A review on recent developments of indole-containing antiviral agents

Abstract

Indole represents one of the most important privileged scaffolds in drug discovery. Indole derivatives have the unique property of mimicking the structure of peptides and to bind reversibly to enzymes, which provide tremendous opportunities to discover novel drugs with different modes of action. There are seven indole-containing commercial drugs in the Top-200 Best Selling Drugs by US Retail Sales in 2012. There are also an amazing number of approved indole-containing drugs in the market as well as compounds currently going through different clinical phases or registration statuses. This review focused on the recent development of indole derivatives as antiviral agents with the following objectives: 1) To present one of the most comprehensive listings of indole antiviral agents, drugs on market or compounds in clinical trials; 2) To focus on recent developments of indole compounds (including natural products) and their antiviral activities, summarize the structure property, hoping to inspire new and even more creative approaches; 3) To offer perspectives on how indole scaffolds as a privileged structure might be exploited in the future.

Some new indole–coumarin hybrids; Synthesis, anticancer and Bcl-2 docking studies

“…Amidst them, heterocycles with polycyclic ring system possess distinct rigid geometry displaying high functional specialization by orienting its substituents in three dimensional spaces, there by attracting great interest [2]. Indole is a bicyclic heterocyclic scaffold that find applications in medical therapy due to a variety of valuable biologic activities such as antiviral [3,4], antiinflammatory [5,6], anti-hyperlipidemic, antihypoglycemic, anti-hypertensive, anti-asthmatic, anti HIV [7], antidepressant [8] and notably anticancer [9][10][11][12][13][14][15] activity. Few marketed anticancer indole derivatives are vincristine, vinblastine, vinorelbine, vindesine, mitraphylline, cediranib and apaziquone [2].…”

Preparation of symmetrical C2-C2-linked bis- and tris-6-bromoindoles by Sonogashira couplings and 5-endo-dig cyclization induced by nBu4NF

“…From previous work in our laboratory, it was found that double Sonogashira coupling of related arenes with aryldialkynes worked well using Pd 2 (dba) 3 , CuI, PPh 3 in DMSO as solvent. 16 Thus, a model set of aryldialkynes 3a-c and alkyldialkynes 3d-i were prepared (See supporting information) and their regioselective Sonogashira coupling with 2 proceeded uneventfully to give the corresponding products 4a-i.…”

Synthesis and crystal structure of (E)-3-(2-methyl-1H-indol-3-yl)-1-(4-methylphenyl)propenone

“…Recently, a number of indole-containing compounds have revealed remarkable pharmacological activity and their utility as therapeutic agents has attracted considerable attention from chemists 1,2 . Libraries based on the indole scaffold have been developed to address the need for novel drugs with increased potency 3,4 .…”