Recent Advances in Medicinal Chemistry

Volume 1

by

Atta-ur-Rahman, Muhammad Iqbal Choudhary, George Perry

DOI: 10.2174/97816080579621140101
eISBN: 978-1-60805-796-2, 2014
ISBN: 978-1-60805-797-9
ISSN: 2215-0722 (Print)



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Recent advances in Medicinal Chemistry is a book series focused on leading-edge...[view complete introduction]

Table of Contents

Foreword

- Pp. i-ii (2)

Daniel C. Hoessli

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Preface

- Pp. iii

George Perry

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List of Contributors

- Pp. iv-xi (8)

Atta-ur-Rahman, Muhammad Iqbal Choudhary and George Perry

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New Functions of Old Drugs: Aureolic Acid Group of Anti- Cancer Antibiotics and Non-Steroidal Anti-Inflammatory Drugs

- Pp. 3-55 (53)

Hirak Chakraborty, Pukhrambam Grihanjali Devi, Munna Sarkar and Dipak Dasgupta

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Updated Report on a Novel Mercaptopyruvate Sulfurtransferase Thioredoxin-Dependent Redox-Sensing Molecular Switch: A Mechanism for the Maintenance of Cellular Redox Equilibrium

- Pp. 56-72 (17)

Noriyuki Nagahara

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Characterization of Inorganic Nanomaterials as Therapeutic Vehicles

- Pp. 73-98 (26)

Tatsuya Murakami, Masako Yudasaka, Sumio Iijima and Kunihiro Tsuchida

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Aromatase Inhibitors: A New Reality for the Adjuvant Endocrine Treatment of Early-Stage Breast Cancer in Postmenopausal Women

- Pp. 99-130 (32)

Colozza Mariantonietta, Minenza Elisa, Nunzi Martina, Sabatini Silvia, Dinh Phuong, Califano Raffaele and De Azambuja Evandro

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Bacterial FabH: Towards the Discovery of New Broad-Spectrum Antibiotics

- Pp. 131-158 (28)

Yunierkis Pérez-Castillo, Matheus Froeyen, Ann Nowé and Miguel Ángel Cabrera-Pérez

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Tannins and their Influence on Health

- Pp. 159-208 (50)

Kateřina Macáková, Vít Kolečkář, Lucie Cahlíková, Jakub Chlebek, Anna Hošťálková, Kamil Kuča, Daniel Jun and Lubomír Opletal

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Rho-GTPases and Statins: A Potential Target and a Potential Therapeutic Tool Against Tumors?

- Pp. 209-245 (37)

Ivana Campia, Sophie Doublier, Elisabetta Aldieri, Amalia Bosia, Dario Ghigo and Chiara Riganti

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Carotenoids that are Involved in Prostate Cancer Risk

- Pp. 246-271 (26)

Charles Y.F. Young, K.V. Donkena, H.-Q. Yuan, M.-L. He and J.-Y. Zhang

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Preclinical Studies of Saponins for Tumor Therapy

- Pp. 272-302 (31)

Christopher Bachran, Silke Bachran, Mark Sutherland, Diana Bachran and Hendrik Fuchs

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Pharmacological Neuroprotection for Acute Spinal Cord Injury

- Pp. 303-331 (29)

Humberto Mestre, Ricardo Balanza and Antonio Ibarra

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HPLC and its Essential Role in the Analysis of Tricyclic Antidepressants in Biological Samples

- Pp. 332-380 (49)

V.F. Samanidou, M.K. Nika and I.N. Papadoyannis

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Gene Expression Profiles in Breast Cancer to Identify Estrogen Receptor Target Genes

- Pp. 381-403 (23)

Maria Aparecida Nagai and Brentani M.M.

