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Mini-Reviews
in Medicinal Chemistry
ISSN: 1389-5575
Mini-Reviews in Medicinal
Chemistry
Volume 9, Number 1, January 2009
Contents
Acne in the Adult Pp. 1-10
A. Ascenso and H. Cabral Marques
[Abstract] [Full
Text Article] [PMID:
19149656 PubMed - indexed for MEDLINE]
Cannabinoid Type 2 Receptor as a Target
for Chronic-Pain Pp. 11-25
Massimiliano Beltramo
[Abstract] [Full
Text Article] [PMID:
19149657 PubMed - indexed for MEDLINE]
Helicobacter Pylori, Zinc and Iron in
Oxidative Stress-Induced Injury of Gastric Mucosa Pp.
26-30
J. Dovhanj, K. Kljaic, K. Dodig-C´urkovic,
M. C´urkovic, M. Volarevic and K. Marjanovic
[Abstract] [Full
Text Article] [PMID:
19149658 PubMed - indexed for MEDLINE]
Distribution and Biological Activities
of the Flavonoid Luteolin Pp. 31-59
Miguel López-Lázaro
[Abstract] [Full
Text Article] [PMID:
19149659 PubMed - indexed for MEDLINE]
NF-κB:
The Inducible Factors of HIV-1 Transcription and their Inhibitors
Pp. 60-69
Yu Mingyan, Liu Xinyong and Erik
De Clercq
[Abstract] [Full
Text Article] [PMID:
19149660 PubMed - indexed for MEDLINE]
Oncomirs: From Tumor Biology to Molecularly
Targeted Anticancer Strategies Pp. 70-80
Simone Mocellin, Sandro Pasquali and
Pierluigi Pilati
[Abstract] [Full
Text Article] [PMID:
19149661 PubMed - indexed for MEDLINE]
α-Halogenoacrylic
Derivatives of Antitumor Agents Pp. 81-94
Romeo Romagnoli, Pier Giovanni Baraldi,
Olga Cruz-Lopez, Carlota Lopez-Cara and Delia Preti
[Abstract] [Full
Text Article] [PMID:
19149662 PubMed - indexed for MEDLINE]
Genesis of Dihydropyrimidinone Calcium
Channel Blockers: Recent Progress in Structure-Activity Relationships
and Other Effects Pp. 95-106
K. Singh, D. Arora, K. Singh and S. Singh
[Abstract] [Full
Text Article] [PMID:
19149663 PubMed - indexed for MEDLINE]
Fighting Against Leishmaniasis: Search
of Alkaloids as Future True Potential Anti-Leishmanial Agents
Pp. 107-123
Bhuwan B. Mishra, Rakesh K. Singh, A. Srivastava, V.J. Tripathi
and Vinod K. Tiwari
[Abstract] [Full
Text Article] [PMID:
19149664 PubMed - indexed for MEDLINE]
Prodrug Designing of NSAIDs Pp.
124-139
Parmeshwari K. Halen, Prashant R. Murumkar,
Rajani Giridhar and Mange Ram Yadav
[Abstract] [Full
Text Article] [PMID:
19149665 PubMed - indexed for MEDLINE]
Abstracts
[Back to top]
[PMID:
19149656 PubMed - indexed for MEDLINE]
Acne in the Adult
A. Ascenso and H. Cabral Marques
[Full
Text Article]
This paper is a general overview that contributes for
the knowledge systematization concerning the characteristics
of the acne in the adult, its prevalence, causes, diagnosis,
classification and drugs available for treatment. The reference
therapy is the combination between topical retinoids and oral
antibiotics. Oral isotretinoin is still the only available
therapy that may modify the different acne physiopathologic
factors and therefore it is the standard treatment for severe
acne. The importance of the acne treatment in the adult should
be enhanced as it can also lead to symptoms of serious
depression and anxiety.
