Isolation, structure elucidation and biological evaluation of novel cathepsin inhibitors from marine cyanobacteria

Planta Medica ◽  
2015 ◽  
Vol 81 (11) ◽  
Author(s):  
FH Al-Awadhi ◽  
V Paul ◽  
H Luesch
Keyword(s):  
Structure Elucidation ◽  
Biological Evaluation ◽  
Marine Cyanobacteria

scholarly journals The myxocoumarins A and B fromStigmatella aurantiacastrain MYX-030

2013 ◽  
Vol 9 ◽  
pp. 2579-2585 ◽  
Author(s):  
Tobias A M Gulder ◽  
Snežana Neff ◽  
Traugott Schüz ◽  
Tammo Winkler ◽  
René Gees ◽  
...  
Keyword(s):  
Natural Products ◽  
Structure Elucidation ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Antifungal Properties ◽  
Structural Framework ◽  
Stigmatella Aurantiaca ◽  
Promising Source ◽  
Active Natural

The myxobacterial strainStigmatella aurantiacaMYX-030 was selected as promising source for the discovery of new biologically active natural products by our screening methodology. The isolation, structure elucidation and initial biological evaluation of the myxocoumarins derived from this strain are described in this work. These compounds comprise an unusual structural framework and exhibit remarkable antifungal properties.

ChemInform Abstract: Isolation, Structure Elucidation, and Biological Evaluation of the Unusual Heterodimer Chrysoxanthone from the Ascomycete IBWF11-95A.

ChemInform ◽  
2009 ◽  
Vol 40 (48) ◽  
Author(s):  
Anja Schueffler ◽  
Johannes C. Liermann ◽  
Heinz Kolshorn ◽  
Till Opatz ◽  
Heidrun Anke
Keyword(s):  
Structure Elucidation ◽  
Biological Evaluation

The Structure Elucidation of Haprolid

Synthesis ◽  
2017 ◽  
Vol 50 (03) ◽  
pp. 529-538 ◽  
Author(s):  
Markus Kalesse ◽  
Jun Li ◽  
Jun Xing ◽  
Daniel Lücke ◽  
Dennis Lübken ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Natural Product ◽  
Structure Elucidation ◽  
Carcinoma Cell ◽  
Hidden Markov ◽  
Biological Evaluation ◽  
Terminal Olefin ◽  
Carcinoma Cell Lines ◽  
Hepatocellular Carcinoma Cell ◽  
Key Steps

The assignment of two stereocenters of the natural product haprolid through the application of a profile hidden Markov model (HMM) and its confirmation through total synthesis of the natural product and of two of its diastereomers are reported. The structure elucidation of this polyketide-peptide hybrid natural product is a telling showcase of how difficult it can be to determine the absolute configuration of isolated stereocenters and the benefits of a gene cluster analysis for structure determination. The key steps of the synthesis are a selective epoxidation of a terminal olefin and the stereodivergent macrolactonization strategy. Furthermore, the biological evaluation of all products showed that all diastereomers are potent inhibitors of hepatocellular carcinoma cell lines.

ChemInform Abstract: Synthesis, Structure Elucidation and Biological Evaluation of C- Norpaclitaxel.

ChemInform ◽  
2010 ◽  
Vol 27 (6) ◽  
pp. no-no
Author(s):  
X. LIANG ◽  
D. G. I. KINGSTON ◽  
B. H. LONG ◽  
C. A. FAIRCHILD ◽  
K. A. JOHNSTON
Keyword(s):  
Structure Elucidation ◽  
Biological Evaluation

Total synthesis and biological evaluation of oscillatoxin D, E, and F

2021 ◽  
Author(s):  
Yusuke Araki ◽  
Yusuke Hanaki ◽  
Masaki Kita ◽  
Koutaro Hayakawa ◽  
Kazuhiro Irie ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Cell Line ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Marine Cyanobacteria ◽  
Methyl Group ◽  
Synthetic Strategy ◽  
Target Molecules ◽  
Synthesis And Biological Evaluation

Abstract Oscillatoxins (OTXs) and aplysiatoxins (ATXs) are biosynthetically related polyketides produced by marine cyanobacteria. We previously developed a synthetic route to phenolic O-methyl analogs of OTX-D and 30-methyl-OTX-D during collective synthesis of these natural products. According to our synthetic strategy, we achieved total synthesis of OTX-D, 30-methyl-OTX-D, OTX-E, and OTX-F by deprotecting the O-methyl group in an earlier intermediate, and determined their biological activities. Although OTX-D and 30-methyl-OTX-D have been reported to show anti-leukemic activity against L1210 cell line, we found that their cytotoxicity in vitro against this cell line is relatively weak (IC50: 29–52 μM). In contrast, OTX-F demonstrated cell line-selective anti-proliferative activity against DMS-114 lung cancer cells, which implies that OTXs target as yet unknown target molecules as part of this unique activity.

scholarly journals Genome-Directed Lead Discovery: Biosynthesis, Structure Elucidation, and Biological Evaluation of Two Families of Polyene Macrolactams against Trypanosoma brucei

2015 ◽  
Vol 10 (10) ◽  
pp. 2373-2381 ◽  
Author(s):  
Christopher J. Schulze ◽  
Mohamed S. Donia ◽  
Jair L. Siqueira-Neto ◽  
Debalina Ray ◽  
Jevgenij A. Raskatov ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Structure Elucidation ◽  
Biological Evaluation ◽  
Lead Discovery
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