Mini-Reviews in Medicinal Chemistry

ISSN: 1389-5575

Mini-Reviews in Medicinal Chemistry
Volume 10, Number 1, January 2010

Contents


Biological Activities of 2-Styrylchromones Pp. 1-7
A. Gomes, M. Freitas, E. Fernandes and J.L.F.C. Lima
[Abstract] [Full text article]


Gastrin: An Acid-Releasing, Proliferative and Immunomodulatory Peptide? Pp. 8-19
S. Calatayud, Á. Álvarez and V.M. Víctor
[Abstract] [Full text article]


Current and Novel Therapies for Hepatitis B Virus Infection Pp. 20-31
K. Sato and M. Mori
[Abstract] [Full text article]


Latest Advancements on Serotonin and Dopamine Transporters in Lymphocytes Pp. 32-40
D. Marazziti, G. Consoli, I. Masala, M.C. Dell’Osso and S. Baroni
[Abstract] [Full text article]


Lycorine and its Derivatives for Anticancer Drug Design Pp. 41-50
D. Lamoral-Theys, C. Decaestecker, V. Mathieu, J. Dubois, A. Kornienko, R. Kiss, A. Evidente and L. Pottier
[Abstract] [Full text article]


Polyketides from Marine Dinoflagellates of the Genus Prorocentrum, Biosynthetic Origin and Bioactivity of Their Okadaic Acid Analogues Pp. 51-61
W. Hu, J. Xu, J. Sinkkonen and J. Wu
[Abstract] [Full text article]


Progress of Bis(heteroaryl)piperazines (BHAPs) as Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) against Human Immunodeficiency Virus Type 1 (HIV-1) Pp. 62-72
Hui Xu
[Abstract] [Full text article]


Knocking Down Gene Expression with Dendritic Vectors Pp. 73-86
M. Raviña, P. Paolicelli, B. Seijo and A.Sanchez
[Abstract] [Full text article]


Peptides for In Vivo Target-Specific Cancer Imaging Pp. 87-97
G. Ferro-Flores, F. de M. Ramírez, L. Meléndez-Alafort and C.L. Santos-Cuevas
[Abstract] [Full text article]




Abstracts

[Back to top] [Full text article]
Biological Activities of 2-Styrylchromones
A. Gomes, M. Freitas, E. Fernandes and J.L.F.C. Lima

2-Styrylchromones (2-SC) are chromone derivatives characterized by the attachment of a styryl group to the 2-position of the chromone structure. The 2-styrylchromone structure has been demonstrated to bear important biological activities such as antiallergic, antitumor, affinity and selectivity for A3 adenosine receptors, antiviral, antioxidant and anti-inflammatory. The aim of the present paper was to review the available information on this field.


[Back to top] [Full text article]
Gastrin: An Acid-Releasing, Proliferative and Immunomodulatory Peptide?
S. Calatayud, Á. Álvarez and V.M. Víctor

Gastrin release is affected by gastric inflammatory conditions. Antral G cells respond to inflammatory mediators by increasing gastrin secretion. Accumulating experimental evidence suggests that gastrin exerts immunomodulatory and proinflammatory effects. Gastrin could be a contributing factor to these pathologies, which may constitute a new justification for pharmacological blockade of gastrin action.


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Current and Novel Therapies for Hepatitis B Virus Infection
K. Sato and M. Mori

Many therapeutic reagents for hepatitis B virus infection have established efficacy in goals such as alanine aminotransferase normalization, hepatitis B virus DNA suppression, HBeAg seroconversion, histological improvement, and reduce disease progression. However, it is not established that the efficacy of these reagents for the long-term survival and prevention of hepatocellular carcinoma although recent meta-analyses have also shown antiviral therapy to be efficacious. This article reviews the current status and innovative new options for antiviral therapy for hepatitis B and also discusses the various mechanisms of action for each drug, the results of clinical studies for each therapy, and the problems yet to be solved with respect to hepatitis B treatment.


