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Pharmaceuticals, Volume 10, Issue 3

2017 September - 19 articles

Cover Story: The consolidation of the combretastatin and bisindolylmaleimide templates towards the inclusion of a novel heterocyclic ring has identified a novel indole trimethoxyphenyl aminopyrazole as an anticancer lead. The unique electronic nature of the 5-aminopyrazole moiety allows for regiospecific substitution on different sites of the ring and further expansion to pyrazolotriazinedione and pyrazolopyrimidine bicyclic systems is possible. The antiproliferative activities of the 3,4-diaryl-5-aminopyrazoles were assessed using the NCI-60 cell screen, disclosing the discovery of distinct selectivity profiles towards a number of cell lines. The lead compound 55 is effective at reducing the growth of HOP-92 lung cancer, UO-31 and CAKI-1 renal cancer cells below 20%. View the paper here
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Articles (19)

  • Article
  • Open Access
5 Citations
8,488 Views
25 Pages

Comparison of In Vitro Assays in Selecting Radiotracers for In Vivo P-Glycoprotein PET Imaging

  • Renske M. Raaphorst,
  • Heli Savolainen,
  • Mariangela Cantore,
  • Evita Van de Steeg,
  • Aren Van Waarde,
  • Nicola A. Colabufo,
  • Philip H. Elsinga,
  • Adriaan A. Lammertsma,
  • Albert D. Windhorst and
  • Gert Luurtsema

20 September 2017

Positron emission tomography (PET) imaging of P-glycoprotein (P-gp) in the blood-brain barrier can be important in neurological diseases where P-gp is affected, such as Alzheimer´s disease. Radiotracers used in the imaging studies are present at very...

(This article belongs to the Special Issue Emerging Theranostic Tracers in the Context of Radiopharmaceutical Drug Development)
  • Article
  • Open Access
24 Citations
8,689 Views
13 Pages

Behavioral and Neurochemical Consequences of Pentylenetetrazol-Induced Kindling in Young and Middle-Aged Rats

  • Alexandre Ademar Hoeller,
  • Cristiane Ribeiro De Carvalho,
  • Pedro Leite Costa Franco,
  • Douglas Affonso Formolo,
  • Alexandre Kracker Imthon,
  • Henrique Rodighero Dos Santos,
  • Ingrid Eidt,
  • Gabriel Roman Souza,
  • Leandra Celso Constantino and
  • Roger Walz
  • + 3 authors

13 September 2017

(1) Objectives: Epilepsy disorder is likely to increase with aging, leading to an increased incidence of comorbidities and mortality. In spite of that, there is a lack of information regarding this issue and little knowledge of cognitive and emotiona...

(This article belongs to the Special Issue Epilepsy and Neurodegeneration: Current Therapeutic Implications)
  • Feature Paper
  • Article
  • Open Access
9 Citations
8,109 Views
23 Pages

Synthesis of Nitric Oxide Donors Derived from Piloty’s Acid and Study of Their Effects on Dopamine Secretion from PC12 Cells

  • Daniele Sanna,
  • Gaia Rocchitta,
  • Maria Serra,
  • Marcello Abbondio,
  • Pier Andrea Serra,
  • Rossana Migheli,
  • Lidia De Luca,
  • Eugenio Garribba and
  • Andrea Porcheddu

5 September 2017

This study investigated the mechanisms and kinetics of nitric oxide (NO) generation by derivatives of Piloty’s acid (NO-donors) under physiological conditions. In order to qualitatively and quantitatively measure NO release, electron paramagnetic res...

(This article belongs to the Special Issue Choices of the Journal)
  • Article
  • Open Access
7 Citations
11,198 Views
11 Pages

Role of CYP2C9, CYP2C19 and EPHX Polymorphism in the Pharmacokinetic of Phenytoin: A Study on Uruguayan Caucasian Subjects

  • Natalia Guevara,
  • Cecilia Maldonado,
  • Manuel Uría,
  • Raquel González,
  • Manuel Ibarra,
  • Silvana Alvariza,
  • Antonella Carozzi,
  • Carlos Azambuja,
  • Pietro Fagiolino and
  • Marta Vázquez

18 August 2017

Phenytoin (PHT) oxidative route leads to its main metabolite p-hydroxyphenytoin (p-HPPH), by means of CYP2C9 and CYP2C19. Formation of p-HPPH proceeds via a reactive arene-oxide intermediate. This intermediate can also be converted into PHT dihydrodi...

