Frontiers in Medicinal Chemistry

Volume 6

by

Atta-ur- Rahman , Allen B. Reitz, M. Iqbal Choudhary

DOI: 10.2174/97816080546401130601
eISBN: 978-1-60805-464-0, 2012
ISBN: 978-1-60805-561-6
ISSN: 1567-2042

  
  




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Table of Contents

Preface , Pp. vii-viii (2)

Allen B. Reitz, Atta-ur-Rahman and M. Iqbal Choudhary
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Contributors , Pp. ix-xiii (5)

Allen B. Reitz, Atta-ur-Rahman and M. Iqbal Choudhary
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AntiViral-HyperActivation Limiting Therapeutics (AV-HALTs): A New Class of Antiviral Drugs , Pp. 3-21 (19)

Franco Lori, Julianna Lisziewicz, Davide De Forni and Mike Stevens
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The Efficacy of Viral Capsid Inhibitors in Human Enterovirus Infection and Associated Diseases , Pp. 22-40 (19)

Shin-Ru Shih, Gary Brewer, Peng-Nien Huang, Kuo-Feng Weng, Chin Li, Hongtao Wang, Tzu-Chun Chen and Mei-Ling Li
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Antibiotic Properties and Applications of Lactoferrin , Pp. 41-61 (21)

Eugene D. Weinberg
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The Targets of Currently Used Antibacterial Agents: Lessons for Drug Discovery , Pp. 62-96 (35)

Roland P. Lange, Hans H. Locher, Pierre C. Wyss and Rudolf L. Then
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Chemotherapy of Leishmaniasis: Past, Present and Future , Pp. 97-130 (34)

Jyotsna Mishra, Anubha Saxena and Sarman Singh
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Antimicrobial Peptides in Oral Cancer: Review Article , Pp. 131-153 (23)

Christina Roebke, Jürgen Harder and Jens E. Meyer
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Inhibiting Cell Cycle Kinases in Cancer Therapy , Pp. 154-188 (35)

Guillermo de Cárcer, Ignacio Pérez de Castro and Marcos Malumbres
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mTOR Inhibitors (Rapamycin and Its Derivatives) and Nitrogen Containing Bisphosphonates: Bi-functional Compounds for the Treatment of Bone Tumours , Pp. 189-202 (14)

Ory Benjamin, Moriceau Gatien, Gobin Bérengère, Redini Françoise and Heymann Dominique
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New Biological Approaches in Asthma: DNA-Based Therapy , Pp. 203-226 (24)

Li-Chieh Wang, Jyh-Hong Lee, Yao-Hsu Yang, Yu-Tsan Lin and Bor-Luen Chiang
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Building a Bridge Between Clinical and Basic Research: the Phenotypic Elements of Familial Predisposition to Type 1 Diabetes , Pp. 227-248 (22)

Elena Matteucci and Ottavio Giampietro
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Molecular Lipophilicity in Protein Modeling and Drug Design , Pp. 249-290 (42)

Roman G. Efremov, Anton O. Chugunov, Timothy V. Pyrkov, John P. Priestle, Vladimir M. Pentkovsky, Alexander S. Arseniev and Edgar Jacoby
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Hydrogen/Deuterium Exchange-Mass Spectrometry: A Powerful Tool for Probing Protein Structure, Dynamics and Interactions , Pp. 291-323 (33)

Yuko Tsutsui and Patrick L. Wintrode
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From Drug Target to Leads-Sketching a Physico-Chemical Pathway for Lead Molecule Design In Silico , Pp. 324-360 (37)

Saher Afshan Shaikh, Tarun Jain, Gurvisha Sandhu, Anjali Soni and Bhyravabhotla Jayaram
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Bis and Tris Indole Alkaloids from Marine Organisms: New Leads for Drug Discovery , Pp. 361-385 (25)

Leena Gupta, Archna Talwar and P. M. S. Chauhan
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Derivatives of Nucleic Acids for Selective RNA Targeting , Pp. 386-411 (26)

