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Pharmaceuticals, Volume 10, Issue 3

September 2017 - 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
4 Citations
7,963 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...

  • Article
  • Open Access
21 Citations
7,911 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
  • Camila Leite Ferreira
  • + 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...

  • Feature Paper
  • Article
  • Open Access
8 Citations
7,559 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...

  • Article
  • Open Access
7 Citations
9,777 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...

  • Article
  • Open Access
75 Citations
12,001 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...

  • Article
  • Open Access
10 Citations
5,499 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...

  • Review
  • Open Access
110 Citations
13,994 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...

  • Article
  • Open Access
9 Citations
6,171 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
51 Citations
9,987 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...

  • Article
  • Open Access
10 Citations
7,299 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...

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Pharmaceuticals - ISSN 1424-8247