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2000
Volume 32, Issue 31
  • ISSN: 0929-8673
  • E-ISSN: 1875-533X

Abstract

Introduction

This study aimed to present the synthesis and characterization of four novel analogs of cyclophosphamide () and their related precursors () and assess their anticancer activity against breast cancerous (MCF-7) and normal (HUVEC) cells.

Methods

Notably, 2-(bis(2-chloroethyl)amino)-1,3,2-diazaphospholidine 2-oxide () and 2-(bis(2-hydroxyethyl)amino)-1,3,2-diazaphospholidine 2-oxide () exhibited concentration-dependent cytotoxicity against the MCF-7 cell line, with IC values of 8.98 and 28.74 M, respectively.

Results

Annexin V/PI staining and ROS assays demonstrated reduced cell viability and mitochondrial dysfunction. studies involving DFT-D optimization and Molegro virtual docking against B-DNA dodecamer and STAT3 receptors revealed enhanced interactions for certain compounds compared to cyclophosphamide.

Conclusion

Importantly, the and results corroborated each other, supporting the potential anticancer efficacy of these novel analogs.

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Design, Synthesis, Docking Studies, and Biological Activity of Novel Analogs of Cyclophosphamide as Potential Anticancer Agents
Curr. Med. Chem. 32, 6825 (2025); https://doi.org/10.2174/0109298673332921240920065129
/content/journals/cmc/10.2174/0109298673332921240920065129
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  • Article Type:     Research Article
Keyword(s): anticancer; breast cancer; Cyclophosphamide; docking studies; MTT assay; ROS assay

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