(This article belongs to the Special Issue Epilepsy and Neurodegeneration: Current Therapeutic Implications)
  • Article
  • Open Access
85 Citations
13,189 Views
17 Pages

Folate Receptor-Positive Gynecological Cancer Cells: In Vitro and In Vivo Characterization

  • Klaudia Siwowska,
  • Raffaella M. Schmid,
  • Susan Cohrs,
  • Roger Schibli and
  • Cristina Müller

15 August 2017

The folate receptor (FR) is expressed in a variety of gynecological cancer types. It has been widely used for tumor targeting with folic acid conjugates of diagnostic and therapeutic probes. The cervical KB tumor cells have evolved as the standard mo...

(This article belongs to the Special Issue Emerging Theranostic Tracers in the Context of Radiopharmaceutical Drug Development)
  • Article
  • Open Access
10 Citations
5,790 Views
9 Pages

The influenza virus hemagglutinin (HA) mediates both receptor (glycan) binding and membrane fusion for cell entry and has been the basis for subtyping influenza viruses. The oligoribonucleotides-d-mannitol (ORNs-d-M) complexes possess an anti-influen...

(This article belongs to the Special Issue Selected Papers from the 2nd International Electronic Conference on Medicinal Chemistry)
  • Review
  • Open Access
126 Citations
15,909 Views
25 Pages

Glycosaminoglycan Interactions with Chemokines Add Complexity to a Complex System

  • Amanda E. I. Proudfoot,
  • Zoë Johnson,
  • Pauline Bonvin and
  • Tracy M. Handel

Chemokines have two types of interactions that function cooperatively to control cell migration. Chemokine receptors on migrating cells integrate signals initiated upon chemokine binding to promote cell movement. Interactions with glycosaminoglycans...

(This article belongs to the Special Issue Glycosaminoglycans and Proteoglycans)
  • Article
  • Open Access
10 Citations
6,804 Views
12 Pages

The Binding Effect of Proteins on Medications and Its Impact on Electrochemical Sensing: Antipsychotic Clozapine as a Case Study

  • George E. Banis,
  • Thomas Winkler,
  • Patricia Barton,
  • Sheryl E. Chocron,
  • Eunkyoung Kim,
  • Deanna L. Kelly,
  • Gregory F. Payne,
  • Hadar Ben-Yoav and
  • Reza Ghodssi

Clozapine (CLZ), a dibenzodiazepine, is demonstrated as the optimal antipsychotic for patients suffering from treatment-resistant schizophrenia. Like many other drugs, understanding the concentration of CLZ in a patient’s blood is critical for managi...

  • Article
  • Open Access
53 Citations
10,771 Views
9 Pages

Assessment of Bone Metastases in Patients with Prostate Cancer—A Comparison between 99mTc-Bone-Scintigraphy and [68Ga]Ga-PSMA PET/CT

  • Lena Thomas,
  • Caroline Balmus,
  • Hojjat Ahmadzadehfar,
  • Markus Essler,
  • Holger Strunk and
  • Ralph A. Bundschuh

Purpose: Bone scintigraphy is the standard of reference in bone metastases in prostate cancer patients. However, new radiotracers employed in prostate-specific membrane antigen (PSMA)-ligands has led to the growing importance of PET/CT as diagnostic...

(This article belongs to the Special Issue Emerging Theranostic Tracers in the Context of Radiopharmaceutical Drug Development)
  • Article
  • Open Access
10 Citations
7,839 Views
19 Pages

Hippocampal Proteome of Rats Subjected to the Li-Pilocarpine Epilepsy Model and the Effect of Carisbamate Treatment

  • José Eduardo Marques-Carneiro,
  • Daniele Suzete Persike,
  • Julia Julie Litzahn,
  • Jean-Christophe Cassel,
  • Astrid Nehlig and
  • Maria José da Silva Fernandes

In adult rats, the administration of lithium–pilocarpine (LiPilo) reproduces most clinical and neuropathological features of human temporal lobe epilepsy (TLE). Carisbamate (CRS) possesses the property of modifying epileptogenesis in this model. Inde...

