Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Shoolini University, Solan, Himachal Pradesh, 173 229, India.
Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Shoolini University, Solan, Himachal Pradesh, 173 229, India; Institute of Pharmaceutical Sciences, Faculty of Pharmacy, Parul University, Vadodara, Gujarat, 391760, India.
Eur J Med Chem. 2024 Dec 15;280:116896. doi: 10.1016/j.ejmech.2024.116896. Epub 2024 Sep 21.
Among all non-communicable diseases, cancer is ranked as the second most common cause of death and is rising constantly. While cancer treatments mainly include radiation therapy, chemotherapy, and surgery; chemotherapy is considered the most commonly employed and effective treatment. Most of the chemotherapeutic agents are azoles based compounds and imidazole is one such insightful azole. The anticancer properties of imidazole-based compounds have been thoroughly explored in recent years and all monosubstituted, disubstituted, trisubstituted, and tetrasubstituted imidazoles have been explored for their anticancer activities. Along with these compounds, other imidazole-based compounds like 1,3-dihydro-2H-imidazole-2-thiones, imidazolones, and poly imidazole compounds have also been explored for their anticancer activities. The activities of these compounds are heavily influenced by their structural resemblance to combretastatin 4A and ABI (2-aryl-4-benzoyl-imidazole). The lead compounds were highly active on breast, gastric, colon, ovarian, cervical, bone marrow, melanoma, prostate, lung, leukemic, neuroblastoma, liver, Ehrlich, melanoma, and pancreatic cancers. The targets of these leads like tubulin, heme oxygenases, VEGF, tyrosine kinases, EGFR, and others have also been explored. The exploration of the anticancer potential of substituted imidazole compounds is the main topic of this review including synthesis, SAR, and mechanism.
在所有非传染性疾病中，癌症是排名第二的主要死因，且其发病率还在不断上升。癌症的治疗方法主要包括放射疗法、化学疗法和手术；而化学疗法被认为是最常用和最有效的治疗方法。大多数化疗药物都是基于唑的化合物，咪唑就是这样一种有见地的唑。近年来，人们对基于咪唑的化合物的抗癌特性进行了深入研究，对所有的单取代、二取代、三取代和四取代咪唑都进行了抗癌活性研究。除了这些化合物，其他基于咪唑的化合物，如 1,3-二氢-2H-咪唑-2-硫酮、咪唑酮和聚咪唑化合物，也被用于研究其抗癌活性。这些化合物的活性受到其与 combretastatin 4A 和 ABI（2-芳基-4-苯甲酰基-咪唑）结构相似性的强烈影响。这些先导化合物对乳腺癌、胃癌、结肠癌、卵巢癌、宫颈癌、骨髓癌、黑色素瘤、前列腺癌、肺癌、白血病、神经母细胞瘤、肝癌、艾氏腹水瘤、黑色素瘤和胰腺癌都具有高度的活性。这些先导化合物的靶点，如微管蛋白、血红素加氧酶、VEGF、酪氨酸激酶、EGFR 等，也已经被探索过了。本综述的主题是取代咪唑化合物的抗癌潜力的探索，包括合成、SAR 和作用机制。
