This review explores the concept of using privileged scaffolds to identify biologically active compounds through building chemical libraries. We hope to accomplish three main objectives: to provide one of the most comprehensive listings of privileged scaffolds; to reveal through four selected examples the present state of the art in privileged scaffold library synthesis (in hopes of inspiring new and even more creative approaches); and also to offer some thoughts on how new privileged scaffolds might be identified and exploited.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2908274 | PMC |
http://dx.doi.org/10.1016/j.cbpa.2010.02.018 | DOI Listing |
Toxicol Rep
June 2025
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India.
Imidazo based heterocyclic derivatives are considered as privileged scaffolds due to their presence in various pharmacologically active compounds and in marketed formulations. The present study reports toxicological evaluation of three imidazo based heterocyclic derivatives which are currently being investigated for their potential anticancer activity. Compounds IG-01-007, IG-01-008, and IG-01-009 were assessed for cytotoxicity, hemolysis, and DNA fragmentation activity.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Department of Medical Chemistry, Institute of Chemistry, Saint Petersburg State University, Saint Petersburg 199034, Russia.
The use of the concept of privileged structures significantly accelerates the search for new leads and their optimization. 6-(methylsulfonyl)-8-(4-methyl-4-1,2,4-triazol-3-yl)-2-(5-nitro-2-furoyl)-2,6-diazaspiro[3.4]octane has been identified as a lead, with MICs of 0.
View Article and Find Full Text PDFCurr Pharm Des
January 2025
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt.
The pyrimidine nucleus is a fundamental component of human DNA and RNA, as well as the backbone of many therapeutic agents. Its significance in medicinal chemistry is well-established, with pyrimidine derivatives receiving considerable attention due to their potent anticancer properties across various cancer cell lines. Numerous derivatives have been synthesized, drawing structural inspiration from known anticancer agents like dihydropyrimidine compounds, which include the active cores of drugs such as 5-fluorouracil and monastrol, both of which have demonstrated strong anticancer efficacy.
View Article and Find Full Text PDFMolecules
December 2024
Laboratory of Evaluation and Synthesis of Bioactive Substances (LASSBio), Institute of Biomedical Sciences, Federal University of Rio de Janeiro, Rio de Janeiro 21941-902, RJ, Brazil.
The 4-aminoquinazoline scaffold is a privileged structure in medicinal chemistry. Regioselective nucleophilic aromatic substitution (SAr) for replacing the chlorine atom at the 4-position of 2,4-dichloroquinazoline precursors is well documented in the scientific literature and has proven useful in synthesizing 2-chloro-4-aminoquinazolines and/or 2,4-diaminoquinazolines for various therapeutic applications. While numerous reports describe reaction conditions involving different nucleophiles, solvents, temperatures, and reaction times, discussions on the regioselectivity of the SAr step remain scarce.
View Article and Find Full Text PDFMolecules
December 2024
College of Materials Science and Technology, Nanjing University of Aeronautics and Astronautics, Nanjing 211106, China.
The advancement of synthetic host-guest chemistry has played a pivotal role in exploring and quantifying weak non-covalent interactions, unraveling the intricacies of molecular recognition in both chemical and biological systems. Macrocycles, particularly calix[4]resorcinarene-based cavitands, have demonstrated significant utility in receptor design, facilitating the creation of intricately organized architectures. Within the realm of macrocycles, these cavitands stand out as privileged scaffolds owing to their synthetic adaptability, excellent topological structures, and unique recognition properties.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!