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2000
Volume 21, Issue 5
  • ISSN: 1573-4072
  • E-ISSN: 1875-6646

Abstract

Background

Although several specialized methods for treating various cancers have been developed, clinical outcomes for patients with colon cancer have shown unfavorable effects in addition to chemotherapeutic drug resistance. Therefore, finding medicinal substances with minimal to no side effects is crucial in the fight against cancer. Further, this study underscores the significance of 2-phenylindolizine acetamide due to the diverse biological features and the extensive application of this moiety as an effective anticancer and antibacterial drug.

Objective

The goal of the study was to investigate novel, prospective 2-phenylindolizines as anticancer and antibacterial drugs.

Methods

The synthesized compounds were characterized by different spectral analyses like 1H NMR, 13C NMR, IR, and mass spectrometry. Pharmacokinetics studies were performed to predict the drug performance in the body using the SwissADME kit. The molecular docking was performed to check the catalytic binding site between the Topoisomerase-IV from and synthesized compounds. The antibacterial activity was assessed using the agar well diffusion method, and the compounds were screened for anticancer activity using an MTT assay with doxorubicin as a reference.

Results

Interestingly, 2-phenylindolizine scaffolds , and revealed a remarkable antibacterial activity against relevant organisms and . The target compounds and showed excellent anticancer activity against Colo-205 and MDA-MB-231 cell lines with IC values of 68.62, 62.91, 54.23, and 46.34 µM, respectively. Compounds , and exhibited the highest hydrogen bonding amino acid interactions Asp83 (2.23 Å), Asp83 (2.08 Å), His74 (2.05 Å), His76 (1.71 Å), and Ser80 (1.05 Å) with active site of Topoisomerase-IV from (4KPE).

Conclusion

This research focused on recent advances in drug design and development, as well as Phenylindolizine derivatives and how they work on anticancer and antibacterial sites of action.

© 2025 Bentham Science Publishers
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2025-09-28

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Synthesis and In-silico Docking Analysis of 2-Phenylindolizine Acetamide Scaffolds: Potent Anticancer and Antibacterial Targets
Curr. Bioact. Compd. 21, E250624231305 (2025); https://doi.org/10.2174/0115734072301391240604062819
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Supplements

The general procedure for the biological activity evaluation and computational docking studies of all the synthesized compounds, as well as copies of 1H NMR and 13C NMR, are included in supporting information. Supplementary material is available on the publisher’s website along with the published article.

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  • Article Type:     Research Article
Keyword(s): 4KPE; antibacterial activity; anticancer activity; molecular modeling; Phenylindolizine; SwissADME

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