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Over the last several years, benzimidazole\u2010based compounds have received much scientific attention because of their wide range of biological activities. The current study offers a detailed discussion of the more recent developments in benzimidazole derivatives for the management of breast cancer with a particular focus on their structure\u2010activity relationships (SAR), molecular pathobiology, and therapeutic consequences. Recent studies between 2019 and 2025 have shown that benzimidazole derivatives are able to effectively react with a number of key molecular targets, including peptidyl\u2010prolyl cis\u2010trans isomerase NIMA\u2010interacting 1 (Pin1), epidermal growth factor receptor (EGFR), B\u2010cell lymphoma 2 (Bcl\u20102), vascular endothelial growth factor receptor (VEGFR\u20102), topoisomerases, tubulin, and histone deacetylases. In such interactions, the compounds trigger apoptosis, cell\u2010cycle arrest, autophagy, and the generation of oxidative stress in malignant cells\u2010and usually exhibit minimal toxicity to normal tissues. The present work summarizes recent information about benzimidazole pharmacophores \u2010, including their pharmacological targets, SAR, and mechanisms of action, and defines future directions for the development of selective, potent, and clinically viable benzimidazole\u2010based compounds for the treatment of breast cancer.<\/jats:p>","DOI":"10.1002\/cbdv.71329","type":"journal-article","created":{"date-parts":[[2026,5,13]],"date-time":"2026-05-13T18:09:21Z","timestamp":1778695761000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["From Scaffold to Therapy: Benzimidazole Pharmacophore Evolution in Breast Cancer Research"],"prefix":"10.1002","volume":"23","author":[{"given":"Appramdeep","family":"Kaur","sequence":"first","affiliation":[{"name":"School of Pharmaceutical Sciences Lovely Professional University  Phagwara Punjab India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7337-3575","authenticated-orcid":false,"given":"Gurvinder","family":"Singh","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Sciences Lovely Professional University  Phagwara Punjab India"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2026,5,13]]},"reference":[{"key":"e_1_2_11_2_1","doi-asserted-by":"publisher","DOI":"10.3322\/caac.21442"},{"key":"e_1_2_11_3_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41572\u2010019\u20100111\u20102"},{"key":"e_1_2_11_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.apsb.2022.09.010"},{"key":"e_1_2_11_5_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules27165245"},{"key":"e_1_2_11_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2014.01.030"},{"key":"e_1_2_11_7_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmc.2012.09.013"},{"key":"e_1_2_11_8_1","doi-asserted-by":"publisher","DOI":"10.1007\/s00044\u2010013\u20100476\u20109"},{"key":"e_1_2_11_9_1","doi-asserted-by":"publisher","DOI":"10.1186\/s13065\u2010019\u20100625\u20104"},{"key":"e_1_2_11_10_1","doi-asserted-by":"publisher","DOI":"10.1111\/cbdd.12462"},{"key":"e_1_2_11_11_1","doi-asserted-by":"publisher","DOI":"10.1002\/med.21290"},{"key":"e_1_2_11_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2014.11.053"},{"key":"e_1_2_11_13_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.rechem.2023.101013"},{"key":"e_1_2_11_14_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2012.04.027"},{"key":"e_1_2_11_15_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2010.07.023"},{"key":"e_1_2_11_16_1","doi-asserted-by":"crossref","unstructured":"R. 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