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Indoles as Promising Scaffold for Drug Discovery: Synthesis, Bioactivities and Applications

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 June 2024) | Viewed by 1608

Special Issue Editor


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Guest Editor
Department of Chemistry, Fudan University, Shanghai, China
Interests: drug design; small-molecule drugs; methodologies for synthetic drugs
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Indole scaffolds represent one of the most promising heterocycles found in natural and synthetic sources and have been shown to possess various biological activities, including anti-inflammatory, antitubercular, antimalarial, anti-HIV, anticancer, antifungal, and antimicrobial activity, etc. New advances in synthetic methodologies that enable rapid access to a wide variety of indole derivatives are of critical importance to medicinal chemists as it can readily generate bulk quantities of desired compounds to discover new and effective pharmaceuticals among indole derivatives.

This Special Issue of Molecules will comprise original research articles and reviews in the field of indole chemistry considering drug design, new synthetic methodologies, process chemistry, and the biological activities of indole derivatives.

Dr. Qiuqin He
Guest Editor

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Keywords

  • indole derivatives
  • drug design
  • synthetic methodologies
  • process chemistry
  • biological activities

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Published Papers (1 paper)

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Research

7 pages, 1191 KiB  
Article
A Novel C3/C4-Fused Indole Scaffold through Acid-Catalyzed Cascade Reaction
by Felix Potlitz, Gottfried J. Palm, Anja Bodtke, Michael Lammers, Dennis Schade and Andreas Link
Molecules 2024, 29(13), 3064; https://doi.org/10.3390/molecules29133064 - 27 Jun 2024
Cited by 1 | Viewed by 1182
Abstract
3,4-bridged indoles are underrepresented among the vast number of indoles described in the literature. Attempts to access 3,4-macrocyclized indoles led to the unexpected formation of a novel tetracyclic indole through intramolecular acid-catalyzed ring contraction. The herein-established one-step synthetic route provides an excellent medicinal [...] Read more.
3,4-bridged indoles are underrepresented among the vast number of indoles described in the literature. Attempts to access 3,4-macrocyclized indoles led to the unexpected formation of a novel tetracyclic indole through intramolecular acid-catalyzed ring contraction. The herein-established one-step synthetic route provides an excellent medicinal chemistry platform for the construction of screening libraries covering a unique chemical space of indoles. Full article
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