Vaijayanti A. Kumar
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Poly(ADP-ribose) Polymerase Inhibitors: New Pharmacological Functions and Potential Clinical Implications , Pp. 412-471 (60)

Catalina Alarcón de la Lastra, Isabel Villegas Lama and Marina Sánchez-Fidalgo
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Preface

Medicinal chemistry is an ever expanding discipline where new and exciting discoveries are made at the interface of chemistry and biology on a daily basis. The 6th volume of the Frontiers in Medicinal Chemistry contains 16 scholarly articles in six broad areas, contributed by some of the leading experts in the field of medicinal and pharmaceutical chemistry.

In the broad field of infectious diseases, five excellent contributions are compiled. The article contributed by Lori et al., reviews the most recent discoveries in the field of viral pathogenesis and the development of a new anti-retroviral class of compounds, termed as Antiviral-Hyper Activation Limiting Therapeutics (AV-HALTS) for the treatment of HIV-1. The use of viral CAPSID inhibitors for the treatment of human enterovirus infection and associated diseases is reviewed by Shih et al. Eugene Weinberg has contributed a very well written account of the use of lactoferrin protein in nutraceutical, preservative and pharmaceutical products.

The molecular basis of infection has been a topic of general interest since the last several decades. Lang et al., have reviewed the molecular targets of most common antibacterial agents. They linked the past experiences with the prospects of new drug discovery and development. Leishmaniasis is a parasitic disease, affecting a large number of people. Misra et al., have reviewed the area of drug development against leishmaniasis. This includes drugs which are based on new molecular targets against the parasite.

Cancer remains an important area of therapeutic research. Volume 6 of Frontiers in Medicinal Chemistry contains three well written articles which review various aspects of cancer chemotherapy. Based on the observations that antimicrobial peptides (AMPs) are differentially regulated in various cancers, such as oral squamous cell carcinomas, AMPs and their synthetic derivatives can be used as potential anticancer agents. This topic is reviewed lucidly by Roebke, et al.

Càrcer et al., in their review have discussed the development of novel inhibitors against cell cycle kinases, a key family of enzymes in cell proliferation. Another review in the field of oncology by Benjamin et al., focuses on newly discovered anti-tumor (primary bone tumors and bone metastases) activity of rapamycin and its derivatives. Rapamycin is a well known antifungal agent. In this review, the mTOR inhibitory activity of rapamycin derivatives is described, along with their primary mechanism of action as anti-tumour agents.

DNA-Based therapy of asthma is reviewed by Wang et al. Asthma is one of the most common health disorders globally, causing considerable morbidity. New approaches to the treatment of asthma by biologicals will certainly be of general interest.

Genetic predisposition to type-1 diabetes (T1D) is an area of considerable scientific interest. A number of marker molecules for T1D have been identified with some degree of confidence. Matteucci and Giampietro describe the results of their own investigations on various factors, genetic and epigenetic, which probably contribute in the development of T1D in certain families and population groups.

Efremov and colleagues have reviewed the role of lipophilicity in protein modeling for in silico drug designing. Molecular hydrophobicity (MHP) is an important property in drug ability assessment (Lipinski’s rule). This review narrates the applications of MHP-based techniques in a number of biologically important tasks.

Recent developments in mass spectrometry have contributed immensely in our understanding of biological processes. Hydrogen / deuterium exchange mass spectrometry, though based on an old concept, is now effectively employed in medicinal chemistry and drug development. Tsutsui and Wintrode have contributed an excellent review on hydrogen exchange mass spectrometry and its applications in structural biology, as well as in rational drug development.

The review by Shaikh et al., is concerned on the relevance of in silico studies in drug discovery and development, as well as in deducing the ADMET properties.

Indole alkaloids are important pharmacophores in various classes of drugs. Gupta et al., have contributed a review on bis- and tris-indole alkaloids, obtained from marine living resources. They have also reviewed the biological studies conducted so far on this important group of natural products.

