Synthesis of Biologically Active Cytoprotective and Anticancer Small Molecules


Book Description

Cancer is the most common cause of disease-related fatalities in the United States of America. It is estimated that more then half a million people per year will die from various forms of cancer. One of the defining characteristics of cancer is an uncontrollable growth of cells. Regardless of its type, cancers evade the various mechanisms by which cells die naturally, apoptosis. In these studies my efforts have been focused on identification, design and synthesis of small molecules that effectively induce death in various cancers by activating the apoptotic cascade. Described herein is discovery of anticancer small molecules that selectively induce cell death in white blood cancers and non-toxic to other cell types. This discovery was further elaborated to the design and synthesis of compounds, which potently and effectively kill melanoma cells. Thus, compounds displaying such selectivity have strong potential for identification of cancer-type specific biological pathways, and optimized versions of these small molecules have potential in targeted anti-cancer therapy.




Diversity-Oriented Synthesis


Book Description

Discover an enhanced synthetic approach to developing and screening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways. This book presents the most effective methods in diversity-oriented synthesis for creating small molecule collections. It offers tested and proven strategies for developing diversity-oriented synthetic libraries and screening methods for identifying ligands. Lastly, it explores some promising new applications based on diversity-oriented synthesis that have the potential to dramatically advance studies in drug discovery and chemical biology. Diversity-Oriented Synthesis begins with an introductory chapter that explores the basics, including a discussion of the relationship between diversity-oriented synthesis and classic combinatorial chemistry. Divided into four parts, the book: Offers key chemical methods for the generation of small molecules using diversity-oriented principles, including peptidomimetics and macrocycles Expands on the concept of diversity-oriented synthesis by describing chemical libraries Provides modern approaches to screening diversity-oriented synthetic libraries, including high-throughput and high-content screening, small molecule microarrays, and smart screening assays Presents the applications of diversity-oriented synthetic libraries and small molecules in drug discovery and chemical biology, reporting the results of key studies and forecasting the role of diversity-oriented synthesis in future biomedical research This book has been written and edited by leading international experts in organic synthesis and its applications. Their contributions are based on a thorough review of the current literature as well as their own firsthand experience developing synthetic methods and applications. Clearly written and extensively referenced, Diversity-Oriented Synthesis introduces novices to this highly promising field of research and serves as a springboard for experts to advance their own research studies and develop new applications.




Green Synthetic Approaches for Biologically Relevant Heterocycles


Book Description

Green Synthetic Approaches for Biologically Relevant Heterocycles, Second Edition, Volume One: Advanced Synthetic Techniques reviews this significant group of organic compounds within the context of sustainable methods and processes, expanding on the first edition with fully updated coverage and a whole range of new chapters. Volume One explores advanced synthetic techniques, with each chapter presenting in-depth coverage of various green protocols for the synthesis of a wide variety of bioactive heterocycles that are classified on the basis of ring-size and/or the presence of heteroatoms. Techniques covered range from high pressure cycloaddition reactions and microwave irradiation to sustainable one-pot domino reactions. This updated edition is an essential resource on sustainable approaches for academic researchers, R&D professionals, and students working across medicinal, organic, natural product and green chemistry. Provides fully updated coverage of the field of greener heterocycle synthesis Includes new chapters on varied multicomponent reactions, alongside both traditional and novel approaches Presents information in an accessible style with an emphasis on sustainability







Beyond the Molecular Frontier


Book Description

Chemistry and chemical engineering have changed significantly in the last decade. They have broadened their scopeâ€"into biology, nanotechnology, materials science, computation, and advanced methods of process systems engineering and controlâ€"so much that the programs in most chemistry and chemical engineering departments now barely resemble the classical notion of chemistry. Beyond the Molecular Frontier brings together research, discovery, and invention across the entire spectrum of the chemical sciencesâ€"from fundamental, molecular-level chemistry to large-scale chemical processing technology. This reflects the way the field has evolved, the synergy at universities between research and education in chemistry and chemical engineering, and the way chemists and chemical engineers work together in industry. The astonishing developments in science and engineering during the 20th century have made it possible to dream of new goals that might previously have been considered unthinkable. This book identifies the key opportunities and challenges for the chemical sciences, from basic research to societal needs and from terrorism defense to environmental protection, and it looks at the ways in which chemists and chemical engineers can work together to contribute to an improved future.




Diversity Oriented Synthesis


Book Description

Has the concept of Diversity Oriented Synthesis remained unchanged over these two decades, or do we observe improvements or deviations from the original guidelines drawn by the pioneers? The aim of this Research Topic is to collect contributions on the state-of-the-art and progress of Diversity Oriented Synthesis, and to foresee its shape in the next decade.




Biologically Active Small Molecules


Book Description

Biologically Active Small Molecules: Modern Applications and Therapeutic Perspectives focuses on small molecules as active pharmacological agents, their pharmacotherapeutically active properties, new approaches in drug discovery using small molecules, and biopharmaceutic approaches for low molecular weight ligands. Molecules of low mass play a pivotal role in pharmacology because they exhibit multifarious pharmacological effects. Small molecules have become universally popular due to their simple chemistry, easy separation techniques, versatile acceptance for computational studies, large number of places for the substitution of active chemical moieties by well-established synthetic routes with less effort, better quality attributes, and ability to demonstrate numerous biological activities. This book provides a multidisciplinary approach that delivers the most updated knowledge and advances of some newly developed therapeutically active low molecular weight compounds. It includes chapters that present up-to-date and concise content on the classification, structures, chemical syntheses, medicinal chemistry, pharmacology, biochemical pathways, mechanism of actions, side effects, and adverse effects of small molecule drug discovery. The book covers a broad area by highlighting the advances of inter- and multidisciplinary fields of medicine, chemical sciences, and pharmaceuticals. The flowcharts, figures, illustrations, and diagrams provide important information and will be of great interest for readers.




Biologically Active Small Molecules


Book Description

"Biologically Active Small Molecules: Modern Applications and Therapeutic Perspectives focuses on small molecules as active pharmacological agents, their pharmacotherapeutically active properties, new approaches in drug discovery using small molecules, and biopharmaceutic approaches for low molecular weight ligands. Molecules of low mass play a pivotal role in pharmacology because they exhibit multifarious pharmacological effects. Small molecules have become universally popular due to their simple chemistry, easy separation techniques, versatile acceptance for computational studies, large number of places for the substitution of active chemical moieties by well-established synthetic routes with less effort, better quality attributes, and ability to demonstrate numerous biological activities. This book provides a multidisciplinary approach that delivers the most updated knowledge and advances of some newly developed therapeutically active low molecular weight compounds. It includes chapters that present up-to-date and concise content on the classification, structures, chemical syntheses, medicinal chemistry, pharmacology, biochemical pathways, mechanism of actions, side effects, and adverse effects of small molecule drug discovery. The book covers a broad area by highlighting the advances of inter- and multidisciplinary fields of medicine, chemical sciences, and pharmaceuticals. The flowcharts, figures, illustrations, and diagrams provide important information and will be of great interest for readers."--