To date, numerous small molecules have been developed as chemical probes that can perturb a physiological system, changing diverse pathophysiological phenotypes, eventually leading to the development of novel and innovative drugs or drug candidates. As new chemical entities were explored and high-throughput screening (HTS) was technically improved, the rate of the overall drug discovery process was increased. However, productivity for the development of novel drugs has not been significantly improved. Recently, the process for drug discovery is sometimes reported to be initiated with the screening of chemical libraries equipped with privileged structures, especially derived from natural compound-like scaffolds. These types of privileged structures are defined as molecular frameworks that can afford useful hits for druggable targets such as enzymes and receptors. Examples of privileged scaffolds are as follows.
• Flavonoids
• Chalcones
• Benzodiazepines
• Aryl indoles
• Bisaryls
• Quinolines
• Curcuminoids
These molecules have various advantages, including rapid accessibilities to find hits for the targets, and structural rigidities to improve on-target effects. This indicates that the approach by screening the privileged structure-derived chemical library might be a viable strategy to improve the productivity of the drug discovery process, especially for the initial stages of the process. For example, synthetic flavonoids such as Alvocidib and Voruciclib are currently investigated as novel CDK9 inhibitors under clinical trials for the treatment of malignant tumors. Thus, considering all of those, the development of synthetic methodologies for privileged natural product scaffolds would be a very important and worthwhile Research Topic. This Research Topic will introduce diverse natural product scaffolds and their preparation methods with novelty and feasibility for successful drug discovery.
• Novel synthetic methodology for privileged scaffolds
• Total synthesis of natural products
• Chemical genetics studies using chemical libraries of privileged scaffolds
• Medicinal chemistry works using privileged scaffolds
To date, numerous small molecules have been developed as chemical probes that can perturb a physiological system, changing diverse pathophysiological phenotypes, eventually leading to the development of novel and innovative drugs or drug candidates. As new chemical entities were explored and high-throughput screening (HTS) was technically improved, the rate of the overall drug discovery process was increased. However, productivity for the development of novel drugs has not been significantly improved. Recently, the process for drug discovery is sometimes reported to be initiated with the screening of chemical libraries equipped with privileged structures, especially derived from natural compound-like scaffolds. These types of privileged structures are defined as molecular frameworks that can afford useful hits for druggable targets such as enzymes and receptors. Examples of privileged scaffolds are as follows.
• Flavonoids
• Chalcones
• Benzodiazepines
• Aryl indoles
• Bisaryls
• Quinolines
• Curcuminoids
These molecules have various advantages, including rapid accessibilities to find hits for the targets, and structural rigidities to improve on-target effects. This indicates that the approach by screening the privileged structure-derived chemical library might be a viable strategy to improve the productivity of the drug discovery process, especially for the initial stages of the process. For example, synthetic flavonoids such as Alvocidib and Voruciclib are currently investigated as novel CDK9 inhibitors under clinical trials for the treatment of malignant tumors. Thus, considering all of those, the development of synthetic methodologies for privileged natural product scaffolds would be a very important and worthwhile Research Topic. This Research Topic will introduce diverse natural product scaffolds and their preparation methods with novelty and feasibility for successful drug discovery.
• Novel synthetic methodology for privileged scaffolds
• Total synthesis of natural products
• Chemical genetics studies using chemical libraries of privileged scaffolds
• Medicinal chemistry works using privileged scaffolds