Vaijayanti Kumar has reviewed the active research area of synthesis of nucleic acid and derivatives for therapeutic purposes. Structural modifications in nucleic acid mimics, which make them capable of binding with the RNA effectively, is the main focus of this well written article.

Pharmacological and clinical properties of PARP inhibitors [Poly (ADP-ribose) polymerase inhibitors] is reviewed by Lastra et al. The PARP family of enzymes is involved in a variety of physiological and pathological processes. PARP plays an important role in diseases such as stroke, cardiovascular, metabolic and inflammatory disorders. PARP inhibition is therefore an important strategy against various diseases, including viral infections.

The volume 6 of book series, “Frontiers in Medicinal Chemistry”, is expected to receive by the global fraternity of medicinal chemists and pharmaceutical researchers as it provides many excellent and comprehensive reviews in frontier areas of medicinal chemistry.

At the end, we acknowledge the dedicated effort and support of staff of the Bentham Science Publishers in connection with the timely processing of manuscripts for this volume of Frontiers in Medicinal Chemistry. Our special thanks go to Mr. Mahmood Alam and Ms. Qurat-ul-Ain in this connection.

ALLEN B. REITZ
Chemical Biology
Institute of Hepatitis and Virus Research
CEO, Fox C hase Chemical Diversity Center
Incorporation Doylestown, PA 18902
USA

ATTA-UR-RAHMAN, FRS
International Center for Chemical and
Biological Sciences, Karachi
Pakistan

M. IQBAL CHOUDHARY
International Center for Chemical and
Biological Sciences
Pakistan

List of Contributors

Co-Editor(s):
Atta-ur- Rahman
International Center for Chemical and Biological Sciences (HEJ Research Institute of Chemistry
Dr. Panjwani Center for Molecular, Medicine & Drug Research), University of Karachi
Karachi, 75270
Pakistan


Allen B. Reitz
Fox Chase Chemical Diversity Center, Inc
Doylestown
PA , 18902
USA


M. Iqbal Choudhary
International Center for Chemical and Biological Sciences (HEJ Research Institute of Chemistry
Dr. Panjwani Center for Molecular, Medicine & Drug Research), University of Karachi
Karachi, 75270
Pakistan




Contributor(s):
Franco Lori
ViroStatics srl,
Alghero
Italy


Julianna Lisziewicz
kft
Budapest
Hungary


Davide De Forni
ViroStatics srl
Alghero
Italy


Mike Stevens
ViroStatics srl
Princeton
United States


Shin-Ru Shih
Research Center for Emerging Viral Infections, Department of Medical Biotechnology & Laboratory Science
Chang-Gung University
Taiwan


Gary Brewer
Biochemistry and Molecular Biology
UMDNJ-Robert Wood Johnson Medical School
Piscataway
NJ , 08854
USA


Peng-Nien Huang
Research Center for Emerging Viral Infections, Department of Medical Biotechnology & Laboratory Science
Chang-Gung University
Taiwan


Kuo-Feng Weng
Research Center for Emerging Viral Infections, Department of Medical Biotechnology & Laboratory Science
Chang-Gung University
Taiwan


Chin Li
Department of Life Science and Graduate Institute of Molecular Biology
National Chung Cheng University
Chiayi,
Taiwan


Hongtao Wang
Department of Molecular Genetics, Microbiology & Immunology
UMDNJ-Robert Wood Johnson Medical School
Piscataway
NJ, 08854
USA


Tzu-Chun Chen
Department of Microbiology and Immunology
Stanford University
Stanford
CA , 94305
USA


Mei-Ling Li
Biochemistry and Molecular Biology
UMDNJ-Robert Wood Johnson Medical School
Piscataway
NJ , 08854
USA


Eugene D. Weinberg
Department of Biology and Program in Medical Sciences
Indiana University
Bloomington
IN
USA


