Department of Pharmaceutical Chemistry, Delhi Institute of Pharmaceutical Sciences and Research, Mehrauli-Badarpur Road, Sector 3, Pushp Vihar, New Delhi, Delhi 110017, India.
Laboratory Services, Botswana Medicines Regulatory Authority, Gaborone, Botswana, South Africa.
Anticancer Agents Med Chem. 2022;22(10):1883-1896. doi: 10.2174/1871520621666210903130152.
Breast cancer (BC) is one of the most frequent malignancies and the most common reasons for impermanence in women. The backbone of therapy for BC is principally chemotherapy, but its non-specific nature to differentiate between normal cells and cancer cells and severe side effects are the main barriers in its use. So, there is an intense requirement to enlarge more efficacious, more specific and safer anti-BC agents.
Isatin (IST) is an endogenous molecule that is a principal class of heterocyclic compounds and exhibits a wide range of therapeutic activities which can be used as a starting material for the synthesis of several drug molecules. Many kinds of literature were reported previously on different pharmacological activities of IST derivatives and particularly on anticancer activity but this review mainly focuses on anti-BC activities of IST derivatives through MCF-7, MDA MB 231, MDA-MB 435 and MDA-MB 468 cell lines. Herein we mentioned; a total of 33 IST derivatives (compound 24- 56) which show good anti-BC activity. IST-derived compounds are also available in the market and are used for various cancer types like sunitinib for renal cell carcinoma (RCC) and Nintedanib for the cryptogenic fibrosing alveolitis treatment, but when evaluated for BC, they did not prove to be much successful.
This review mainly highlights anti-BC activities of various IST analogues using MCF-7, MDA MB 231, MDA-MB 435 and MDA-MB 468 cell lines, displaying the potent compound of the series and structure-activity relationships of compounds with molecular docking also. So, this study mainly shows the importance of IST as a major source for drug design and development of newer anti-BC drugs.
乳腺癌(BC)是最常见的恶性肿瘤之一,也是女性丧失生命的最常见原因。BC 的治疗基础主要是化疗,但它对正常细胞和癌细胞的区分缺乏特异性,且副作用严重,这成为了其应用的主要障碍。因此,迫切需要开发更有效、更特异和更安全的抗乳腺癌药物。
靛红(IST)是一种内源性分子,属于杂环化合物的主要类别,具有广泛的治疗活性,可用作合成多种药物分子的起始原料。先前有许多文献报道了 IST 衍生物的不同药理活性,特别是抗癌活性,但本综述主要关注 IST 衍生物通过 MCF-7、MDA MB 231、MDA-MB 435 和 MDA-MB 468 细胞系的抗乳腺癌活性。在此,我们提到了;共 33 种 IST 衍生物(化合物 24-56)表现出良好的抗乳腺癌活性。IST 衍生化合物也可在市场上用于各种癌症类型,如舒尼替尼治疗肾细胞癌(RCC)和尼达尼布治疗特发性肺纤维化,但在评估乳腺癌时,它们的效果并不明显。
本综述主要强调了各种 IST 类似物通过 MCF-7、MDA MB 231、MDA-MB 435 和 MDA-MB 468 细胞系的抗乳腺癌活性,展示了该系列的有效化合物以及化合物的构效关系和分子对接。因此,这项研究主要表明 IST 作为药物设计和开发新型抗乳腺癌药物的主要来源的重要性。