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- Volume 22, Issue 12, 2016
Current Pharmaceutical Design - Volume 22, Issue 12, 2016
Volume 22, Issue 12, 2016
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Mycobacterium tuberculosis-Secreted Tyrosine Phosphatases as Targets Against Tuberculosis: Exploring Natural Sources in Searching for New Drugs
Tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis (Mtb), which primarily affects the respiratory tract. Combinations of drugs are used for therapeutic synergism and to prevent the emergence of drug resistant strains, but even first- or secondchoice drugs present some disadvantages, such as significant side effects and the need for long duration of treatments. Thus, new strategies for TB control a Read More
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An Update on Natural Products with Carbonic Anhydrase Inhibitory Activity
Authors: Anastasia Karioti, Fabrizio Carta and Claudiu T. SupuranCarbonic anhydrases (CAs, EC 4.2.1.1) catalyze the fundamental reaction of CO2 hydration in all living organisms, being actively involved in the regulation of a plethora of patho/physiological processes. They represent a typical example of enzyme convergent evolution, as six genetically unrelated families of such enzymes were described so far. It is more than 70 years that synthetic compounds, mainly sulfonamides, hav Read More
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Synthetic Glycosides and Glycoconjugates of Low Molecular Weight Natural Products
Authors: G. Grynkiewicz and W. SzejaEnzymatically controlled transfer of saccharide moieties constitutes a fundamental biological process, essential for both primary and secondary metabolism. Natural products, including countless glycosides, with a rich tradition of use in ethnopharmacology, remain a prime source of inspiration for medicinal chemistry and molecular pharmacology, but their availability from biological sources is usually scarce, hamperi Read More
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Biomimetic Approaches Towards The Synthesis of Complex Dimeric Natural Products
We present a selection of elegant and diverse biomimetic syntheses of complex natural product dimers. The dimerisation pathways discussed encompass the most prevalent strategies, including: Diels-Alder, Aldol, Mannich, conjugate addition, oxidative, radical and photochemical approaches; each underpinned through rational biosynthetic speculation.
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One Hundred Faces of Cyclopamine
Authors: Valentina Iovine, Mattia Mori, Andrea Calcaterra, Simone Berardozzi and Bruno BottaThe natural steroidal alkaloid cyclopamine has been identified as the first inhibitor of the Hedgehog (Hh) signaling pathway, which is implicated in embryonic development and tumorigenesis, as well as is hyperactivated in cancer stem cells (CSCs). The list of Hh-dependent tumors is steadily growing, and it has been estimated that about 25% of all cancer deaths show signs of aberrant Hh pathway activation. Notably, cyclopa Read More
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Reactivity of Diterpenoid Quinones: Royleanones.
Naturally occurring abietane diterpenoids have been studied over the years and have shown to display a wide range of biological activities. This review covers three main aspects of the abietane-type diterpenoids with hydroxy-p-quinone C ring, designated as royleanones. An overview of 1) the naturally occurrence, 2) chemical features and 3) the biological activities of this abietane group of compounds, including rearranged Read More
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Molecular Recognition of Natural Products by Resorc[4]arene Receptors
This review is aimed at providing an overview of the up-to-now published literature on resorc[4]arene macrocycles exploited as artificial receptors for the molecular recognition of some classes of natural products. A concise illustration of the main synthetic strategies developed to afford the resorc[4]arene scaffold is followed by a report on the principles of the gas-phase investigation of recognition phenomena by mass spect Read More
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Natural Product-Based Antibiotics: Synthesis and SAR-Studies.
More LessEfficient control of the infectious diseases in the era of the emerging bacterial resistance demands consistent development of new antibiotic agents with novel modes of action. With some notable exceptions, the majority of the currently used antibiotics are natural product-derived compounds which were elaborated upon lead structures discovered by screening of various isolates. In this review, we summarized some selected e Read More
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The Therapeutic Aspects of the Endocannabinoid System (ECS) for Cancer and their Development: From Nature to Laboratory
The endocannabinoid system (ECS) is a group of neuromodulatory lipids and their receptors, which are widely distributed in mammalian tissues. ECS regulates various cardiovascular, nervous, and immune system functions inside cells. In recent years, there has been a growing body of evidence for the use of synthetic and natural cannabinoids as potential anticancer agents. For instance, the CB1 and CB2 receptors are Read More
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Synthesis of Tetracyclic Diterpenoids with Pharmacologic Relevance
Authors: Miroslav Sisa and Tomas VanekThis review covers the chemical reactions, synthesis, and biological activities of tetracyclic diterpenoids including ent-kauranes, ent-beyeranes, ent-atisanes, ingenanes, tyglianes, stemodanes, stemaranes, sordarin, salvileucalin B, harringtonolide and hainanolidol. It comprises of the un-reviewed references from the year 2000.
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The Pictet-Spengler Reaction Still on Stage
Today, in spite of being older than a century (born in 1911), the Pictet-Spengler two component reaction (PS-2CR) is still one of the most popular reactions, not only for the synthesis of tetrahydroisoquinolines (THIQs), tetrahydro-β-carbolines (THBCs), or more complex structures containing these two privileged moieties, but also for the construction of novel scaffolds, available for structure-activity relationship (SAR) studies a 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)
- Issue 46
- Issue 45
- Issue 44
- Issue 43
- Issue 41
- Issue 42
- Issue 40
- Issue 39
- Issue 38
- Issue 37
- Issue 36
- Issue 35
- Issue 34
- Issue 32
- 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
- Issue 8
- Issue 7
- Issue 6
- Issue 5
- Issue 4
- Issue 33
- Issue 3
- Issue 2
- Issue 1
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Volume 21 (2015)
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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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