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The development of new drugs/drug candidates for medical treatment remains an exciting but challenging process as only a limited number of synthetic compounds fit well into the discovery and development process after multiple experimentation and screening efforts in search of their preclinical properties. Over the years, this continuous demand has been fueled by the use of organic/synthetic chemistry protocols that deliver new molecules or improve the existing toolbox diversifying libraries of pharmacophores of medicinal interest. The application of new methodologies particularly employing green and sustainable commercial feedstock chemicals for the discovery and development of biological therapeutics opens up new avenues of research. In parallel, the discovery and development of new organic molecules have always proved effective in designing drugs while overcoming critical challenges to the pharmaceutical industry and providing innovative solutions toward commercialized medicines. This reprint aims to provide a far-reaching overview of the most recent developments in synthetic methodologies as well as medicinal chemistry applications of small-molecule inhibitors.

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