Preliminary in vitro evaluation of anti-leukemic and antimalarial activities of pyrrolo[1,2-a]quinoxaline-carboxylic acid hydrazone derivatives.
Abstract
New pyrrolo[1,2-a]quinoxaline-2-carboxylic acid hydrazone derivatives were synthesized from nitroaniline using a multi-step pathway. Structure characterization of these novel substituted pyrrolo[1,2-a]quinoxaline-carboxylic acid hydrazones was achieved by using FT-IR, 1H NMR, 13C NMR, X-Ray and HRMS spectral analysis. These pyrroloquinoxaline hydrazone compounds were then evaluated in vitro for their potential on the human acute myeloid leukemia cell line MV4-11, in which (N'-pyridin-2-ylmethylene)pyrrolo[1,2-a]quinoxaline-2-carboxylic acid hydrazone 1a showed an IC50 value of 15.51 µM. Given the structural similarities between our hydrazone derivatives 1 and some recently published quinoline-type hydrazone compounds for antimalarial use, our compounds were also evaluated for their antimalarial activity. Among them, compound 1c demonstrated promising antiplasmodial activity, with an IC50 of 0.02 μM against the 3D7 strain of Plasmodium falciparum, exhibiting a selectivity index (SI) exceeding 5000 against this strain. Against the chloroquine-resistant Plasmodium falciparum W2 strain, hydrazone 1e emerged as the most potent and promising antimalarial candidate (IC50 = 0.03 mM), demonstrating a cytotoxicity to-antiprotozoal activity ratio exceeding 3333.
Related
- Synthesis of a Series of Heterocyclic N-Substituted Derivatives of Alendronic Acid and Their Preliminary Biological Evaluation.
- Antileishmanial and Antimalarial Activities of Synthetic Marine Endoperoxides
- Scaffold-Controlled Evaluation of Molecular Representations for Antimalarial Activity Prediction
- Chemical Synthesis and Immunological Evaluation of Archaeal Rare Sugar L-TalNAcA and Its Derivatives
- Design, Synthesis, and Evaluation of Novel Cephalotaxine-Cinnamic Acid Derivatives Against Hepatocellular Carcinoma
BibTeX
@article{gullion2026preliminary,
title = {{Preliminary in vitro evaluation of anti-leukemic and antimalarial activities of pyrrolo[1,2-a]quinoxaline-carboxylic acid hydrazone derivatives.}},
author = {Jean Gullion and Noël Pinaud and Lindita Lari and Luisa Ronga and Patrice Agnamey and Céline Damiani and Solène Savrimoutou and Elise Si Ahmed Charrier and Tshering Zangmo and Stéphane Moreau and Mathieu Marchivie and Sandra Albenque and Vanessa Desplat and Pascal Sonnet},
journal = {Acta Chimica Slovenica},
year = {2026},
month = oct,
doi = {10.17344/acsi.2026.9975},
url = {https://u-picardie.hal.science/hal-05786533v1},
note = {CC BY-SA 4.0},
}
RIS
TY - JOUR
TI - Preliminary in vitro evaluation of anti-leukemic and antimalarial activities of pyrrolo[1,2-a]quinoxaline-carboxylic acid hydrazone derivatives.
AU - Jean Gullion
AU - Noël Pinaud
AU - Lindita Lari
AU - Luisa Ronga
AU - Patrice Agnamey
AU - Céline Damiani
AU - Solène Savrimoutou
AU - Elise Si Ahmed Charrier
AU - Tshering Zangmo
AU - Stéphane Moreau
AU - Mathieu Marchivie
AU - Sandra Albenque
AU - Vanessa Desplat
AU - Pascal Sonnet
PY - 2026
DA - 2026/10/08
JO - Acta Chimica Slovenica
DO - 10.17344/acsi.2026.9975
UR - https://u-picardie.hal.science/hal-05786533v1
AB - New pyrrolo[1,2-a]quinoxaline-2-carboxylic acid hydrazone derivatives were synthesized from nitroaniline using a multi-step pathway. Structure characterization of these novel substituted pyrrolo[1,2-a]quinoxaline-carboxylic acid hydrazones was achieved by using FT-IR, 1H NMR, 13C NMR, X-Ray and HRMS spectral analysis. These pyrroloquinoxaline hydrazone compounds were then evaluated in vitro for their potential on the human acute myeloid leukemia cell line MV4-11, in which (N'-pyridin-2-ylmethylene)pyrrolo[1,2-a]quinoxaline-2-carboxylic acid hydrazone 1a showed an IC50 value of 15.51 µM. Given the structural similarities between our hydrazone derivatives 1 and some recently published quinoline-type hydrazone compounds for antimalarial use, our compounds were also evaluated for their antimalarial activity. Among them, compound 1c demonstrated promising antiplasmodial activity, with an IC50 of 0.02 μM against the 3D7 strain of Plasmodium falciparum, exhibiting a selectivity index (SI) exceeding 5000 against this strain. Against the chloroquine-resistant Plasmodium falciparum W2 strain, hydrazone 1e emerged as the most potent and promising antimalarial candidate (IC50 = 0.03 mM), demonstrating a cytotoxicity to-antiprotozoal activity ratio exceeding 3333.
SN - 1318-0207
SN - 1580-3155
ER -