[Back to top]
[PMID:
19149657 PubMed - indexed for MEDLINE]
Cannabinoid Type 2 Receptor as a Target for Chronic - Pain
Massimiliano Beltramo
[Full
Text Article]
Availability of selective pharmacological tools enabled
a great advance of our knowledge of cannabinoid receptor 2
(CB2) role in pathophysiology. In particular CB2 emerged as
an interesting target for chronic pain treatment as demonstrated
by several studies on inflammatory and neuropathic preclinal
pain models. The mechanisms at the basis of CB2-mediated analgesia
are still controversial but data are pointing out in two main
directions: an effect on inflammatory cells and/or an action
on nociceptors and spinal cord relay centers. In this review
will be described the second messenger pathways activated
by CB2 agonists, the data underpinning the analgesic profile
of CB2 selective agonists and the mechanisms invoked to explain
their analgesic action. Finally the ongoing clinical trials
and the potential issues for the development of a CB2 agonist
drug will be examined.
[Back to top]
[PMID:
19149658 PubMed - indexed for MEDLINE]
Helicobacter Pylori, Zinc and Iron in Oxidative Stress-Induced
Injury of Gastric Mucosa
J. Dovhanj, K. Kljaic, K. Dodig-C´urkovic,
M. C´urkovic, M. Volarevic and K. Marjanovic
[Full
Text Article]
A number of study have suggested a relationship between
Helicobacter pylori infection and oxidative stress in the
gastric epithelium. The oxidant- induced changes in zinc,
iron, and vitamin C increase susceptibility to oxidative injury.
Understanding of pathophysiologic mechanisms may provide new
therapeutic strategies in treatment of oxidative injury of
mucosa .
[Back to top]
[PMID:
19149659 PubMed - indexed for MEDLINE]
Distribution and Biological Activities of the Flavonoid Luteolin
Miguel López-Lázaro
[Full
Text Article]
Epidemiological evidence suggests that flavonoids may
play an important role in the decreased risk of chronic diseases
associated with a diet rich in plant-derived foods. Flavonoids
are also common constituents of plants used in traditional
medicine to treat a wide range of diseases. The purpose of
this article is to summarize the distribution and biological
activities of one of the most common flavonoids: luteolin.
This flavonoid and its glycosides are widely distributed in
the plant kingdom; they are present in many plant families
and have been identified in Bryophyta, Pteridophyta, Pinophyta
and Magnoliophyta. Dietary sources of luteolin include, for
instance, carrots, peppers, celery, olive oil, peppermint,
thyme, rosemary and oregano. Preclinical studies have shown
that this flavone possesses a variety of pharmacological activities,
including antioxidant, anti-inflammatory, antimicrobial and
anticancer activities. The ability of luteolin to inhibit
angiogenesis, to induce apoptosis, to prevent carcinogenesis
in animal models, to reduce tumor growth in vivo
and to sensitize tumor cells to the cytotoxic effects of some
anticancer drugs suggests that this flavonoid has cancer chemopreventive
and chemotherapeutic potential. Modulation of ROS levels,
inhibition of topoisomerases I and II, reduction of NF-kappaB
and AP-1 activity, stabilization of p53, and inhibition of
PI3K, STAT3, IGF1R and HER2 are possible mechanisms involved
in the biological activities of luteolin.
[Back to top]
[PMID:
19149660 PubMed - indexed for MEDLINE]
NF-κB:
The Inducible Factors of HIV-1 Transcription and their Inhibitors
Yu Mingyan, Liu Xinyong and Erik
De Clercq
[Full
Text Article]
NF-kappaB (NF-κB),
the transcription factors of HIV-1, play an important role
in triggering HIV transcription. The inhibition of NF-κB
activation and their signaling pathway offers a potential
anti-HIV therapy strategy. This review reports the mode of
action of NF-κB
in triggering HIV-1 transcription and the status of the inhibitors.
[Back to top]
[PMID:
19149661 PubMed - indexed for MEDLINE]
Oncomirs: From Tumor Biology to Molecularly Targeted Anticancer
Strategies
Simone Mocellin, Sandro Pasquali and
Pierluigi Pilati
[Full
Text Article]
Deregulation of microRNA (miRNA) promotes carcinogenesis,
as these molecules can act as oncogenes or tumor suppressor
genes. Here we provide an overview of miRNA biology, discuss
the most recent findings on miRNA and cancer development/progression,
and report on how tumor-related miRNAs (oncomirs) are being
used to develop novel cancer specific therapeutic approaches.
