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- Volume 21, Issue 38, 2015
Current Pharmaceutical Design - Volume 21, Issue 38, 2015
Volume 21, Issue 38, 2015
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Synthesis and Pharmacological Effects of the Anti-Cancer Agent 2-Methoxyestradiol
Authors: Eirik Johansson Solum, Oyvind W. Akselsen, Anders Vik and Trond V. HansenThe endogenous steroid 2-methoxyestradiol (2-ME) is a metabolite of 17β-estradiol and its biosynthesis is well established. Moreover, 2-ME is also biosynthesized from estrone. For several years, 2-ME was perceived as an inactive metabolite devoid of any interesting biological activities. Since the late 1980s, a number of biological and pharmacological studies have revealed that 2-ME possesses interesting anti-cancer effects wi Read More
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Xenicane Natural Products: Biological Activity and Total Synthesis
Authors: Leo Betschart and Karl-Heinz AltmannThe xenicanes are a large class of mostly bicyclic marine diterpenoids featuring a cyclononane ring as a common structural denominator. After a brief introduction into the characteristic structural features of xenicanes and some biogenetic considerations, the major focus of this review will be on the various biological activities that have been reported for xenicanes and on efforts towards the total synthesis of these structures. Read More
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“Non-Taxifolin” Derived Flavonolignans: Phytochemistry and Biology
Authors: Christopher S. Chambers, Katerina Valentova and Vladimir krenFlavonolignans are plant natural products, composed of a flavonoid moiety and a lignan (phenylpropanoid) part. Current literature focuses on flavonolignans formed from taxifolin and coniferyl alcohol as e.g. silybin and its congeners from fruit extract from the purple variety of the milk thistle (Silybum marianum) denoted as “silymarin”. This review describes chemistry and biological activity of so far neglected “non-taxifo Read More
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Thapsigargin, Origin, Chemistry, Structure-Activity Relationships and Prodrug Development
Authors: Nhu Thi Quynh Doan and Soren Brogger ChristensenThapsigargin was originally isolated from the roots of the Mediterranean umbelliferous plant Thapsia garganica in order to characterize the skin irritant principle. Characteristic chemical properties and semi-syntheses are reviewed. The biological activity was related to the subnanomolar affinity for the sarco/endoplasmic reticulum calcium ATPase. Prolonged inhibition of the pump afforded collapse of the calcium homeost Read More
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Indolo[2,3-a]quinolizidines and Derivatives: Bioactivity and Asymmetric Synthesis
Authors: Maria Perez, Margarida Espadinha and Maria M. M. SantosCorynantheine alkaloids with a tetracyclic indole[2,3-a]-quinolizidine motif are an important issue in academia and in the life science industries due to their broad bioactivity profile. In particular, the main biological effects described for indoloquinolizidines include analgesic, anti-inflammatory, antihypertensive, and antiarrhythmic activities, as well as inhibition of multiple ion channels, affinity for opioid receptors, and activity ag Read More
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Natural Products and Cancer Stem Cells
The development of modern technologies casts a new light on the natural products as an invaluable source of lead compounds that could guide drug discovery. Cancer stem cells are a subpopulation of cancer cells with a high clonogenic capacity and the ability to reform the parental tumours upon transplantation. They have been proposed to drive tumorigenesis and metastases. In this review, we present the ability of forty-nin Read More
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Heterogeneous Diastereoselective Catalysis - A Powerful Strategy Toward C(15) Stereoselectivity from PGF2α Analogues Structure
Authors: Simona M. Coman and Vasile I. Parvulescumajor trend in fine chemicals and pharmaceuticals is the synthesis of molecules with increased complexity. This trend translates the aim of organic syntheses to conditions in which high degrees of chemo-, regioand stereoselectivity can be provided. In this context, the chemoselective hydrogenation of one functional group in the presence of other reactive groups is a frequently encountered problem in fine chemicals Read More
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Natural Products as Promising Therapeutics for Treatment of Influenza Disease
The influenza virus represents a permanent global health threat because it circulates not only within but also between numerous host populations, thereby frequently causing unexpected outbreaks in animals and humans with a generally unpredictable course of disease and epidemiology. Conventional influenza therapy is directed against the viral neuraminidase protein, which promotes virus release from infected cells, an Read More
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New Approaches With Natural Product Drugs for Overcoming Multidrug Resistance in Cancer
Authors: Jelena Dinic, Ana Podolski-Renic, Tijana Stankovic, Jasna Bankovic and Milica PesicResistance to chemotherapeautic drugs is one of the main obstacles to effective cancer treatment. Multidrug resistance (MDR) is defined as resistance to structurally and/or functionally unrelated drugs, and has been extensively investigated for the last three decades. There are two types of MDR: intrinsic and acquired. Tumor microenvironment selection pressure leads to the development of intrinsic MDR, while acquired re Read More
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From 2D to 3D - a New Dimension for Modelling the Effect of Natural Products on Human Tissue
Authors: Krzysztof Wrzesinski and Stephen J. FeyNatural products, or their synthetic derivatives are a treasure trove to find potential candidates for novel drugs for human treatment. The selection of diamonds from the huge pile of worthless stone is a critical – and difficult - stage in the discovery pipeline. Of all the factors to be considered, perhaps the most important, is that the compound should have the desired effect on the tissue in vivo. Since it is not possible (or ethical) Read More
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Volumes & issues
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Volume 31 (2025)
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Volume 30 (2024)
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Volume 29 (2023)
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Volume 28 (2022)
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Volume 27 (2021)
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Volume 26 (2020)
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Volume 25 (2019)
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Volume 24 (2018)
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Volume 23 (2017)
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Volume 22 (2016)
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Volume 21 (2015)
- Issue 42
- Issue 41
- Issue 40
- Issue 39
- Issue 38
- Issue 37
- Issue 36
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- Issue 33
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- Issue 31
- Issue 30
- Issue 29
- Issue 28
- Issue 27
- Issue 26
- Issue 25
- Issue 24
- Issue 23
- Issue 22
- Issue 21
- Issue 20
- Issue 19
- Issue 18
- Issue 17
- Issue 16
- Issue 15
- Issue 14
- Issue 13
- Issue 12
- Issue 11
- Issue 10
- Issue 9
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- Issue 7
- Issue 6
- Issue 5
- Issue 4
- Issue 3
- Issue 2
- Issue 1
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Volume 20 (2014)
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Volume 19 (2013)
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Volume 18 (2012)
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Volume 17 (2011)
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Volume 16 (2010)
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Volume 15 (2009)
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Volume 14 (2008)
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Volume 13 (2007)
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Volume 12 (2006)
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Volume 11 (2005)
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Volume 10 (2004)
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Volume 9 (2003)
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Volume 8 (2002)
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Volume 7 (2001)
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Volume 6 (2000)
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