Journal ArticleDOI
Biological importance of the indole nucleus in recent years: A comprehensive review
TLDR
Indole has a benzene ring and pyrrole ring sharing one double bond and is a heterocyclic system with 10 electrons from four double bonds and the lone pair from the nitrogen atom as mentioned in this paper.About:
This article is published in Journal of Heterocyclic Chemistry.The article was published on 2010-05-01. It has received 385 citations till now. The article focuses on the topics: Indole test & Ring (chemistry).read more
Citations
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Indoles - A promising scaffold for drug development.
T.V. Sravanthi,S. L. Manju +1 more
TL;DR: A clear knowledge is provided on the wide-ranging biological activities of 2-arylindoles over the past two decades, which would be beneficial for the designing of more potent drug targets in order to compete with the existing drugs.
Journal ArticleDOI
Beyond C2 and C3: Transition-Metal-Catalyzed C–H Functionalization of Indole
TL;DR: This review focuses on the contributions made in benzenoid C–H functionalization of indoles and other related heteroaromatics such as carbazoles.
Journal ArticleDOI
Medicinal chemistry of indole derivatives: Current to future therapeutic prospectives.
Archana Kumari,Rajesh K. Singh +1 more
TL;DR: This review summarizes some of the recent effective chemical synthesis (2014-2018) for indole ring and emphasized on the structure-activity relationship (SAR) to reveal the active pharmacophores of various indole analogues accountable for anticancer, anticonvulsant, antimicrobial, antitubercular, antimalarial, antiviral, antidiabetic and other miscellaneous activities which have been investigated in the last five years.
Journal ArticleDOI
Indole in the target-based design of anticancer agents: A versatile scaffold with diverse mechanisms.
Sakineh Dadashpour,Saeed Emami +1 more
TL;DR: The present article aims to review the current application of indole core in the design of new anticancer agents that may act via various targets such as histone deacetylases, sirtuins, PIM kinases, DNA topoisomerases and σ receptors.
Journal ArticleDOI
Recent progress in transition-metal-catalyzed enantioselective indole functionalizations.
Jing-Biao Chen,Yi-Xia Jia +1 more
TL;DR: This review summarizes the major achievements in the transition-metal-catalyzed enantioselective indole functionalization reactions since 2010 and focuses on C-C bond formation processes, including alkylations, arylations, cycloaddition reactions, and other reactions.
References
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Journal ArticleDOI
Inhibition of Cytosolic Phospholipase A2α: Hit to Lead Optimization
John C. McKew,Megan A. Foley,Paresh Thakker,Mark L. Behnke,Frank Lovering,Fuk-Wah Sum,Tam Steve Yik-Kai,Kun Wu,Marina W.H. Shen,Wen Zhang,Mario D. Gonzalez,Shanghao Liu,Anu Mahadevan,Howard Sard,Soo Peang Khor,James D. Clark +15 more
TL;DR: In this article, an electrophilic ketone was inserted between the indole and benzoic acid moieties, and the distance between the two moieties gave a compound with activity in the GLU (7-hydroxycoumarinyl-γ-linolenate) micelle assay, which contains lipid and detergent.
Journal ArticleDOI
Indol-1-yl Acetic Acids as Peroxisome Proliferator-Activated Receptor Agonists: Design, Synthesis, Structural Biology, and Molecular Docking Studies
Neeraj Mahindroo,Chiung-Chiu Wang,Chun-Chen Liao,Chien-Fu Huang,I-Lin Lu,Tzu-Wen Lien,Yi-Huei Peng,Wei-Jan Huang,Ying-Ting Lin,Ming-Chen Hsu,Chia Hui Lin,Chia-Hua Tsai,John T.A. Hsu,Xin Chen,Ping-Chiang Lyu,Yu-Sheng Chao,Su-Ying Wu,Hsing Pang Hsieh +17 more
TL;DR: The structural biology and molecular docking studies revealed that the distances between the acidic group and the linker, when a ligand was complexed with PPARgamma protein, were important for the potent activity of 10k.
Journal ArticleDOI
The potential insulin sensitizing and glucose lowering effects of a novel indole derivative in vitro and in vivo.
Ying-Yin Li,Hao-Shu Wu,Lei Tang,Chu-Rui Feng,Juanhong Yu,Yu Li,Yushe Yang,Bo Yang,Qiao-jun He +8 more
TL;DR: GY3 could improve insulin resistance and lower glucose level, GY3 and its derivatives might be developed as a substitution therapy for diseases with insulin resistance.
Journal ArticleDOI
Synthesis of new heteroaryl and heteroannulated indoles from dehydrophenylalanines: Antitumor evaluation.
Maria João R. P. Queiroz,Ana S. Abreu,M. Solange D. Carvalho,Paula M. T. Ferreira,Nair Nazareth,M. São-José Nascimento +5 more
TL;DR: Three cyclized compounds were evaluated for their capacity to inhibit the in vitro growth of three human tumor cell lines, MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer), and SF-268 (CNS cancer).
Journal ArticleDOI
New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists.
Page Daniel,Hua Yang,William Brown,Christopher Walpole,Manon Fleurent,Meredith Fyfe,François Gaudreault,Stephane St-Onge +7 more
TL;DR: The preparation and evaluation of a novel class of CB2 agonists based on a 1,2,3,4-tetrahydropyrrolo[3, 4-b]indole moiety are reported, which showed moderate to good selectivity over the CB1 receptor.