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- Volume 17, Issue 9, 2017
Mini Reviews in Medicinal Chemistry - Volume 17, Issue 9, 2017
Volume 17, Issue 9, 2017
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Novobiocin Analogs as Potential Anticancer Agents
Authors: Angelika Dlugosz and Anna JaneckaBackground: The aminocoumarin antibiotic, novobiocin, is a natural product that inhibits DNA gyrase, a bacterial enzyme involved in cell division. Method: More recently, novobiocin was found to act also on eukaryotic cells by blocking the 90 kDa heat shock protein (Hsp90). Hsp90 is a molecular chaperone, critical for folding, stabilization and activation of many proteins, in particular oncoproteins responsible for cancer Read More
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New Analogues of Mycophenolic Acid
Authors: Agnieszka Siebert, Michal Prejs, Grzegorz Cholewinski and Krystyna DzierzbickaBackground: Mycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. It is a non-competitive and reversible inhibitor of dehydrogenase inosine-5'-monophosphate (IMPDH). This compound belongs to the immunosuppressive drugs used for the prevention of both acute and chronic transplant rejection. Until now, two derivatives of MPA have been used clinically: Read More
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In Situ Intestinal Perfusion in Rodents: Future Perspectives for Application on Absorption Studies and Classification of Drugs
Background: In 1995, the Biopharmaceutics Classification System (BCS) was proposed by Amidon and colleagues as a tool that considers two important parameters regarding drugs: solubility and permeability. Since then, several methods for solubility and permeability studies have been developed for drug delivery and absorption prediction. In recent years, permeability has gained a great highlight and the interaction bet Read More
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An Overview of Bioactive Peptides for in vivo Imaging and Therapy in Human Diseases
Authors: Anna Lucia Tornesello, Maria Lina Tornesello and Franco M. BuonaguroBackground: Radiolabeled peptides, designed to bind with high affinity receptors selectively expressed on cell membranes of different human tissues, represent valuable tools for in vivo imaging of several human diseases. Solid-phase peptide synthesis as well as availability of bifunctional chelating agents and prosthetic groups allows the production and radiolabeling of several peptidebased molecules which are useful to ta Read More
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Recent Advances of Metallocenes for Medicinal Chemistry
Authors: Miguel M. Santos, Pedro Bastos, Isabelle Catela, Karolina Zalewska and Luis C. BrancoBackground: The recent advances for the synthesis and application of different metallocenes for Medicinal Chemistry is reviewed. Objective: This manuscript presents the different metallocene scaffolds, with special emphasis on ferrocene derivatives, and their potential pharmaceutical application. Over the last years, the synthesis of new metallocene compounds and their biological and medicinal effects against some ty Read More
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Recent Updates in Melanocyte Function: The Use of Promising Bioactive Compounds for the Treatment of Hypopigmentary Disorders
Authors: Sharique A. Ali, Ishrat Naaz, Kamal Uddin Zaidi and Ayesha S. AliBackground: Skin pigmentation is a broadly appearing phenomenon in nature which plays an important task of determining the appearance and biology of all vertebrates including human beings. Skin color is a crucial attribute, determined by the synthesis of melanin pigment within melanocytes by the process of melanogenesis and is regulated by many extrinsic as well as intrinsic factors. Tyrosinase catalyzes the ke Read More
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Synthesis and Study of Analgesic and Anti-inflammatory Activities of Amide Derivatives of Ibuprofen
Authors: Abbas Ahmadi, Mohsen Khalili, Zahra Olama, Shirin Karami and Babak Nahri-NiknafsNonsteroidal anti-inflammatory drugs (NSAIDs) are among the most widely used drugs worldwide and represent a mainstay in the therapy of acute and chronic pain and inflammation. The traditional NSAIDs like ibuprofen (I) contain free carboxylic acid group which can produce gastrointestinal (GI) damage for long-term use. Objective: In order to obtain the novel NSAIDs with less side effects; carboxylic acid moiety has been mo Read More
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Green Synthesis and Molecular Docking of Thiazolyl-thiazole Derivatives as Potential Cytotoxic Agents
Authors: Sobhi M. Gomha, Mohamad R. Abdelaziz, Hassan M. Abdel-Aziz and Shaimaa A. HassanMethod: A series of novel thiazole derivatives were synthesized in a good yield via reaction of 2-(1-(4-methyl-2-phenylthiazol-5-yl)ethylidene)hydrazine carbothioamide with hydrazonoyl halides. The reaction was performed in the presence of DABCO as an organocatalyst in short reaction times, easy workup, good to excellent yields. The structure of the newly synthesized products was elucidated via element Read More
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Volumes & issues
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Volume 25 (2025)
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Volume 24 (2024)
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Volume 23 (2023)
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Volume 22 (2022)
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Volume 21 (2021)
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Volume 20 (2020)
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Volume 19 (2019)
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Volume 18 (2018)
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Volume 17 (2017)
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Volume 16 (2016)
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Volume 15 (2015)
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Volume 14 (2014)
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Volume 13 (2013)
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Volume 12 (2012)
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Volume 11 (2011)
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Volume 10 (2010)
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Volume 9 (2009)
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Volume 8 (2008)
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Volume 7 (2007)
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Volume 6 (2006)
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Volume 5 (2005)
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Volume 4 (2004)
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Volume 3 (2003)
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Volume 2 (2002)
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Volume 1 (2001)
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