Synthesis and biological evaluation of ...
Document type :
Article dans une revue scientifique
PMID :
23618708
Permalink :
Title :
Synthesis and biological evaluation of fluoro analogues of antimitotic phenstatin
Author(s) :
Ghinet, Alina [Auteur]
Tourteau, Aurelien [Auteur]
Rigo, Benoit [Auteur]
Stocker, Vivien [Auteur]
Leman, Marie [Auteur]
Farce, Amaury [Auteur]
Dubois, Joelle [Auteur]
Gautret, Philippe [Auteur]
Tourteau, Aurelien [Auteur]
Rigo, Benoit [Auteur]
Stocker, Vivien [Auteur]
Leman, Marie [Auteur]
Farce, Amaury [Auteur]
Dubois, Joelle [Auteur]
Gautret, Philippe [Auteur]
Journal title :
Bioorganic & medicinal chemistry
Abbreviated title :
Bioorg. Med. Chem.
Volume number :
21
Pages :
2932-2940
Publication date :
2013-06-01
ISSN :
0968-0896
English keyword(s) :
Tubulin
Phenstatin
Eaton''s reagent
Fluorobenzophenone
Antimitotic agent
Phenstatin
Eaton''s reagent
Fluorobenzophenone
Antimitotic agent
HAL domain(s) :
Sciences du Vivant [q-bio]
English abstract : [en]
With the aim of investigating the influence of fluorine, in particular on the A-ring, a new series of fluoro analogues (7a-l) of phenstatin (3) was synthesized and tested for interactions with tubulin polymerization and ...
Show more >With the aim of investigating the influence of fluorine, in particular on the A-ring, a new series of fluoro analogues (7a-l) of phenstatin (3) was synthesized and tested for interactions with tubulin polymerization and evaluated for cytotoxicity on an NCI-60 human cancer cell lines panel. We have shown that the replacement of 3,4,5-trimethoxyphenyl A-ring of phenstatin with 2,4,5-trifluoro-3-methoxyphenyl unit, results in the conservation of both antitubulin and cytotoxic effect. Fluoro isocombretastatin 7k was the most effective anticancer agent in the present study and demonstrated the highest antiproliferative potential on leukemia cell lines SR (GI50=15 nM) and HL-60(TB) (GI50=23 nM) and on melanoma cell line MDA-MB-435 (GI50=19 nM).Show less >
Show more >With the aim of investigating the influence of fluorine, in particular on the A-ring, a new series of fluoro analogues (7a-l) of phenstatin (3) was synthesized and tested for interactions with tubulin polymerization and evaluated for cytotoxicity on an NCI-60 human cancer cell lines panel. We have shown that the replacement of 3,4,5-trimethoxyphenyl A-ring of phenstatin with 2,4,5-trifluoro-3-methoxyphenyl unit, results in the conservation of both antitubulin and cytotoxic effect. Fluoro isocombretastatin 7k was the most effective anticancer agent in the present study and demonstrated the highest antiproliferative potential on leukemia cell lines SR (GI50=15 nM) and HL-60(TB) (GI50=23 nM) and on melanoma cell line MDA-MB-435 (GI50=19 nM).Show less >
Audience :
Internationale
Popular science :
Non
Administrative institution(s) :
CHU Lille
Inserm
Université de Lille
Inserm
Université de Lille
Research team(s) :
Therapeutic innovation targetting inflammation
Submission date :
2019-05-17T13:14:32Z