Design, Synthesis, and Biological Evaluation of Potential Photodynamic Therapy Dyes PDF Download
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Author: Todd Simard
Publisher:
ISBN:
Category :
Languages : en
Pages : 92
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Book Description
Author: Todd Simard
Publisher:
ISBN:
Category :
Languages : en
Pages : 92
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Book Description
Author: Gregory Allen Schamerhorn
Publisher:
ISBN:
Category :
Languages : en
Pages : 307
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Book Description
Based upon the promising results of previous libraries that incorporated a thioamide/amide "switch", we have prepared a new library of thiorhodamine analogues in order to more closely examine the effects of isolated structural modifications on P-gp activity. Biological examination of these thiorhodamines suggested that P-gp expressing cells exhibit "selection rules" with respect to incorporation of amide and/or thioamide functionality; rates of transport by the pump for amide-bearing derivatives were more rapid than for thioamides. The results of this library suggested that appropriate functionalization of rhodamine dyes could allow one to tune their in vivo properties to be desirable for a particular application. To this end, we have prepared several libraries of selenorhodamine dyes and examined them for their ability to function as photosensitizers in the photodynamic therapy of malignant cells, as well as in the selective depletion of alloreactive T cells in extracorporeal photopheresis. Thioamide-bearing dyes were found to be effective photosensitizers in photodynamic therapy (PDT), whereas amide-bearing dyes showed desirable activity in extracorporeal photopheresis. Recently, the use of tellurorosamine dyes as reversible fluorescent probes for the continuous monitoring of reactive oxygen species in vivo was reported. Such probes are based on the Te(II)/Te(IV) redox cycle. We have evaluated several tellurorosamine dyes for their potential use as reversible probes, explored various methods of their oxidation, and examined their chemical stabilities under cell-like conditions. Oxidized analogues of tellurorosamine dyes in which the 9-phenyl substituent has been functionalized with ortho-methyl groups display increased hydrolytic stability relative to those bearing solely hydrogens at ortho-positions. Our original examination of thiorhodamine dyes and their effects on P-gp activity also showed that dyes having fused ring moieties at the 3-amino position resulted in decreased ATPase stimulation and increased binding affinity relative to those having dimethylamino fragments at the 3-amino position. Hence, we have developed synthetic routes towards rhodamine dyes having fused rings at both the 3- and 6-amino positions in an effort to develop novel, potent inhibitors of P-gp. Initial results suggest that selenorhodamines having fused ring moieties at both the 3- and 6-amino positions are more effective photosensitizers in PDT of cancer cells than those having fused rings only at the 3-amino position. Furthermore, oxidized analogues of tellurorosamine dyes functionalized with fused rings at both the 3- and 6-amino positions display increased hydrolytic stability relative to the analogous 3,6-bis(dimethylamino) tellurorosamine derivatives.
Author: Louis Mark-Antony Rogers
Publisher:
ISBN:
Category :
Languages : en
Pages : 221
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Author: Gilles Gasser
Publisher: John Wiley & Sons
ISBN: 111851002X
Category : Science
Languages : en
Pages : 437
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Book Description
Understanding, identifying and influencing the biological systems are the primary objectives of chemical biology. From this perspective, metal complexes have always been of great assistance to chemical biologists, for example, in structural identification and purification of essential biomolecules, for visualizing cellular organelles or to inhibit specific enzymes. This inorganic side of chemical biology, which continues to receive considerable attention, is referred to as inorganic chemical biology. Inorganic Chemical Biology: Principles, Techniques and Applications provides a comprehensive overview of the current and emerging role of metal complexes in chemical biology. Throughout all of the chapters there is a strong emphasis on fundamental theoretical chemistry and experiments that have been carried out in living cells or organisms. Outlooks for the future applications of metal complexes in chemical biology are also discussed. Topics covered include: • Metal complexes as tools for structural biology • IMAC, AAS, XRF and MS as detection techniques for metals in chemical biology • Cell and organism imaging and probing DNA using metal and metal carbonyl complexes • Detection of metal ions, anions and small molecules using metal complexes • Photo-release of metal ions in living cells • Metal complexes as enzyme inhibitors and catalysts in living cells Written by a team of international experts, Inorganic Chemical Biology: Principles, Techniques and Applications is a must-have for bioinorganic, bioorganometallic and medicinal chemists as well as chemical biologists working in both academia and industry.