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Trans-Plasma Membrane Electron Transport in Human Blood Platelets: An Update

- Pp. 404-432 (29)

Luciana Avigliano, I. Savini, M. V. Catani and D. Del Principe

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Role of Intermediate States in Protein Folding and Misfolding

- Pp. 433-455 (23)

Roberto Santucci, Fabio Polticelli, Federica Sinibaldi and Laura Fiorucci

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Index

- Pp. 456-469 (14)

Atta-ur-Rahman, Muhammad Iqbal Choudhary and George Perry

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Foreword

The 1st volume of “Recent Adances in Medicinal Chemistry” offers a very rich panorama of authoritative reviews covering old , as well as new, unexpected issues. Once established, drugs rarely become undisputed therapeutic weapons against one specific kind of disease and reevaluations of such drugs needs to be carried out regularly. The present volume does indeed provide a number of such reevaluations, as, for instance, the aureolic acid group of anti-cancer drugs and the non-steroidal anti-inflammatory drugs (Chakraborty et al.). In the ever-expanding collection of anti-cancer drugs, the aromatase inhibitor tamoxifen has long been the gold standard to treat hormone-receptor positive, early forms of breast cancer. However, new generation aromatase inhibitors show definitive advantages over tamoxifen and these advantages are discussed by Colozza et al. On the same subject, the precise identification of estrogen receptors is becoming of prime importance in deciding which inhibitor to use (Nagai M. and Brentani M.M.).

The already widespread utilization of statins may further extend to neoplastic diseases, as statins were shown to inhibit Rho-GTPases (often hyperexpressed in tumors) by inhibiting the synthesis of their prenyl groups (C. Riganti).

New molecules such as plant glycosides (saponins) display anti-tumor activity that could be utilized in combination with existing anti-tumor compounds (C. Bachran et al.).

Chemoprevention undoubtedly offers effective means to delay or altogether prevent the development of most diseases. Macáková et al., discuss extensively the protective effects of tannins, a group of natural polyphenols with anti-oxidant activity. On the same line, Young et al., consider the activity of carotenoids in the chemoprevention of prostate cancer.

Delivery of pharmacologically active compounds and drugs was always of importance to ascertain that active molecules preferentially reach their target cells or tissues, and Murakami et al., review the recent advances in nanoparticular vehicles.

Antimicrobials are acutely needed to treat bacterial diseases, especially those caused by micro-organisms resistant to existing antibiotics. Pérez-Castillo et al., review how the 3-D structure of the targeted bacterial enzyme may be utilized to design new antibiotics.

Enzymatic activities are essential to carry out biological functions and their perturbations are often caused by disturbances of the intracellular redox potential. In this respect, Nagahara reports on the mechanisms to maintain the cellular redox equilibrium. The plasma membrane redox system is an important property of plasma membranes. In particular, Avigliano et al., review the plasma membrane redox system of blood platelets and the role of anti-oxidant vitamins in this context.

The acute spinal cord injuries (traumatic) represent an unsolved problem in medicine. H. Mestre et al., elaborate on the ongoing efforts made to develop a pharmacological way to ensure the neuroprotection of the injured spine.

The precise assessement of the levels of pharmacologically active molecules in patients needs to be met and Samanidou et al., review how HPLC (high-performance liquid chromatography) can be utilized to monitor the levels of tricyclic anti-depressants.

Lastly, Santucci et al., review chosen instances where misfolded proteins cause pathologies, namely how non-native forms of cytochrome c are involved in apoptosis triggering and participate in amyloid formation.

By the variety of subjects reviewed dealing with chemoprevention and treatment of common diseases, the changing scope of action of medicinal chemistry is illustrated in this volume. It is indeed quite possible that our physiology and pathologies also evolve comcomittantly with the drugs we take to prevent or treat diseases.

Daniel C. Hoessli
Panjwani Center for Molecular Medicine and Drug Research
International Center for Chemical and Biological Sciences
University of Karachi, Karachi-75270
Pakistan


Preface

Consolidation, failure of high throughput approaches and rationale design to deliver as promised, and uncertainty of future finances have drawn industry away from innovation to reformulation and repackaging. In this new world, academic research plays an even greater role in drug development, whether built on natural products or novel insights. Blurring of the lines between the traditional fields of chemistry and biology offers opportunities for new discoveries. In this milieu “Recent Advances in Medicinal Chemistry” will find a welcome home.

