DataSheet1_Comprehensive review of α-carboline alkaloids: Natural products, updated synthesis, and biological activities.docx

α-carboline (9H-pyrido[2,3-b]indole), contains a pyridine ring fused with an indole backbone, is a promising scaffold for medicinal chemistry. In recent decades, accumulating evidence shows that α-carboline natural products and their derivatives possess diverse bioactivities. However, hitherto, there is no comprehensive review to systematically summarize this important class of alkaloids. In this perspective, this paper represents the first review to provide a comprehensive description of α-carbolines including natural products, updated literature of synthesis, and their diverse biological activities. Their biological activities including antitumor, anti-microbial, anti-Alzheimer’s disease, anti-atherosclerosis, and antioxidant activities were hilighted. And the targets and the main structure activity relationships (SARs) will be presented. Finally, challenges and future directions of this class of compounds will be discussed. This review will be helpful in understanding and encouraging further exploration for this group of alkaloids.

α-咔啉（α-carboline，9H-吡啶并[2,3-b]吲哚）是吡啶环与吲哚母核稠合而成的杂环化合物，是药物化学领域颇具应用前景的骨架结构。近数十年来，越来越多的研究证据表明，天然α-咔啉类产物及其衍生物具备多样的生物活性。然而截至目前，尚无一篇综述能够系统总结这一类重要的生物碱。本综述作为该领域首篇全面综述，将系统阐述α-咔啉类化合物的相关研究，涵盖其天然产物来源、最新合成研究进展以及多样的生物活性。本文重点介绍了该类化合物的抗肿瘤、抗微生物、抗阿尔茨海默病、抗动脉粥样硬化与抗氧化等活性，同时将阐述其作用靶点及主要的构效关系（structure activity relationships, SARs）。最后，本文将探讨该类化合物目前面临的挑战与未来研究方向。本综述将有助于学界深入理解α-咔啉类生物碱，并推动该领域的进一步探索与研究。