Design, synthesis and biological evaluation of a 4,6-di(aziridin-1-yl)-1,3,5-triazine–benzimidazole hybrid as a potential dual-targeting anticancer agent

AIMS: This study aimed to develop a novel aziridine-1,3,5-triazine derivative combining DNA-alkylating aziridine rings with a benzimidazole-containing fragment associated with PARP-related chemotypes. MATERIALS AND METHODS: in A549 and HCT-116 xenografts in immunodeficient BALB/c Nude mice. RESULTS: < 0.05) and demonstrated dose-dependent activity in HCT-116 xenografts (up to 82.9% TGI at 6 mg/kg, i.v.).

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Publication Details

Journal
Future Medicinal Chemistry
Published
2026-04-22
DOI
https://doi.org/10.1080/17568919.2026.2658014
Primary Topic
Synthesis and Characterization of Heterocyclic Compounds
Type
article
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article

Design, synthesis and biological evaluation of a 4,6-di(aziridin-1-yl)-1,3,5-triazine–benzimidazole hybrid as a potential dual-targeting anticancer agent

Ilya V. Kornyakov, Ivan S. Chernov, Olga V. Mikolaichuk, Natalia V. Petukhova et al.
Future Medicinal Chemistry
Synthesis and Characterization of Heterocyclic Compounds
article

Design, synthesis and biological evaluation of a 4,6-di(aziridin-1-yl)-1,3,5-triazine–benzimidazole hybrid as a potential dual-targeting anticancer agent

Ilya V. Kornyakov, Ivan S. Chernov, Olga V. Mikolaichuk, Natalia V. Petukhova, Vadim S. Pokrovsky, Vladimir V. Sharoyko, Olga S. Shemchuk, A. V. Protas, Gulalek Babayeva, Vyacheslav E. Bulakov, Pavel K Kozhukhov, Konstantin N. Semenov, Valeria M. Tretiakova
article en

Abstract

AIMS: This study aimed to develop a novel aziridine-1,3,5-triazine derivative combining DNA-alkylating aziridine rings with a benzimidazole-containing fragment associated with PARP-related chemotypes. MATERIALS AND METHODS: in A549 and HCT-116 xenografts in immunodeficient BALB/c Nude mice. RESULTS: < 0.05) and demonstrated dose-dependent activity in HCT-116 xenografts (up to 82.9% TGI at 6 mg/kg, i.v.).

Future Medicinal ChemistryVol. 18(10)
Peoples' Friendship University of Russia (RU), Russian Academy of Sciences (RU), St Petersburg University (RU), First Pavlov State Medical University of St. Petersburg (RU), Togliatti State University (RU), Russian Cancer Research Center NN Blokhin (RU), Russian Scientific Center of Radiology and Surgical Technologies (RU), Czech Academy of Sciences, Institute of Experimental Medicine (CZ)
Good health and well-being
Openalex Percentile: Top 22%
Synthesis and Characterization of Heterocyclic Compounds
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