George Perry
College of Sciences
University of Texas at San Antonio
San Antonio
Texas
USA

List of Contributors

Editor(s):
Atta-ur-Rahman
Honorary Life Fellow
Kings College
University of Cambridge
UK


Muhammad Iqbal Choudhary
H.E.J. Research Institute of Chemistry
International Center for Chemical and Biological Sciences
University of Karachi
Karachi
Pakistan


George Perry
Department of Biology
University of Texas
San Antonio
Texas
USA




Contributor(s):
Amalia Bosia
Department of Oncology, Biology and Biochemistry
Research Center on Experimental Medicine (CeRMS)
University of Torino, Via Santena 5/bis
Torino, 10126
Italy


Ann Nowé
Computational Modeling Lab (CoMo)
Department of Computer Sciences
Faculty of Sciences
VrijeUniversiteit Brussel, Pleinlaan 2
Brussel, B-1050
Belgium


Anna Hošťálková
Department of Pharmaceutical Botany and Ecology
ADINACO Research Group, Faculty of Pharmacy
Charles University
Hradec Kralove
Czech Republic
/
Centro de Investigación del Proyecto CAMINA A.C.
Mexico City
Mexico


Antonio Ibarra
Facultad de Ciencias de la Salud
Universidad Anáhuac México Norte
Huixquilucan
Estado de México
Mexico


Charles Y.F. Young
Departments of Urology and Biochemistry and Molecular Biology
Mayo Clinic College of Medicine
Mayo Clinic
Rochester
Minnesot
USA


Chiara Riganti
Department of Oncology, Biology and Biochemistry
Research Center on Experimental Medicine (CeRMS)
University of Torino, Via Santena 5/bis
Torino, 10126
Italy


Christopher Bachran
Institut für Laboratoriumsmedizin
Klinische Chemie und Pathobiochemie
Charité – Universitätsmedizin Berlin
Campus Benjamin Franklin
Hindenburgdamm 30
Berlin, D-12200
Germany


D. Del Principe
Department of Experimental Medicine & Surgery
University of Rome ‘Tor Vergata’
Italy


Daniel Jun
Centre of Advanced Studies
Faculty of Military Health Sciences
University of Defence
Hradec Kralove
Czech Republic


Dario Ghigo
Department of Oncology, Biology and Biochemistry
Research Center on Experimental Medicine (CeRMS)
University of Torino, Via Santena 5/bis
Torino, 10126
Italy


Diana Bachran
Institut für Laboratoriumsmedizin
Klinische Chemie und Pathobiochemie
Charité – Universitätsmedizin Berlin
Campus Benjamin Franklin
Hindenburgdamm 30
Berlin, D-12200
Germany


Dipak Dasgupta
Chemical Sciences Division
Biophysics Division
Saha Institute of Nuclear Physics
1/AF Bidhannagar
Kolkata, 700 064
India


E. De Azambuja
Medical Oncology Clinic
Jules Bordet Institute
Boulevard de Waterloo, 125
Brussels, 1000
Belgium


E. Minenza
S.C. Oncologia Medica
Ospedale Civile
Via Santa Lucia 2
Macerata, 62100
Italy


Elisabetta Aldieri
Department of Oncology, Biology and Biochemistry
Research Center on Experimental Medicine (CeRMS)
University of Torino, Via Santena 5/bis
Torino, 10126
Italy


Fabio Polticelli
Dipartimento di Biologia
Università Roma Tre
V.le Marconi 446
Rome, 00146
Italy
/
Dipartimento di Biologia
Università Roma Tre
V.le Marconi 446
Rome, 00146
Italy
/
Istituto Nazionale di Fisica Nucleare
Sezione Rome Tre
Rome, 00146
Italy


Federica Sinibaldi
Dipartimento di Scienze Cliniche e Medicina Traslazionale
Università di Roma ‘Tor Vergata’
Via Montpellier 1
Rome, 00133
Italy


George Perry
College of Sciences
University of Texas at San Antonio
San Antonio
Texas
USA


H.-Q. Yuan
Institute of Biochemistry and Molecular Biology
Medical College
Shandong University
Jinan
People's Republic of China