Roland P. Lange
Actelion Pharmaceuticals Ltd.
Gewerbestrasse 1,
Allschwil, 4123
Switzerland


Hans H. Locher
Actelion Pharmaceuticals Ltd.
Gewerbestrasse 1,
Allschwil, 4123
Switzerland


Pierre C. Wyss
Actelion Pharmaceuticals Ltd.
Gewerbestrasse 1,
Allschwil, 4123
Switzerland


Rudolf L. Then
Actelion Pharmaceuticals Ltd.
Gewerbestrasse 1,
Allschwil, 4123
Switzerland


Jyotsna Mishra
Division of Clinical Microbiology, Department of Laboratory
Medicine, All India Institute of Medical Sciences
New Delhi
India


Anubha Saxena
Division of Clinical Microbiology, Department of Laboratory
Medicine, All India Institute of Medical Sciences
New Delhi
India


Sarman Singh
Division of Clinical Microbiology, Department of Laboratory
Medicine, All India Institute of Medical Sciences
New Delhi
India


Christina Roebke
Department of Otorhinolaryngology, Head, Neck and Plastic Surgery
Lohmuehlenstr. 5
Hamburg, 20099
Germany


Jürgen Harder
Clinical Research Unit, Department of Dermatology
Schittenhelmstr. 11
Kiel, 24105
Germany


Jens E. Meyer
Department of Otorhinolaryngology, Head, Neck and Plastic Surgery
Lohmuehlenstr. 5
Hamburg, 20099
Germany


Guillermo de Cárcer
Cell Division and Cancer Group, Centro Nacional de Investigaciones Oncológicas (CNIO)
Madrid
Spain


Ignacio Pérez de Castro
Cell Division and Cancer Group, Centro Nacional de Investigaciones Oncológicas (CNIO)
Madrid
Spain


Marcos Malumbres
Cell Division and Cancer Group, Centro Nacional de Investigaciones Oncológicas
Madrid
Spain


ORY Benjamin
INSERM, UMR957, Faculté de Médecine, 1 rue Gaston Veil
Université de Nantes, Laboratoire de Physiopathologie de la Résorption Osseuse et Thérapie des Tumeurs Osseuses Primitives
EA3822, 44035 Nantes cedex 1
Nantes, F-44035
France


Moriceau Gatien
INSERM, UMR957, Faculté de Médecine, 1 rue Gaston Veil
Université de Nantes, Laboratoire de Physiopathologie de la Résorption Osseuse et Thérapie des Tumeurs Osseuses Primitives
EA3822, 44035 Nantes cedex 1
Nantes, F-44035
France


Gobin Bérengère
INSERM, UMR957, Faculté de Médecine, 1 rue Gaston Veil
Université de Nantes, Laboratoire de Physiopathologie de la Résorption Osseuse et Thérapie des Tumeurs Osseuses Primitives
EA3822, 44035 Nantes cedex 1
Nantes, F-44035
France


Redini Françoise
INSERM, UMR957, Faculté de Médecine, 1 rue Gaston Veil
Université de Nantes, Laboratoire de Physiopathologie de la Résorption Osseuse et Thérapie des Tumeurs Osseuses Primitives
EA3822, 44035 Nantes cedex 1
Nantes, F-44035
France


Heymann Dominique
INSERM, UMR957, Faculté de Médecine, 1 rue Gaston Veil
Université de Nantes, Laboratoire de Physiopathologie de la Résorption Osseuse et Thérapie des Tumeurs Osseuses Primitives
EA3822, 44035 Nantes cedex 1
Nantes, F-44035
France


Li-Chieh Wang
Department of Pediatrics
National Taiwan University Hospital
Taipei
Taiwan ROC


Jyh-Hong Lee
Department of Pediatrics
National Taiwan University Hospital
Taipei
Taiwan ROC


Yao-Hsu Yang
Department of Pediatrics
National Taiwan University Hospital
Taipei
Taiwan ROC


