-
121
Mechanism-based approaches of 1,3,4 thiadiazole scaffolds as potent enzyme inhibitors for cytotoxicity and antiviral activity
Published 2023-02-01“…As a result, there is an urgent need for the development of novel, more effective anticancer and antiviral therapeutics. Scientists, medicinal chemists and researchers are continuously finding novel targets, mechanisms and molecules against theses severe and dangerous infections. …”
Get full text
Article -
122
Binding and Action of Triphenylphosphonium Analog of Chloramphenicol upon the Bacterial Ribosome
Published 2021-04-01“…The synthesized compound represents a promising chemical scaffold for further development by medicinal chemists because it simultaneously targets the two key functional centers of the bacterial ribosome—PTC and peptide exit tunnel.…”
Get full text
Article -
123
Exploring the mode of action of bioactive compounds by microfluidic transcriptional profiling in mycobacteria.
Published 2013-01-01“…It is often very difficult for medicinal chemists to visualize if the novel compounds synthesized for understanding SAR of a particular scaffold have similar molecular mechanism of action (MoA) as that of the initial hit. …”
Get full text
Article -
124
A review on versatile applications of transition metal complexes incorporating Schiff bases
Published 2015-06-01“…Development of a new chemotherapeutic Schiff bases and their metal complexes is now attracting the attention of medicinal chemists. This review compiles examples of the most promising applied Schiff bases and their complexes in different areas.…”
Get full text
Article -
125
Greedy 3-Point Search (G3PS)—A Novel Algorithm for Pharmacophore Alignment
Published 2021-11-01“…Chemical features of small molecules can be abstracted to 3D pharmacophore models, which are easy to generate, interpret, and adapt by medicinal chemists. Three-dimensional pharmacophores can be used to efficiently match and align molecules according to their chemical feature pattern, which facilitates the virtual screening of even large compound databases. …”
Get full text
Article -
126
Advancement in the synthesis of metal complexes with special emphasis on Schiff base ligands and their important biological aspects
Published 2024-01-01“…Development of new Schiff base metal complexes is now attracting the attention of medicinal chemists. This review compiles the synthesis of various multidentate Schiff bases ligands and their complexation with various metals such as Zr, V, Mo, Mn, Fe, Zn, Re, Cd, and Ln. …”
Get full text
Article -
127
Cyanobacterial Metabolite Calothrixins: Recent Advances in Synthesis and Biological Evaluation
Published 2016-01-01“…Due to the low isolation yields from the marine source and the promise this scaffold holds for anticancer and antimicrobial drugs, organic and medicinal chemists around the world have embarked on developing efficient synthetic routes to produce calothrixins. …”
Get full text
Article -
128
Marine Natural Products as Models to Circumvent Multidrug Resistance
Published 2016-07-01“…It is expected that the data gathered during the last decades concerning their synthesis and MDR-inhibiting activities will help medicinal chemists develop potential drug candidates using marine natural products as models which can deliver new ABC transporter inhibitor scaffolds.…”
Get full text
Article -
129
Mutagenicity in a Molecule: Identification of Core Structural Features of Mutagenicity Using a Scaffold Analysis.
Published 2016-01-01“…The recognized mutagenic groups of scaffold can serve as a guide for medicinal chemists to prevent the development of potentially mutagenic therapeutic agents in early drug design or development phases, by modifying the core structures of mutagenic compounds to form non-mutagenic compounds. …”
Get full text
Article -
130
25 Years of Collaboration with A Genius: Deciphering Adenine Nucleotide Ca<sup>2+</sup> Mobilizing Second Messengers Together with Professor Barry Potter
Published 2020-09-01“…For 25 years, Professor Barry Potter has been one of the major medicinal chemists in this topical area, designing and contributing numerous analogues to develop structure–activity relationships (SAR) as a basis for tool development in biochemistry and cell biology and for lead development in proof-of-concept studies in disease models. …”
Get full text
Article -
131
An Update on Synthesis of Coumarin Sulfonamides as Enzyme Inhibitors and Anticancer Agents
Published 2022-02-01“…The research and development of coumarin, sulfonamide-based pharmacology, and medicinal chemistry have become active topics, and attracted the attention of medicinal chemists, pharmacists, and synthetic chemists. …”
Get full text
Article -
132
Target-Based Anticancer Indole Derivatives for the Development of Anti-Glioblastoma Agents
Published 2023-03-01“…The final goal is to pave the way for medicinal chemists in the future design and development of novel effective indole-based anti-GBM agents.…”
Get full text
Article -
133
Indole-Based Compounds in the Development of Anti-Neurodegenerative Agents
Published 2024-05-01“…In this context, the urgency of discovering viable therapies is critical and, despite significant efforts by medicinal chemists in developing potential drug candidates and exploring various small molecules as therapeutics, regrettably, a truly effective treatment is yet to be found. …”
Get full text
Article -
134
Engineering Saccharomyces cerevisiae for the de novo Production of Halogenated Tryptophan and Tryptamine Derivatives
Published 2023-04-01“…Inspired by the versatility of these compounds, medicinal chemists have for decades exploited indole as a core structure in the drug discovery process. …”
Get full text
Article -
135
Visualisation and efficient communication in structure-based lead discovery
Published 2011“…The appropriate integration and visualisation of this data maximises the impact of the underlying information within the context of a project both not only for computational chemists and structural biologists but also for biologists and medicinal chemists. In this chapter we will discuss current approaches and outstanding issues associated with this particular challenge in the context of SBLD. © 2011 Bentham Science Publishers Ltd. …”
Journal article -
136
A compendium of cyclic sugar amino acids and their carbocyclic and heterocyclic nitrogen analogues.
Published 2013“…These building blocks provide access to hydrophilic and hydrophobic peptide isosteres whose physical properties allow entry to a region of chemotherapeutic space which is still under-explored by medicinal chemists. These building blocks are also important in providing amino acids whose inherent conformational bias leads to predisposition to secondary structure upon oligomerisation in relatively short sequences. …”
Journal article -
137
An Overview on Synthetic 2-Aminothiazole-Based Compounds Associated with Four Biological Activities
Published 2021-03-01“…Owing to their wide scale of biological activities, their structural variations have produced attention amongst medicinal chemists. The present review highlights the recently synthesized 2-aminothiazole-containing compounds in the last thirteen years (2008–2020). …”
Get full text
Article -
138
An Overview of Anticancer Chalcones with Apoptosis Inducing Activity
Published 2017-03-01“…The diversity of scaffolds described in this review along with their structure-activity relationships could help medicinal chemists in development of new selective anticancer chalcones with improved potency.…”
Get full text
Article -
139
New Synthesis of Imidazo[1,2-a]pyrimidines Catalyzed Using Gold Nanoparticles
Published 2021-11-01“…Heterocyclic compounds are abundant in natural products and bioactive compounds and play a huge role in the present repertoire of medicinal chemists due to their potential capability to modulate physicochemical properties. …”
Get full text
Article -
140
Design and Synthesis of Imidazopyrazolopyridines as Novel Selective COX-2 Inhibitors
Published 2015-08-01“…The presence of a strong connection between reported COX-2 inhibitors and cardiac toxicity encourages medicinal chemists to explore new scaffolds. In the present study, we introduced imidazopyrazolopyridines as new potent and selective COX-2 inhibitors that lack the standard pharmacophoric binding features to hERG. …”
Get full text
Article