[Back to top] [Full text article]
Latest Advancements on Serotonin and Dopamine Transporters in Lymphocytes
D. Marazziti, G. Consoli, I. Masala, M.C. Dell’Osso and S. Baroni

Different data show that circulating lymphocytes possess functional serotonin and dopamine transporters (SERT and DAT, respectively). This papers aims to review most of the available literature on this topic, while highlighting the possible role of SERT and DAT, as well as that of their substrates including antidepressants on the immune system.


[Back to top] [Full text article]
Lycorine and its Derivatives for Anticancer Drug Design
D. Lamoral-Theys, C. Decaestecker, V. Mathieu, J. Dubois, A. Kornienko, R. Kiss, A. Evidente and L. Pottier

Amaryllidaceae alkaloids are extensively studied for their biological activities in several pharmaceutical areas, including, for example, Alzheimer’s disease for which galanthamine has already reached the market. Among this chemical family, lycorine displays very promising anti-tumor properties. This review first focuses on the chemical diversity of natural and synthetic analogues of lycorine and their metabolites, and then on mechanisms of action and biological targets through which lycorine and its derivatives display their anti-tumor activity. Our analysis of the structure-activity relationships of this family of compounds highlights the existence of various potential leads for the development of novel anti-cancer agents.


[Back to top] [Full text article]
Polyketides from Marine Dinoflagellates of the Genus Prorocentrum, Biosynthetic Origin and Bioactivity of Their Okadaic Acid Analogues
W. Hu, J. Xu, J. Sinkkonen and J. Wu

Marine dinoflagellates of the genus Prorocentrum are famous for the production of okadaic acid (OA) and its analogues. This review covers first the source, chemistry and bioactivity of polyketides from Prorocentrum species. Then recent advances in the studies of biosynthetic origin of OA and its analogues are included. Moreover, the pharmacophore for the selective inhibition of OA to protein phosphatases types 1 (PP1) and 2A (PP2A) is highlighted.


[Back to top] [Full text article]
Progress of Bis(heteroaryl)piperazines (BHAPs) as Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) against Human Immunodeficiency Virus Type 1 (HIV-1)
Hui Xu

Since the first case of acquired immunodeficiency syndrome (AIDS) was reported in 1981, AIDS, as the global disease affecting 33.2 million people in 2007, has always been an unsolved problem worldwide. Reverse transcriptase (RT) is a crucial enzyme in the life cycle of human immunodeficiency virus type 1 (HIV-1), and thereby has been the prime drugs target for antiretroviral (ARV) therapy against AIDS. To date, two classes of RT inhibitors (RTIs), e.g., nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs), and a lot of compounds tested as RTIs have been described. To our knowledge, bis(heteroaryl)piperazines (BHAPs) have been considered as one class of promising NNRTIs, such as structurally and chemically related NNRTI delavirdine, which was approved by the U. S. Food and Drug Administration (FDA) for the treatment of HIV-1 infection in 1997. In this mini-review, we make attempts to report the progress of synthesis and structure–activity relationship (SAR) of BHAPs, in the meantime, the synergistic inhibition of HIV-1 replication by combining delavirdine with other HIV-1 inhibitors is also discussed. It will pave the way for the design and development of BHAPs as anti-HIV-1 agents in AIDS chemotherapy in the future.


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Knocking Down Gene Expression with Dendritic Vectors
M. Raviña, P. Paolicelli, B. Seijo and A.Sanchez

The aim of this review is to provide the reader with an overview on the potential of dendritic polymers in the antisense delivery technology. Special emphasis has been placed on the different types of dendritic structures that have been reported and the modifications performed to increase their efficacy and safety. Therefore the advances made in their chemistry and how it has been adapted to meet the specific requirements of the antisense delivery technology are reviewed and discussed.


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Peptides for In Vivo Target-Specific Cancer Imaging
G. Ferro-Flores, F. de M. Ramírez, L. Meléndez-Alafort and C.L. Santos-Cuevas

Molecular imaging comprises non-invasive monitoring of functional and spatiotemporal processes at molecular and cellular levels in living systems. Advanced imaging techniques can monitor such processes. Peptide receptors over-expressed in tumours can be targeted by peptides conjugated to radionuclides, near-infrared fluorochromes, metallic nanoparticles or quantum dots for target-specific cancer imaging.