(This article belongs to the Special Issue Epilepsy and Neurodegeneration: Current Therapeutic Implications)
  • Article
  • Open Access
13 Citations
9,740 Views
15 Pages

Modernization of Enoxaparin Molecular Weight Determination Using Homogeneous Standards

  • Katelyn M. Arnold,
  • Stephen J. Capuzzi,
  • Yongmei Xu,
  • Eugene N. Muratov,
  • Kevin Carrick,
  • Anita Y. Szajek,
  • Alexander Tropsha and
  • Jian Liu

Enoxaparin is a low-molecular weight heparin used to treat thrombotic disorders. Following the fatal contamination of the heparin supply chain in 2007–2008, the U.S. Pharmacopeia (USP) and U.S. Food and Drug Administration (FDA) have worked extensive...

(This article belongs to the Special Issue Glycosaminoglycans and Proteoglycans)
  • Article
  • Open Access
8 Citations
6,297 Views
14 Pages

Tumor suppressor genes can be silenced genetically as well as epigenetically. One approach to reversing epigenetic suppression of tumor suppressor genes is to inhibit DNA methyl transferase. 5-aza-2′,2′-difluorodeoxycytidine (NUC013) is a novel DNA m...

  • Article
  • Open Access
100 Citations
14,961 Views

Neuroprotective Effects of β-Caryophyllene against Dopaminergic Neuron Injury in a Murine Model of Parkinson’s Disease Induced by MPTP

  • Juan M. Viveros-Paredes,
  • Rocio E. González-Castañeda,
  • Juerg Gertsch,
  • Veronica Chaparro-Huerta,
  • Rocio I. López-Roa,
  • Eduardo Vázquez-Valls,
  • Carlos Beas-Zarate,
  • Antoni Camins-Espuny and
  • Mario E. Flores-Soto

Parkinson’s disease (PD) is one of the most common neurodegenerative disorders and is characterized by the loss of dopaminergic neurons in the substantia nigra (SN). Although the causes of PD are not understood, evidence suggests that its pathogenesi...

(This article belongs to the Special Issue Epilepsy and Neurodegeneration: Current Therapeutic Implications)
  • Editorial
  • Open Access
17 Citations
6,111 Views
4 Pages

2017 marks the 20th anniversary of the molecular cloning by David Julius and colleagues (1997) of the long sought-after capsaicin receptor, now known as TRPV1 (Transient Receptor Potential Vanilloid 1) [1]. This seminal discovery has opened up a “hot...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts)
  • Article
  • Open Access
5 Citations
7,363 Views
20 Pages

Synthesis and Antiproliferative Activity of Novel Heterocyclic Indole-Trimethoxyphenyl Conjugates

  • Michael M. Cahill,
  • Kevin D. O’Shea,
  • Larry T. Pierce,
  • Hannah J. Winfield,
  • Kevin S. Eccles,
  • Simon E. Lawrence and
  • Florence O. McCarthy

The synthesis and biological evaluation of a series of novel heterocyclic indole derivatives is described. The consolidation of the combretastatin and bisindolylmaleimide templates towards the inclusion of a novel heterocyclic ring proffered a versat...

(This article belongs to the Special Issue Selected Papers from the 2nd International Electronic Conference on Medicinal Chemistry)
  • Review
  • Open Access
46 Citations
10,805 Views
30 Pages

Nanofiber Scaffolds as Drug Delivery Systems to Bridge Spinal Cord Injury

  • Angela Faccendini,
  • Barbara Vigani,
  • Silvia Rossi,
  • Giuseppina Sandri,
  • Maria Cristina Bonferoni,
  • Carla Marcella Caramella and
  • Franca Ferrari

The complex pathophysiology of spinal cord injury (SCI) may explain the current lack of an effective therapeutic approach for the regeneration of damaged neuronal cells and the recovery of motor functions. A primary mechanical injury in the spinal co...

(This article belongs to the Special Issue Tissue-Protective Agents: New Drugs and Technologies)
  • Article
  • Open Access
28 Citations
9,912 Views
12 Pages

Current therapeutic unfractionated heparin available in Europe and US is of porcine mucosal origin. There is now interest, specifically in the US, to use bovine mucosa as an additional source for the production of heparin. The anticoagulant action of...

(This article belongs to the Special Issue Glycosaminoglycans and Proteoglycans)
  • Article
  • Open Access
62 Citations
9,701 Views
15 Pages

Pseudomonas aeruginosa is involved in a variety of difficult-to-treat infections frequently due to biofilm formation. To identify useful antibiofilm strategies, this article evaluated efficacy of two newly engineered cationic antimicrobial peptides (...

(This article belongs to the Special Issue Choices of the Journal)
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Pharmaceuticals - ISSN 1424-8247