scholarly journals Trending Topics on Coumarin and Its Derivatives in 2020

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 501
Author(s):  
Aitor Carneiro ◽  
Maria João Matos ◽  
Eugenio Uriarte ◽  
Lourdes Santana
Keyword(s):  
Drug Discovery ◽  
Fluorescent Probes ◽  
Chemical Biology ◽  
Physicochemical Characteristics ◽  
Research Articles ◽  
Research Papers ◽  
Naturally Occurring ◽  
Privileged Scaffold ◽  
Trending Topics ◽  
Source Of Information

Coumarins are naturally occurring molecules with a versatile range of activities. Their structural and physicochemical characteristics make them a privileged scaffold in medicinal chemistry and chemical biology. Many research articles and reviews compile information on this important family of compounds. In this overview, the most recent research papers and reviews from 2020 are organized and analyzed, and a discussion on these data is included. Multiple electronic databases were scanned, including SciFinder, Mendeley, and PubMed, the latter being the main source of information. Particular attention was paid to the potential of coumarins as an important scaffold in drug design, as well as fluorescent probes for decaging of prodrugs, metal detection, and diagnostic purposes. Herein we do an analysis of the trending topics related to coumarin and its derivatives in the broad field of drug discovery.

scholarly journals Steroid diversification by multicomponent reactions

2019 ◽  
Vol 15 ◽  
pp. 1236-1256 ◽  
Author(s):  
Leslie Reguera ◽  
Cecilia I Attorresi ◽  
Javier A Ramírez ◽  
Daniel G Rivera
Keyword(s):  
Amino Acids ◽  
Drug Discovery ◽  
Carboxylic Acid ◽  
Supramolecular Chemistry ◽  
Boronic Acid ◽  
Chemical Biology ◽  
Multicomponent Reactions ◽  
Naturally Occurring ◽  
Almost All ◽  
Structural Diversification

Reports on structural diversification of steroids by means of multicomponent reactions (MCRs) have significantly increased over the last decade. This review covers the most relevant strategies dealing with the use of steroidal substrates in MCRs, including the synthesis of steroidal heterocycles and macrocycles as well as the conjugation of steroids to amino acids, peptides and carbohydrates. We demonstrate that steroids are available with almost all types of MCR reactive functionalities, e.g., carbonyl, carboxylic acid, alkyne, amine, isocyanide, boronic acid, etc., and that steroids are suitable starting materials for relevant MCRs such as those based on imine and isocyanide. The focus is mainly posed on proving the amenability of MCRs for the diversity-oriented derivatization of naturally occurring steroids and the construction of complex steroid-based platforms for drug discovery, chemical biology and supramolecular chemistry applications.

scholarly journals Epigenetics: the first 25 centuries

2018 ◽  
Vol 373 (1748) ◽  
pp. 20170067 ◽  
Author(s):  
A. Ganesan
Keyword(s):  
Drug Discovery ◽  
Translational Research ◽  
Chemical Biology ◽  
Research Articles ◽  
Recent Advances ◽  
Natural Progression ◽  
Epigenetic Drug ◽  
History Of ◽  
Key Issues ◽  
Eukaryotic Organisms

Epigenetics is a natural progression of genetics as it aims to understand how genes and other heritable elements are regulated in eukaryotic organisms. The history of epigenetics is briefly reviewed, together with the key issues in the field today. This themed issue brings together a diverse collection of interdisciplinary reviews and research articles that showcase the tremendous recent advances in epigenetic chemical biology and translational research into epigenetic drug discovery. This article is part of a discussion meeting issue ‘Frontiers in epigenetic chemical biology’.

Experimental and Computational Approaches to Improve Binding Affinity in Chemical Biology and Drug Discovery

2020 ◽  
Vol 20 (19) ◽  
pp. 1651-1660
Author(s):  
Anuraj Nayarisseri
Keyword(s):  
Drug Discovery ◽  
Drug Design ◽  
Binding Affinity ◽  
Chemical Biology ◽  
De Novo ◽  
Structure Based Drug Design ◽  
Computational Approaches ◽  
Drug Designing ◽  
Traditional Drug ◽  
Computer Based

Drug discovery is one of the most complicated processes and establishment of a single drug may require multidisciplinary attempts to design efficient and commercially viable drugs. The main purpose of drug design is to identify a chemical compound or inhibitor that can bind to an active site of a specific cavity on a target protein. The traditional drug design methods involved various experimental based approaches including random screening of chemicals found in nature or can be synthesized directly in chemical laboratories. Except for the long cycle design and time, high cost is also the major issue of concern. Modernized computer-based algorithm including structure-based drug design has accelerated the drug design and discovery process adequately. Surprisingly from the past decade remarkable progress has been made concerned with all area of drug design and discovery. CADD (Computer Aided Drug Designing) based tools shorten the conventional cycle size and also generate chemically more stable and worthy compounds and hence reduce the drug discovery cost. This special edition of editorial comprises the combination of seven research and review articles set emphasis especially on the computational approaches along with the experimental approaches using a chemical synthesizing for the binding affinity in chemical biology and discovery as a salient used in de-novo drug designing. This set of articles exfoliates the role that systems biology and the evaluation of ligand affinity in drug design and discovery for the future.