[Back to top]
[PMID:
19149662 PubMed - indexed for MEDLINE]
α-Halogenoacrylic
Derivatives of Antitumor Agents
Romeo Romagnoli, Pier Giovanni Baraldi,
Olga Cruz-Lopez, Carlota Lopez-Cara and Delia Preti
[Full
Text Article]
In this review article we have reported a series of hybrid
compounds characterized by the presence of a α-halogenocryloyl
alkylating moiety of low chemical reactivity, linked to known
antitumor agents or their active moieties. Among them, brostallicin
(PNU-166196), was selected for clinical development and is
now undergoing Phase II studies in patients with advanced
or metastatic soft tissue sarcoma.
[Back to top]
[PMID:
19149663 PubMed - indexed for MEDLINE]
Genesis of Dihydropyrimidinone Calcium Channel Blockers: Recent
Progress in Structure-Activity Relationships and Other Effects
K. Singh, D. Arora, K. Singh and S. Singh
[Full
Text Article]
In the armamentarium of calcium channel blockers appropriately
functionalized 3,4-dihydropyrimidin-2(1H)-ones have
received considerable attention in recent past owing to their
structural similarity with 1,4-dihydropyridine based drugs.
In this review, we highlight detailed investigations in the
calcium channel blocking and other activities of this category
of compounds as well as trace their genesis from 1,4-dihydropyridine
based drugs.
[Back to top]
[PMID:
19149664 PubMed - indexed for MEDLINE]
Fighting Against Leishmaniasis: Search of Alkaloids as Future
True Potential Anti-Leishmanial Agents
Bhuwan B. Mishra, Rakesh K. Singh, A. Srivastava,
V.J. Tripathi and Vinod K. Tiwari
[Full
Text Article]
Leishmaniasis, a group of tropical diseases caused by
protozoan parasites of genus Leishmania, is a major
health problem worldwide that affects millions of people especially
in the developing nations. Generic pentavalent antimonials
have been the mainstay for therapy in the endemic regions
due to efficacy and cost effectiveness, but the growing incidence
of their resistance has seriously hampered their use. In many
cases the drugs employed for the treatment are toxic, marginally
effective, given by injection and, compromised by the development
of resistance. Therefore, the development of new mechanism
based safe, effective and affordable chemotherapeutic agents
to fight leishmaniasis would be an urgent priority research.
The recent researches focused on natural products have shown
a wise way to get a true and potentially rich source of drug
candidates against leishmaniasis, where alkaloids have been
found more effective. The present review briefly illustrates
an account on current status of leishmaniasis, life cycle
of parasites and biology, synergy of the disease with HIV,
therapeutic options available to cure this disease and, highlights
why natural products especially alkaloids as folk medicines
are so important? Additionally, the outlines for the leishmanicidal
activities of various alkaloids including indole, quinoline,
isoquinoline, pyrimidine-β-carboline,
steroidal and diterpene alkaloids from various plants as well
as alkaloids from marine sources have been provided with their
mechanistic studies.
[Back to top]
[PMID:
19149665 PubMed - indexed for MEDLINE]
Prodrug Designing of NSAIDs
Parmeshwari K. Halen, Prashant R. Murumkar,
Rajani Giridhar and Mange Ram Yadav
[Full
Text Article]
Non-steroidal anti-inflammatory drugs (NSAIDs), commonly
used for the treatment of chronic inflammatory diseases suffer
from several undesired side effects, the most important being
gastrointestinal (GI) irritation and ulceration. The prodrug
designing is one of the several strategies used to overcome
this drawback. The rationale behind the prodrug concept is
to achieve temporary blockade of the free carboxylic group
present in the NSAIDs till their systemic absorption. In this
paper, a review on the concept of prodrugs designing of NSAIDs
to improve their efficacy and reduce the toxicity is being
presented.
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