Mounika S, K Hemalatha, Pal Rohit, Matada Gurubasavaraja Swamy Purawarga, Jain Pradan P, E Haripriya, Sk Md Ashadul, M P Viji
Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru 560107, Karnataka, India.
Department of Pharmaceutical Chemistry, M S Ramaiah University of Applied Sciences, Bangalore, 560058, Karnataka, India.
Curr Top Med Chem. 2025 Jan 7. doi: 10.2174/0115680266336395241115092048.
Despite ongoing advancements in drug design and developments, breast cancer remains a serious and devastating disease and is ranked as the second most common illness in women. Breast cancer rates have increased significantly during the last 40 years. This necessitates the development of novel treatment techniques. Currently, chemotherapy is the primary mode of treatment for breast cancer; however, its toxicity to normal cells and drug resistance are considered the main obstacles. Researchers are looking for novel anti-breast cancer medication classes to improve cancer therapy efficacy and survival rates. Using non-targeting medicines in a 'one-size-fits-all' strategy can harm healthy cells and may not be effective for all patients. Thus, now, the treatment of breast cancer is exploring targeted-based therapy. The tactics involved in this therapy may improve patient survival rates, but their extended usage can lead to significant side effects and medication resistance. Targeted therapy enables precision medicine by targeting particular oncogenic markers in malignancies. Because of their strong cytotoxicity against several cancer cell types, heterocyclic compounds play an important role in the development of therapeutically effective anticancer drugs. Benzimidazole derivatives have grown in favour of anti-breast cancer medicines in recent years due to their broad biological characteristics and therapeutic applications. This review provides healthcare professionals and researchers with an overview of current breakthroughs (2019-2024) in benzimidazole derivatives as breast cancer-targeted therapy, based on the perspectives of leading experts. We have illuminated the diverse and evolving landscape of hybridized benzimidazole, along with its biological targets and anti-breast cancer activity. Further, we also have compiled the various ongoing clinical trials of benzimidazole scaffolds as anti-breast cancer agents. A detailed illustration of the structure-activity connection with special emphasis is provided. The effort may help to develop potent, selective, and effective drugs to combat breast cancer.
尽管在药物设计和开发方面不断取得进展，但乳腺癌仍然是一种严重且具有毁灭性的疾病，在女性中排名第二常见。在过去40年中，乳腺癌发病率显著上升。这就需要开发新的治疗技术。目前，化疗是乳腺癌的主要治疗方式；然而，其对正常细胞的毒性和耐药性被认为是主要障碍。研究人员正在寻找新型抗乳腺癌药物类别，以提高癌症治疗效果和生存率。采用“一刀切”策略使用非靶向药物可能会损害健康细胞，而且对所有患者可能都无效。因此，目前乳腺癌治疗正在探索基于靶点的疗法。这种疗法所涉及的策略可能会提高患者生存率，但其长期使用可能会导致严重的副作用和药物耐药性。靶向治疗通过针对恶性肿瘤中的特定致癌标志物实现精准医疗。由于杂环化合物对多种癌细胞类型具有强大的细胞毒性，它们在开发治疗有效的抗癌药物中发挥着重要作用。近年来，苯并咪唑衍生物因其广泛的生物学特性和治疗应用，在抗乳腺癌药物方面越来越受青睐。本综述基于顶尖专家的观点，为医疗保健专业人员和研究人员提供了苯并咪唑衍生物作为乳腺癌靶向治疗的当前突破（2019 - 2024年）概述。我们阐述了杂化苯并咪唑的多样且不断演变的格局，以及其生物学靶点和抗乳腺癌活性。此外，我们还汇编了苯并咪唑支架作为抗乳腺癌药物的各种正在进行的临床试验。提供了对结构 - 活性关系的详细说明，并特别强调了这一点。这项工作可能有助于开发强效、选择性和有效的抗乳腺癌药物。
