scholarly journals Synthesis and biological evaluation of new 3-amino-2-azetidinone derivatives as anti-colorectal cancer agents

MedChemComm ◽  
2018 ◽  
Vol 9 (5) ◽  
pp. 843-852 ◽  
Author(s):  
Farida Tripodi ◽  
Federico Dapiaggi ◽  
Fulvia Orsini ◽  
Roberto Pagliarin ◽  
Guido Sello ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Natural Product ◽  
South African ◽  
Drug Efficacy ◽  
Biological Evaluation ◽  
The South ◽  
Combretastatin A4 ◽  
Synthesis And Biological Evaluation ◽  
Combretum Caffrum

Several synthetic combretastatin A4 (CA-4) derivatives were recently prepared to increase the drug efficacy and stability of the natural product isolated from the South African tree Combretum caffrum.

Synthesis and Biological Evaluation of the Antimicrobial Natural Product Lipoxazolidinone A

2018 ◽  
Author(s):  
Jonathan J. Mills ◽  
Kaylib R. Robinson ◽  
Troy E. Zehnder ◽  
Joshua G. Pierce
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Mechanism Of Action ◽  
Marine Natural Products ◽  
Biological Evaluation ◽  
Lead Compounds ◽  
Follow Up Studies ◽  
Initial Resistance ◽  
Synthesis And Biological Evaluation

The lipoxazolidinone family of marine natural products, with an unusual 4-oxazolidinone heterocycle at their core, represents a new scaffold for antimicrobial discovery; however, questions regarding their mechanism of action and high lipophilicity have likely slowed follow-up studies. Herein, we report the first synthesis of lipoxazolidinone A, 15 structural analogs to explore its active pharmacophore, and initial resistance and mechanism of action studies. These results suggest that 4-oxazolidinones are valuable scaffolds for antimicrobial development and reveal simplified lead compounds for further optimization.

Isolation and structure of combretastatin

1982 ◽  
Vol 60 (11) ◽  
pp. 1374-1376 ◽  
Author(s):  
George R. Pettit ◽  
Gordon M. Cragg ◽  
Delbert L. Herald ◽  
Jean M. Schmidt ◽  
Prasert Lohavanijaya
Keyword(s):  
Total Synthesis ◽  
South African ◽  
Spectral Methods ◽  
Biological Evaluation ◽  
Crystallographic Analysis ◽  
Structural Elucidation ◽  
The South ◽  
X Ray

The South African tree Combretumcaffrum has been shown to contain a constituent capable of significantly reversing astrocyte formation employing the National Cancer Institute's 9ASK system. The constituent responsible for astrocyte reversal was isolated and designated combretastatin (1). Structural elucidation was initiated employing spectral methods and completed by X-ray crystallographic analysis. By this means combretastatin was assigned structure 1. Further biological evaluation and a total synthesis are now in progress.

ChemInform Abstract: Synthesis and Biological Evaluation of KRIBB3 Analogues on a Proliferation of HCT-116 Colorectal Cancer Cells.

ChemInform ◽  
2011 ◽  
Vol 42 (17) ◽  
pp. no-no
Author(s):  
Sangku Lee ◽  
Jae Nyoung Kim ◽  
Ji Hye Min ◽  
Kab Seog Yoon ◽  
Ki Deok Shin ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Cancer Cells ◽  
Biological Evaluation ◽  
Colorectal Cancer Cells ◽  
Hct 116 ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of acylated oligorhamnoside derivatives structurally related to mezzettiaside-6 with cytotoxic activity

2016 ◽  
Vol 14 (28) ◽  
pp. 6691-6702 ◽  
Author(s):  
Gaopeng Song ◽  
Sumei Li ◽  
Zhiwei Lei ◽  
Yibin Li ◽  
Junhua Li ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Natural Product ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Two partially acylated oligorhamnoside derivatives 1 and 2 structurally related to the natural product mezzettiaside-6 were synthesized via a ‘2 + 1 + 1’ convergent strategy.

Total synthesis and biological evaluation of the natural product (−)-cyclonerodiol, a new inhibitor of IL-4 signaling

2014 ◽  
Vol 12 (47) ◽  
pp. 9707-9715 ◽  
Author(s):  
Jens Langhanki ◽  
Kristina Rudolph ◽  
Gerhard Erkel ◽  
Till Opatz
Keyword(s):  
Total Synthesis ◽  
Natural Product ◽  
Specific Inhibitor ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

The sesquiterpene (−)-cyclonerodiol is a specific inhibitor of IL-4 induced STAT6 signaling and is readily available from (−)-linalool.

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