Preliminary in vitro evaluation of anti-leukemic and antimalarial activities of pyrrolo[1,2-a]quinoxalinecarboxylic acid hydrazone derivatives
Year: 2026
Type: article
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.
Source: Acta chimica slovenica
Institutions: Centre National de la Recherche Scientifique, Université de Bordeaux, Institut des Sciences Moléculaires, Institut Polytechnique de Bordeaux, Inserm, Acides nucléiques: Régulations naturelles et artificielles, BoRdeaux Institute of onCology, Université de Pau et des Pays de l'Adour, Institut des Sciences Analytiques et de Physico-Chimie pour l'Environnement et les Matériaux, Agents infectieux, résistance et chimiothérapie, Université de Picardie Jules Verne, Institut de Chimie de la Matière Condensée de Bordeaux
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: diamond
OpenAlex ID: W7212419623