Biological evaluation of synthetic analogues of curcumin: chloro-substituted-2′-hydroxychalcones as potential inhibitors of tubulin polymerization and cell proliferation

A series of chloro-substituted-2′-hydroxychalcones were prepared and evaluated for their cytotoxic effects against K562 and SK-N-MC human cancer cell lines and as the inhibitors of tubulin polymerization. The 3,5′-dichloro- analogue (compound 3 ) inhibited the assembly of protofilaments with 89% inh...

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Bibliographic Details
Published in:Medicinal chemistry research 2011-05, Vol.20 (4), p.503-510
Main Authors: Aryapour, Hassan, Riazi, Gholam Hossein, Foroumadi, Alireza, Ahmadian, Shahin, Shafiee, Abbas, Karima, Oveis, Mahdavi, Majid, Emami, Saeed, Sorkhi, Maedeh, Khodadady, Sirus
Format: Article
Language:English
Subjects:
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Original Research
Pharmacology/Toxicology
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Summary:A series of chloro-substituted-2′-hydroxychalcones were prepared and evaluated for their cytotoxic effects against K562 and SK-N-MC human cancer cell lines and as the inhibitors of tubulin polymerization. The 3,5′-dichloro- analogue (compound 3 ) inhibited the assembly of protofilaments with 89% inhibition. Compound 3 was found to be bound to tubulin with a dissociation constant of 3.7 μM and altered far-UV circular dichroism spectrum of tubulin and altered far-UV circular dichroism spectrum of tubulin.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-010-9344-z