Hendrik Fuchs
Institut für Laboratoriumsmedizin
Klinische Chemie und Pathobiochemie
Charité – Universitätsmedizin Berlin
Campus Benjamin Franklin
Hindenburgdamm 30
Berlin, D-12200
Germany


Hirak Chakraborty
Department of Biochemistry and Biophysics
University of North Carolina
Chapel Hill
Chapel Hill
NC, 27599
USA


Humberto Mestre
Facultad de Ciencias de la Salud
Universidad Anáhuac México Norte
Huixquilucan
Estado de México
Mexico


I. Savini
Department of Experimental Medicine & Surgery
University of Rome ‘Tor Vergata’
Italy


I.N. Papadoyannis
Laboratory of Analytical Chemistry
Department of Chemistry
Aristotle University of Thessaloniki
Thessaloniki, 541 24
Greece


Ivana Campia
Department of Oncology, Biology and Biochemistry
Research Center on Experimental Medicine (CeRMS)
University of Torino, Via Santena 5/bis
Torino, 10126
Italy


J.-Y. Zhang
Institute of Biochemistry and Molecular Biology
Medical College
Shandong University
Jinan
People's Republic of China


Jakub Chlebek
Department of Pharmaceutical Botany and Ecology
ADINACO Research Group
Faculty of Pharmacy, Charles University
Hradec Kralove
Czech Republic


K.V. Donkena
Departments of Urology and Biochemistry and Molecular Biology
Mayo Clinic College of Medicine
Mayo Clinic
Rochester
Minnesota
USA


Kamil Kuča
Centre of Advanced Studies
Faculty of Military Health Sciences
University of Defence
Hradec Kralove
Czech Republic


Kateřina Macáková
Department of Pharmaceutical Botany and Ecology
ADINACO Research Group, Faculty of Pharmacy
Charles University
Hradec Kralove
Czech Republic


Kunihiro Tsuchida
Division for Therapies against Intractable Diseases
Institute for Comprehensive Medical Science (ICMS)
Fujita Health University
Toyoake
Aichi, 470-1192
Japan


Luciana Avigliano
Department of Experimental Medicine & Surgery
University of Rome ‘Tor Vergata’
Italy


Laura Fiorucci
Dipartimento di Scienze Cliniche e Medicina Traslazionale
Università di Roma ‘Tor Vergata’
Via Montpellier 1
Rome, 00133
Italy


Lubomír Opletal
Department of Pharmaceutical Botany and Ecology
ADINACO Research Group, Faculty of Pharmacy
Charles University
Hradec Kralove
Czech Republic


Lucie Cahlíková
Department of Pharmaceutical Botany and Ecology
ADINACO Research Group, Faculty of Pharmacy
Charles University
Hradec Kralove
Czech Republic


M. Nunzi
S.C. Oncologia Medica
Azienda Ospedaliera
Via Tristano di Joannuccio 1
Terni, 05100
Italy


Maria Aparecida Nagai
Disciplina de Oncologia
Departamento de Radiologia e Oncologia da Faculdade de Medicina da Universidade de São Paulo
Av. Dr. Arnaldo, 455, 4°andar
São Paulo
CEP, 01246-903
Brazil
/
Laboratório de Genética Molecular do Centro de Investigação Translacional em Oncologia
Av. Dr. Arnaldo, 251, 8 andar
São Paulo
CEP, 01246-000
Brazil


M.K. Nika
Laboratory of Analytical Chemistry
Department of Chemistry
Aristotle University of Thessaloniki
Thessaloniki, 541 24
Greece


M.-L. He
Institute of Cancer Research
Life Science School
Tongji University
Shanghai
People's Republic of China


M.M. Brentani
Disciplina de Oncologia
Departamento de Radiologia e Oncologia da Faculdade de Medicina da Universidade de São Paulo
Av. Dr. Arnaldo, 455, 4°andar
São Paulo
CEP, 01246-903
Brazil


M.V. Catani
Department of Experimental Medicine & Surgery
University of Rome ‘Tor Vergata’
Italy


