Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, P. R. China.
ChemistryOpen. 2023 Feb;12(2):e202200235. doi: 10.1002/open.202200235.
In recent years, the incidence of cancer is high around the world, and the resistance of bacteria is increasing. To cope with the potentially adverse side effects of cancer chemotherapy and surgery, researchers are turning to the construction of new drug scaffolds. The indoline structure exists in a huge number of natural products, but drugs with indoline have only been formally studied in recent years. With the deepening of research, drugs containing indoline have played important roles in more disease treatment aspects, such as anti-tumor, anti-bacterial, anti-inflammatory and have been used as analgesics, to treat cardiovascular diseases and so on. The synthesis and pharmacological activity of indoline derivatives is summarized in this review in order to support the addition of the indoline component to the toolbox of medicinal chemists. This review focuses on the advantages of indoline compounds in development and synthesis of and for the use as anticancer drugs, antibacterial drugs, to treat cardiovascular diseases and as anti-inflammatory and analgesic drugs. Indoline structures are commonly found in natural and synthetic compounds with medicinal value and are now beginning to be exploited as the basic backbone of various drugs. As research continues, dihydroindoles and their derivatives will play a greater role in the medical field.
近年来，癌症在全球的发病率居高不下，细菌的耐药性也在不断增加。为了应对癌症化疗和手术可能产生的不良反应，研究人员开始转向构建新的药物支架。吲哚啉结构存在于大量的天然产物中，但近年来才对含有吲哚啉的药物进行了正式研究。随着研究的深入，含有吲哚啉的药物在更多疾病治疗方面发挥了重要作用，如抗肿瘤、抗菌、抗炎，并已被用作镇痛药，用于治疗心血管疾病等。本文综述了吲哚啉衍生物的合成和药理学活性，以期为药物化学家提供更多的工具，支持将吲哚啉作为药物化学的组成部分。本文重点介绍了吲哚啉化合物在抗癌药物、抗菌药物、心血管疾病治疗药物和抗炎、镇痛药物开发和应用方面的优势。吲哚啉结构在具有药用价值的天然和合成化合物中很常见，现在开始被用作各种药物的基本骨架。随着研究的继续，二氢吲哚及其衍生物将在医学领域发挥更大的作用。
