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Research Article Open access CC BY 4.0

Synthesis and Evaluation of Cytotoxic Activity of 2-Aryl-2-(3-Indolyl)Propionic Acid Derivatives

Alexander V. Aksenov, Nicolai A. Aksenov, Nikolai A. Arutiunov, Dmitrii A. Aksenov, Anna M. Zatsepilina, Daria I. Murashkina, Maksim O. Shcheglov, Sergei N. Ovcharov

Organics · pp. 11–11 · Published 3 Mar 2026

10.3390/org7010011

Abstract

2-Aryl-2-(3-indolyl)acetohydroxamic acids have emerged as promising antitumor agents; however, their poor pharmacokinetic profile remains a significant drawback. To address this limitation, we have synthesized a homolog of such acids—specifically 2-aryl-2-(3-indolyl)propionic acid (IC50 > 100 mM (U87)), along with several other derivatives: ethyl ester (IC50 > 100 mM (U87)), hydroxamate (IC50 21.2 ± 1.0 mM (U87)) and hydrazide (IC50 > 100 mM (U87)). The cytotoxicity of these compounds against glioblastoma cell lines was evaluated and compared to that of the parent acetohydroxamic acid derivatives.

Cytotoxicity Chemistry Hydrazide Cytotoxic T cell Acetohydroxamic acid Cell culture Biochemistry Pharmacokinetics

References (12)

  1. 1 Gao, 2021, Antitumor Agents Based on Metal–Organic Frameworks [DOI]
  2. 2 Cháirez-Ramírez, M.H., de la Cruz-López, K.G., and García-Carrancá, A. (2021). Polyphenols as Antitumor Agents Targeting Key Players in Cancer-Driving Signaling Pathways. Front. Pharmacol., 12. [DOI]
  3. 3 Mehra, 2022, Indole Derived Anticancer Agents [DOI]
  4. 4 Russo, E., Grondona, C., Brullo, C., Spallarossa, A., Villa, C., and Tasso, B. (2023). Indole Antitumor Agents in Nanotechnology Formulations: An Overview. Pharmaceutics, 15. [DOI]
  5. 5 Salerno, S., Barresi, E., Baglini, E., Poggetti, V., Da Settimo, F., and Taliani, S. (2023). Target-Based Anticancer Indole Derivatives for the Development of Anti-Glioblastoma Agents. Molecules, 28. [DOI]
  6. 6 Yan, 2022, Structure Modification and Biological Evaluation of Indole-Chalcone Derivatives as Anti-Tumor Agents through Dual Targeting Tubulin and TrxR [DOI]
  7. 7 Devi, 2021, Recent Development in Indole Derivatives as Anticancer Agent: A Mechanistic Approach [DOI]
  8. 8 Aksenov, 2015, Activity of 2-Aryl-2-(3-Indolyl)Acetohydroxamates against Drug-Resistant Cancer Cells [DOI]
  9. 9 Segat, 2020, A new series of acetohydroxamates shows in vitro and in vivo anticancer activity against melanoma [DOI]
  10. 10 Aksenov, D.A., Aksenov, A.V., Prityko, L.A., Aksenov, N.A., Frolova, L.V., and Rubin, M. (2021). Methylation of 2-Aryl-2-(3-Indolyl)Acetohydroxamic Acids and Evaluation of Cytotoxic Activity of the Products. Molbank, 2022. [DOI]
  11. 11 Lima, 2019, Homologation: A Versatile Molecular Modification Strategy to Drug Discovery [DOI]
  12. 12 Mosmann, 1983, Rapid colorimetric assay for cellular growth and survival: Application to proliferation and cytotoxicity assays [DOI]

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