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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
11 Citations
8,543 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...

  • Article
  • Open Access
5 Citations
5,940 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
96 Citations
13,776 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...

  • Editorial
  • Open Access
17 Citations
5,623 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...

  • Article
  • Open Access
4 Citations
6,845 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...

  • Review
  • Open Access
45 Citations
10,137 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...

  • Article
  • Open Access
24 Citations
9,014 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...

  • Article
  • Open Access
60 Citations
9,090 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 (...

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Pharmaceuticals - ISSN 1424-8247