scholarly journals Recent Advances in Kinase Drug Discovery Part I: The Editors’ Take

2021 ◽  
Vol 22 (14) ◽  
pp. 7560
Author(s):  
Julie A. Tucker ◽  
Mathew P. Martin
Keyword(s):  
Drug Discovery ◽  
Research Articles ◽  
Special Issue ◽  
Recent Advances ◽  
Enzyme Family ◽  
Selection Of

This special issue on Advances in Kinase Drug Discovery provides a selection of research articles and topical reviews covering all aspects of drug discovery targeting the phosphotransferase enzyme family [...]

Syntheses of Spiro(2-oxopyrrolidinyl)-5,4′-pyrazolones via Organocatalyzed Michael/Ammonolysis Cascade Reaction of 4-Aminopyrazolones and α,β-Unsaturated Acyl Phosphates

Synlett ◽  
2021 ◽  
Author(s):  
Lin Chen ◽  
You-Fen Li ◽  
Zheng-Jun Chen ◽  
Wen-Ya Jiao ◽  
Zhi-Jiao Chen
Keyword(s):  
Drug Discovery ◽  
Chemical Biology ◽  
Cascade Reaction ◽  
Unsaturated Acyl

AbstractThe efficient organocatalyzed Michael/ammonolysis cascade reaction of N-protected 4-aminopyrazolones and α,β-unsaturated acyl phosphates has been developed. This tactic gives rise to architecturally multifarious spiro(2-oxopyrrolidinyl)-5,4′-pyrazolones in good productiveness (up to 88% yield) and with moderate to good diastereoselectivities (up to 20:1 dr). These novel hybrid heterocycles would be promising candidates for drug-discovery programs and chemical biology.

Triazol: a privileged scaffold for proteolysis targeting chimeras

2019 ◽  
Vol 11 (22) ◽  
pp. 2919-2973 ◽  
Author(s):  
Li-Wen Xia ◽  
Meng-Yu Ba ◽  
Wei Liu ◽  
Weyland Cheng ◽  
Chao-Ping Hu ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Anticancer Activity ◽  
Mode Of Action ◽  
Critical Analysis ◽  
Enzyme Inhibitors ◽  
Structure Activity Relationship ◽  
Target Protein ◽  
Activity Relationship ◽  
Structure Activity ◽  
Privileged Scaffold

Current traditional drugs such as enzyme inhibitors and receptor agonists/antagonists present inherent limitations due to occupancy-driven pharmacology as the mode of action. Proteolysis targeting chimeras (PROTACs) are composed of an E3 ligand, a connecting linker and a target protein ligand, and are an attractive approach to specifically knockdown-targeted proteins utilizing an event-driven mode of action. The length, hydrophilicity and rigidity of connecting linkers play important role in creating a successful PROTAC. Some PROTACs with a triazole linker have displayed promising anticancer activity. This review provides an overview of PROTACs with a triazole scaffold and discusses its structure–activity relationship. Important milestones in the development of PROTACs are addressed and a critical analysis of this drug discovery strategy is also presented.

scholarly journals Recent Advances in Synthesis of 4-Arylcoumarins

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2417 ◽  
Author(s):  
Jong-Wha Jung ◽  
Nam-Jung Kim ◽  
Hwayoung Yun ◽  
Young Han
Keyword(s):  
Biological Activities ◽  
Synthetic Methods ◽  
Metal Catalysis ◽  
Naturally Occurring ◽  
Recent Advances ◽  
Formation Type ◽  
Privileged Scaffold ◽  
Acid Catalyzed ◽  
A Minor ◽  
Synthetic Approaches

4-Arylcoumarins (4-aryl-2H-1-benzopyran-2-one), also known as neoflavones, comprise a minor subclass of naturally occurring flavonoids. Because of their broad-spectrum biological activities, arylcoumarins have been attracting the attention of the organic and medicinal chemistry communities, and are considered as an important privileged scaffold. Since the development of Pechmann condensation, a classical acid-catalyzed condensation between phenol and β-keto-carboxylic acid, several versatile and efficient synthetic approaches for 4-arylcoumarins have been reported. This review summarizes recent advances in the synthesis of the 4-arylcoumarin scaffold by classifying them based on the final bond-formation type. In particular, synthetic methods executed under mild and highly efficient conditions, such as solvent-free reactions and transition metal catalysis, are highlighted.

Sign in / Sign up

Export Citation Format

Share Document