
Publication statusE-pub ahead of print - 11 May 2023

Keywords / Materials (for Non-textual outputs)

  • aryl urea
  • benzylethoxyaryl urea
  • angiogenesis
  • PD-L1
  • VEGFR-2
  • TLCRs
  • immune checkpoints
  • PD-1
  • TIM-3
  • LAG-3
  • CD11b
  • CD69
  • OX-40
  • CD8+
  • T cell
  • LCK
  • Fyn
  • LAT
  • ZAP70


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