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Molecules, Volume 22, Issue 3

March 2017 - 163 articles

Cover Story: In the New Medicines for Trypanosomatidic Infections (NMTRypI) project funded by the EU, we have discovered novel anti-leishmania and anti-trypanosoma hits that inhibit pteridine reductase 1 (PTR1). Here, we synthesized compounds with a flavanone scaffold and characterized their antiparasitic activity and ADME-tox properties. Crystal structure determination and computational docking explain differences in their inhibition of PTR1. Two crystal structures of one compound with different PTR1 enzymes provide a basis for further scaffold optimization to develop inhibitors targeting PTR1 enzymes from different parasites. View this paper.
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Articles (163)

  • Article
  • Open Access
34 Citations
13,302 Views
10 Pages

Despite the apparent clinical benefits of high-dose cytarabine (Ara-C) over lower dose Ara-C in acute myeloid leukemia (AML) therapy, the mechanism behind high-dose Ara-C therapy remains uncertain. In this study, a LC-MS-based method was carried out...

  • Article
  • Open Access
9 Citations
6,879 Views
12 Pages

Biosynthesis of Oligomeric Anthocyanins from Grape Skin Extracts

  • Jin-Woo Hwang,
  • Sithranga Boopathy Natarajan,
  • Yon-Suk Kim,
  • Eun-Kyung Kim,
  • Jae Woong Lee,
  • Sang-Ho Moon,
  • Byong-Tae Jeon and
  • Pyo-Jam Park

We synthesized oligomeric anthocyanins from grape skin-derived monomeric anthocyanins such as anthocyanidin and proanthocyanidin by a fermentation technique using Aspergillus niger, crude enzymes and glucosidase. The biosyntheses of the oligomeric an...

  • Article
  • Open Access
8 Citations
5,894 Views
24 Pages

The present work is directed toward understanding the mechanisms of excited state deactivation in three neutral model peptides containing the phenylalanine residue. The excited state dynamics of theγL(g+)folded form of N-acetylphenylalaninylamide (NA...

  • Article
  • Open Access
47 Citations
8,596 Views
15 Pages

New Chiral Ebselen Analogues with Antioxidant and Cytotoxic Potential

  • Agata J. Pacuła,
  • Katarzyna B. Kaczor,
  • Jędrzej Antosiewicz,
  • Anna Janecka,
  • Angelika Długosz,
  • Tomasz Janecki,
  • Andrzej Wojtczak and
  • Jacek Ścianowski

New chiral camphane-derived benzisoselenazol-3(2H)-ones and corresponding diselenides have been synthetized using a convenient one-pot procedure. Se-N bond was efficiently converted to an Se-Se bond, which could also be easily re-oxidized to the init...

  • Article
  • Open Access
14 Citations
5,492 Views
9 Pages

Irradiation of (E)-4-(2-(2-naphthyl)vinyl)pyridine (1a) and (E)-4-(2-(1-naphthyl)vinyl)pyridine (1b) with a 250 W high-pressure mercury lamp in acidic solution afforded synHT dimers in high stereoselectivities. Similar results were obtained by visibl...

  • Review
  • Open Access
168 Citations
15,863 Views
24 Pages

Pretreatment is very important for the efficient production of value-added products from lignocellulosic biomass. However, traditional pretreatment methods have several disadvantages, including low efficiency and high pollution. This article gives an...

  • Article
  • Open Access
16 Citations
7,749 Views
15 Pages

Effects of Momordica charantia (Bitter Melon) on Ischemic Diabetic Myocardium

  • Attila Czompa,
  • Alexandra Gyongyosi,
  • Kitti Szoke,
  • Istvan Bak,
  • Evelin Csepanyi,
  • David D. Haines,
  • Arpad Tosaki and
  • Istvan Lekli

Objective: A rat model is here used to test a hypothesis that Momordica charantia (Bitter melon (BM)) extract favorably alters processes in cardiovascular tissue and is systemically relevant to the pathophysiology of type 2 diabetes (T2DM) and relate...

  • Communication
  • Open Access
1 Citations
5,948 Views
10 Pages

Separation of Alkyne Enantiomers by Chiral Column HPLC Analysis of Their Cobalt-Complexes

  • Qiaoyun Liu,
  • Jing Wang,
  • Junfei Li,
  • Xiaolei Wang,
  • Shichao Lu,
  • Xuan Li,
  • Yaling Gong and
  • Shu Xu

Separation of the enantiomers of new chiral alkynes in strategic syntheses and bioorthogonal studies is always problematic. The chiral column high-performance liquid chromatography (HPLC) method in general could not be directly used to resolve such s...

  • Article
  • Open Access
16 Citations
6,615 Views
13 Pages

Ginsenoside PPD’s Antitumor Effect via Down-Regulation of mTOR Revealed by Super-Resolution Imaging

  • Bo Teng,
  • Junguang Jiang,
  • Lijing Zhao,
  • Jing Gao,
  • Junyu Chen,
  • Zhe Liu,
  • Hongda Wang and
  • Binfeng Lu

Derived from Panax ginseng, the natural product 20(S)-Protopanaxadiol (PPD) has been reported for its cytotoxicity against several cancer cell lines. The molecular mechanism is, however, not well understood. Here we show that PPD significantly inhibi...

  • Feature Paper
  • Review
  • Open Access
8 Citations
9,070 Views
22 Pages

Synthesis of Substituted α-Trifluoromethyl Piperidinic Derivatives

  • Sarah Rioton,
  • Domingo Gomez Pardo and
  • Janine Cossy

A comprehensive survey of pathways leading to the generation of α-trifluoromethyl monocyclic piperidinic derivatives is provided (65 references). These compounds have been synthesized either from 6-membered rings e.g., pipecolic acid or lactam deriva...

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Molecules - ISSN 1420-3049