Yu-Tsan Lin
Department of Pediatrics
National Taiwan University Hospital
Taipei
Taiwan ROC


Bor-Luen Chiang
Department of Pediatrics
National Taiwan University Hospital
Taipei
Taiwan ROC


Elena Matteucci
Department of Internal Medicine
University of Pisa,
Pisa
Italy


Ottavio Giampietro
Department of Internal Medicine
University of Pisa,
Pisa
Italy


Roman G. Efremov
M.M. Shemyakin and Yu.A. Ovchinnikov Institute of Bioorganic Chemistry
Russian Academy of Sciences, Ul. Miklukho-Maklaya, 16/10
Moscow V-437
GSP, 117997
Russia


Anton O. Chugunov
M.M. Shemyakin and Yu.A. Ovchinnikov Institute of Bioorganic Chemistry, Department of Bioengineering, Biological Faculty
Russian Academy of Sciences, Ul. Miklukho-Maklaya, 16/10, M.V. Lomonosov Moscow State University, Vorobiovy gory, 119899
Moscow V-437
GSP, 117997
Russia


Timothy V. Pyrkov
M.M. Shemyakin and Yu.A. Ovchinnikov Institute of Bioorganic Chemistry
Russian Academy of Sciences, Ul. Miklukho-Maklaya, 16/10
Moscow V-437
GSP, 117997
Russia


John P. Priestle
Novartis Institute for Biomedical Research, WSJ-350.3.15
CH-4002 Basel
Switzerland


Vladimir M. Pentkovsky
Moscow Institute of Physics and Technology (State University)
Institutskii per., 9, Dolgoprudny
Moscow region, 141700
Russia


Alexander S. Arseniev
M.M. Shemyakin and Yu.A. Ovchinnikov Institute of Bioorganic Chemistry
Russian Academy of Sciences, Ul. Miklukho-Maklaya, 16/10
Moscow V-437
GSP, 117997
Russia


Edgar Jacoby
Novartis Institute for Biomedical Research, WSJ-350.3.15
Basel
CH, 4002
Switzerland


Yuko Tsutsui
Department of Physiology & Biophysics
Case Western Reserve University
Cleveland
Ohio , 44106
USA


Patrick L. Wintrode
Department of Physiology & Biophysics
Case Western Reserve University
Cleveland
Ohio , 44106
USA


Saher Afshan Shaikh
Beckman Institute
Urbana
IL
USA


Tarun Jain
Daiichi Sankyo India Pharma Pvt. Ltd., Gurgaon
Haryana
India


Gurvisha Sandhu
Leadinvent, Delhi University South Campus
New Delhi
India


Anjali Soni
Department of Chemistry & Supercomputing Facility for Bioinformatics & Computational Biology
IIT Delhi
India


Bhyravabhotla Jayaram
Department of Chemistry & Supercomputing Facility for Bioinformatics & Computational Biology & School of Biological Sciences
Indian Institute of Technology, Hauz Khas
New Delhi , 110016
India


Leena Gupta
Division of Medicinal and Process Chemistry
Central Drug Research Institute
Lucknow, 226001
India


Archna Talwar
Department of Chemistry
Isabella Thouborn P.G College
Lucknow, 226001
India


P.M.S. Chauhan
Division of Medicinal and Process Chemistry
Central Drug Research Institute,
Lucknow, 226001
India


Vaijayanti A. Kumar
Organic Chemistry Division National Chemical Laboratory
Pune , 411008
India


Catalina Alarcón de la Lastra
Departamento de Farmacología, Facultad de Farmacia
Universidad de Sevilla
Spain


Isabel Villegas Lama
Departamento de Farmacología, Facultad de Farmacia
Universidad de Sevilla
Spain


Marina Sánchez-Fidalgo
Departamento de Farmacología, Facultad de Farmacia
Universidad de Sevilla
Spain




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