Wati First Ambar, Santoso Mardi, Moussa Ziad, Fatmawati Sri, Fadlan Arif, Judeh Zaher M A
Department of Chemistry, Institut Teknologi Sepuluh Nopember Kampus ITS, Sukolilo Surabaya 60111 Indonesia.
Department of Chemistry, College of Science, United Arab Emirates University P. O. Box 15551 Al Ain United Arab Emirates.
RSC Adv. 2021 Jul 21;11(41):25381-25421. doi: 10.1039/d1ra03091d. eCollection 2021 Jul 19.
Heterocyclic nitrogen compounds are privileged structures with many applications in the pharmaceutical and nutraceutical industries since they possess wide bioactivities. Trisindolines are heterocyclic nitrogen compounds consisting of an isatin core bearing two indole moieties. Trisindolines have been synthesized by reacting isatins with indoles using various routes and the yield greatly depends on the catalyst used, reaction conditions, and the substituents on both the isatin and indole moieties. Amongst the synthetic routes, acid-catalyzed condensation reaction between isatins and indoles are the most useful due to high yield, wide scope and short reaction times. Trisindolines are biologically active compounds and show anticancer, antimicrobial, antitubercular, antifungal, anticonvulsant, spermicidal, and antioxidant activities, among others. Trisindolines have not previously been reviewed. Therefore, this review aims to provide a comprehensive account of trisindolines including their natural occurrence, routes of synthesis, and biological activities. It aims to inspire the discovery of lead trisindoline drug candidates for further development.
杂环氮化合物是具有特殊结构的化合物，由于其具有广泛的生物活性，在制药和营养保健品行业有许多应用。三吲哚啉是一种杂环氮化合物，由一个异吲哚酮核心和两个吲哚部分组成。三吲哚啉可通过多种途径使异吲哚酮与吲哚反应合成，其产率很大程度上取决于所用催化剂、反应条件以及异吲哚酮和吲哚部分上的取代基。在这些合成途径中，异吲哚酮与吲哚之间的酸催化缩合反应最为有用，因为其产率高、适用范围广且反应时间短。三吲哚啉是具有生物活性的化合物，具有抗癌、抗菌、抗结核、抗真菌、抗惊厥、杀精和抗氧化等活性。此前尚未对三吲哚啉进行过综述。因此，本综述旨在全面介绍三吲哚啉，包括它们的天然存在情况、合成途径和生物活性。其目的是激发发现先导性三吲哚啉候选药物以进行进一步开发。