Author: Mahmoud H. Abdel-Kader
Publisher: Springer Science & Business Media
ISBN: 3642396291
Category : Science
Languages : en
Pages : 317
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Book Description
Photodynamic Therapy: From Theory to Application brings attention to an exceptional treatment strategy, which until now has not achieved the recognition and breadth of applications it deserves. The authors, all experts and pioneers in their field, discuss the history and basic principles of PDT, as well as the fundamentals of the theory, methods, and instrumentation of clinical diagnosis and treatment of cancer. Non-oncological applications such as the use of PDT in control of parasites and noxious insects are also discussed. This book serves as a standard reference for researchers and students at all levels, clinical specialists interested in the topic and those in industry exploring new areas for development. A comprehensive exposition of both the theory and application of PDT, this book fills the gaps in the current literature by bringing together both basic understanding of the process of PDT and an expanded vision of its applications.
Author: Herwig Kostron
Publisher: Royal Society of Chemistry
ISBN: 1782624511
Category : Medical
Languages : en
Pages : 680
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Book Description
Comprehensive Series in Photochemical and Photobiological Sciences. Photodynamic therapy (PDT) is increasingly being used amongst health practitioners in combating a variety of disease. This book reviews the current state of development of PDT, and also presents the foreseeable advancements of the field in the next decade. Practitioners in biological sciences, biotechnology and medicinal and pharmaceutical chemistry will find this book an invaluable source of information. Chapters are drawn from research discusses at the 10th International Symposium on Photodynamic Therapy and Photodiagnosis in Clinical Practice in Brixen and are written and edited by leaders in the field. Mirroring the philosophy of that meeting, this book contains an informative balance of the basic sciences and clinical applications of PDT. Following an introduction to PDT, its history, and how techniques have developed, chapter serve as a practical guide for practitioners, covering topics such as sensitizer dosage and light dosage, and examples of relevant studies. The text goes further tp explore areas outside the medical field, such as the impact of PDT on society and the environment, and the economics of therapies. This book is dedicated to the memory of Professor Giulio Jori, and expert in this field, who sadly passed away on the 23rd December 2014.
Author: Michael H. Gold
Publisher: Springer Science & Business Media
ISBN: 1441912983
Category : Medical
Languages : en
Pages : 209
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Book Description
Photodynamic therapy is a proven effective treatment of actinically damaged skin cells, nonmelanoma skin cancers, and acne and other pilosebaceous conditions. As an agent for general facial rejuvenatin it has untapped potential. The current state of PDT therapy and future applications are discussed in detail in this exciting new volume. Throughout, the focus is on evidence-based clinical uses of PDT, including pretreatment regimens, avoidance and management of complications, and posttreatment suggestions.
Author: Antonello Mai
Publisher: Springer Nature
ISBN: 3030429822
Category : Science
Languages : en
Pages : 569
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Book Description
This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.
Author: B.E. Maryanoff
Publisher: Elsevier
ISBN: 0080526373
Category : Science
Languages : en
Pages : 338
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Book Description
Volume 4 of Advances in Medicinal Chemistry is comprised of six chapters on a wide range of topics in medicinal chemistry, including molecular modeling, structure-based drug design, organic synthesis, peptide conformational analysis, biological assessment, structure-activity correlation, and lead optimization. Chapter 1 presents an account about amino acid-based peptide mimetics corresponding to b-turn, loop, helical motifs in proteins as a probe of ligand-receptor and ligand-enzyme molecular interactions. Chapter 2 addresses new facets of the medicinal chemistry of the important anticancer drug Taxol® (paclitaxel). Chapter 3 relates an account of the search for new drugs for the treatment of malaria based on the natural product artemisinin. Chapter 4 applies computational chemistry to the evaluation of compound libraries for biological testing. Chapter 5 describes the construction of a 3-dimensional molecular model of the human thrombin receptor, the first protease-activated G-protein coupled receptor (PAR-1), as a means to explore the intermolecular contacts involved in agonist peptide recognition. Finally, Chapter 6 describes the research conducted at Merck on inhibitors of farnesyl transferase as a potential treatment for human cancers.
Author: Michael R. Hamblin
Publisher: Artech House
ISBN: 1596932783
Category : Medical
Languages : en
Pages : 601
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Book Description
With today's focus on targeted and minimally invasive therapies, photodynamic therapy (PDT) is now being studied and used to combat many disease states and to investigate critical biological questions. This groundbreaking resource brings you the latest advances in photodynamic therapy and offers you a solid understanding of the design, delivery and dosimetry of the three basic ingredients of PDT - photosensitizers, light and oxygen. The book covers novel areas of mechanistic and innovative translational approaches. Moreover, it gives you an overview of the important medical applications of PDT, including approved treatments, clinical trials, and investigated therapies for cancer and non-malignant diseases.
