Simple thalidomide analogs in melanoma: Synthesis and biological activity

Alexia Barbarossa, Alessia Catalano, Jessica Ceramella, Alessia Carocci, Domenico Iacopetta, Camillo Rosano, Carlo Franchini, Maria Stefania Sinicropi

Research output: Contribution to journalArticlepeer-review

Abstract

Thalidomide is an old well-known drug that is still of clinical interest, despite its terato-genic activities, due to its antiangiogenic and immunomodulatory properties. Therefore, efforts to design safer and effective thalidomide analogs are continually ongoing. Research studies on thalidomide analogs have revealed that the phthalimide ring system is an essential pharmacophoric fragment; thus, many phthalimidic compounds have been synthesized and evaluated as anticancer drug candidates. In this study, a panel of selected in vitro assays, performed on a small series of phthalimide derivatives, allowed us to characterize compound 2k as a good anticancer agent, acting on A2058 melanoma cell line, which causes cell death by apoptosis due to its capability to inhibit tubulin polymerization. The obtained data were confirmed by in silico assays. No cytotoxic effects on normal cells have been detected for this compound that proves to be a valid candidate for further investigations to achieve new insights on possible mechanism of action of this class of compounds as anticancer drugs.

Original languageEnglish
Article number5823
JournalApplied Sciences (Switzerland)
Volume11
Issue number13
DOIs
Publication statusPublished - Jul 1 2021

Keywords

  • Anticancer
  • Apoptosis
  • Drugs repositioning
  • Molecular docking studies
  • Thalidomide analogs
  • Tubulin

ASJC Scopus subject areas

  • Materials Science(all)
  • Instrumentation
  • Engineering(all)
  • Process Chemistry and Technology
  • Computer Science Applications
  • Fluid Flow and Transfer Processes

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