Discovery of new non-symmetrical heterocyclic pentanoid derivatives targeting metastatic triple-negative breast cancer
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 effect...
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| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | en |
| Published: |
Elsevier
2025
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| Online Access: | http://psasir.upm.edu.my/id/eprint/120323/1/120323.pdf http://psasir.upm.edu.my/id/eprint/120323/ https://linkinghub.elsevier.com/retrieve/pii/S0960894X25001416 |
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| Summary: | 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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