Mariantonietta Colozza
S.C. Oncologia Medica
Azienda Ospedaliera
Via Tristano di Joannuccio 1
Terni, 05100
Italy


Mark Sutherland
University of Bradford
Institute of Cancer Therapeutics
Bradford
West Yorkshire
United Kingdom


Masako Yudasaka
National Institute of Advanced Industrial Science and Technology (AIST)
Nanotube Research Center
Central 5, 1-1-1 Higashi
Tsukuba, 305-8565
Japan


Matheus Froeyen
Laboratory for Medicinal Chemistry
Rega Institute for Medical Research
Katholieke Universiteit Leuven
Minderbroedersstraat 10
Leuven, B-3000
Belgium


Miguel Ángel Cabrera-Pérez
Molecular Simulation & Drug Design Group, Centro de BioactivosQuímicos
Universidad Central de Las Villas
Villa Clara
Santa Clara, 54830
Cuba, USA
/
Engineering Department, Pharmacy and Pharmaceutical Technology Area
Faculty of Pharmacy
University Miguel Hermandez
Plicante, D3550
Spain


Munna Sarkar
Chemical Sciences Division
Biophysics Division
Saha Institute of Nuclear Physics
1/AF Bidhannagar
Kolkata, 700 064
India


Noriyuki Nagahara
Department of Environmental Medicine
Nippon Medical School
1-1-5 Sendagi Bunkyo-ku
Tokyo, 113-8602
Japan


P. Dinh
Medical Oncology Clinic
Jules Bordet Institute
Boulevard de Waterloo, 125
Brussels, 1000
Belgium


Pukhrambam Grihanjali Devi
Department of Chemistry
Imphal College
Imphal
India


R. Califano
Department of Medical Oncology
The Christie NHS Foundation Trust
Wilmslow Road
Manchester, M20 4BX
UK


Ricardo Balanza
Facultad de Ciencias de la Salud
Universidad Anáhuac México Norte
Huixquilucan
Estado de México
Mexico


Roberto Santucci
Dipartimento di Scienze Cliniche e Medicina Traslazionale
Università di Roma ‘Tor Vergata’
Via Montpellier 1
Rome, 00133
Italy


S. Sabatini
S.C. Oncologia Medica
Azienda Ospedaliera
Via Tristano di Joannuccio 1
Terni, 05100
Italy


Silke Bachran
Institut für Laboratoriumsmedizin
Klinische Chemie und Pathobiochemie
Charité – Universitätsmedizin Berlin
Campus Benjamin Franklin
Hindenburgdamm 30
Berlin, D-12200
Germany


Sophie Doublier
Department of Oncology, Biology and Biochemistry
Research Center on Experimental Medicine (CeRMS)
University of Torino
Via Santena 5/bis
Torino, 10126
Italy


Sumio Iijima
National Institute of Advanced Industrial Science and Technology (AIST)
Nanotube Research Center
Central 5, 1-1-1 Higashi
Tsukuba, 305-8565
Japan


Tatsuya Murakami
Division for Therapies against Intractable Diseases
Institute for Comprehensive Medical Science (ICMS)
Fujita Health University
Toyoake
Aichi, 470-1192
Japan


V.F. Samanidou
Laboratory of Analytical Chemistry
Department of Chemistry
Aristotle University of Thessaloniki
Thessaloniki, 541 24
Greece


Vít Kolečkář
Centre of Advanced Studies
Faculty of Military Health Sciences
University of Defence
Hradec Kralove
Czech Republic


Yunierkis Pérez-Castillo
Molecular Simulation & Drug Design Group
Centro de Bioactivos Químicos
Universidad Central de Las Villas
Santa Clara
Villa Clara, 54830
Cuba
/
Laboratory for Medicinal Chemistry
Rega Institute for Medical Research
Katholieke Universiteit Leuven
Minderbroedersstraat 10
Leuven, B-3000
Belgium
/
Computational Modeling Lab (CoMo)
Department of Computer Sciences, Faculty of Sciences
VrijeUniversiteit Brussel
Pleinlaan 2
Brussel, B-1050
Belgium




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