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Preparation of Primary Acute Lymphoblastic Leukemia Cells in Different Cell Cycle Phases by Centrifugal Elutriation
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Synthetic 1,2,4-triazole-3-carboxamides Induce Cell Cycle Arrest and Apoptosis in Leukemia Cells

Zhidkova Ekaterina1, Stepanycheva Daria2, Grebenkina Lyubov2

  • 1Department of Chemical Carcinogenesis, N.N. Blokhin Russian Cancer Research Center, Ministry of Health of Russia, 24 Kashirskoe Shosse, Moscow 115478, Russia.

Current Pharmaceutical Design
|December 12, 2023
PubMed
Abstract

Insights

New ribavirin analogues, 1,2,4-triazole-3-carboxamide derivatives, show significant antiproliferative effects against leukemia cells. These compounds may offer a promising alternative for cancer therapy with fewer side effects.

Area of Science:

  • Medicinal Chemistry
  • Cancer Biology
  • Pharmacology

Background:

  • Ribavirin demonstrates anticancer efficacy in preclinical models but causes significant side effects.
  • There is a need for novel ribavirin analogues with improved therapeutic indices.

Purpose of the Study:

  • To synthesize and evaluate the antiproliferative activity of 1,2,4-triazole-3-carboxamide derivatives against leukemia cells.
  • To investigate the mechanism of action, including cell cycle arrest and apoptosis induction.

Main Methods:

  • Synthesis of four 1,2,4-triazole-3-carboxamide derivatives.
  • In vitro antiproliferative assays using K562 and CCRF-SB leukemia cell lines and healthy volunteer monocytes.
  • Cell cycle analysis and apoptosis assessment via flow cytometry and Western blotting.

Main Results:

  • Two derivatives, 5-(tetrahydropyran-2-yl)-1,2,4-triazole-3-carboxamide and 1-(tetrahydropyran-2-yl)-1,2,4-triazol-3-carboxamide, exhibited significant antiproliferative effects on leukemia cells.
  • These effects were more pronounced in leukemia cells compared to non-transformed monocytes.

Conclusions:

  • 1,2,4-triazole-3-carboxamide derivatives demonstrate potent antiproliferative activity against leukemia cells.
  • The compounds induce cell cycle arrest, suggesting their potential as antimetabolites for anticancer therapy.
Keywords:
124-triazole-3-carboxamidesacute lymphoblastic leukemiacancer treatmentchronic myeloid leukemiarepurposing.ribavirin

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