Discovery of new non-symmetrical heterocyclic pentanoid derivatives targeting metastatic triple-negative breast cancer

Citation

Khor, Poh Yen and Stanslas, Johnson and Rasol, Nurulfazlina Edayah and Chan, Kok Meng and Mock, Phooi Yan and Lam, Kok Wai (2025) Discovery of new non-symmetrical heterocyclic pentanoid derivatives targeting metastatic triple-negative breast cancer. Bioorganic and Medicinal Chemistry Letters, 123. art. no. 130232. pp. 1-7. ISSN 0960-894X; eISSN: 1464-3405

Abstract

This study describes the synthesis and structure-activity relationship (SAR) analysis of non- symmetrical heterocyclic pentanoid derivative as potential anti-cancer agents. The lead compound, 5d, exhibited potent (IC50 = 0.38 ± 0.05 μM) and selective (Selectivity Index: 2–9) growth inhibitory effects on the metastatic triple-negative breast cancer (TNBC) cells. Mechanistic studies revealed that 5d attenuates proteasomal degradation activity via the ubiquitin-proteasome pathway, leading to G2/M phase cell cycle arrest and the induction of apoptotic cell death.

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Additional Metadata

Item Type:	Article
Subject:	Biochemistry
Subject:	Molecular Medicine
Divisions:	Faculty of Medicine and Health Science
DOI Number:	https://doi.org/10.1016/j.bmcl.2025.130232
Publisher:	Elsevier
Keywords:	Anti-cancer; Proteasome; Ubiquitinated proteasome pathway
Depositing User:	Ms. Nur Faseha Mohd Kadim
Date Deposited:	20 Feb 2026 01:28
Last Modified:	20 Feb 2026 01:28
Altmetrics:	http://www.altmetric.com/details.php?domain=psasir.upm.edu.my&doi=10.1016/j.bmcl.2025.130232
URI:	http://psasir.upm.edu.my/id/eprint/122602
Statistic Details:	View Download Statistic

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