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4,5-Diaryl-3H-1,2-dithiole-3-thiones and related compounds as combretastatin A-4/oltipraz hybrids: Synthesis, molecular modelling and evaluation as antiproliferative agents and inhibitors of tubulin.
- Source :
-
European Journal of Medicinal Chemistry . Oct2016, Vol. 122, p520-529. 10p. - Publication Year :
- 2016
-
Abstract
- A new series of 4,5-diaryl-3 H -1,2-dithiole-3-thiones and related compounds were designed and synthesised as combretastatin A-4/oltipraz hybrids. We evaluated the antiproliferative activities, inhibition of tubulin polymerization, and cell-cycle effects of these compounds. Several compounds in this series, such as 4d and 5c , displayed significant activity against SGC-7901, KB and HT-1080 cell lines, as determined using MTT assays. The most active compound, 4d , markedly inhibited tubulin polymerization, with an IC 50 value of 4.44 μM being observed. In mechanistic studies, 4d caused cell arrest in G2/M phase, induced apoptotic cell death, and disrupted microtubule formation. Molecular docking studies revealed that 4d interacts and binds efficiently with the tubulin protein. [ABSTRACT FROM AUTHOR]
- Subjects :
- *THIONES
*ORGANIC synthesis
*TUBULINS
*ANTINEOPLASTIC agents
*POLYMERIZATION
Subjects
Details
- Language :
- English
- ISSN :
- 02235234
- Volume :
- 122
- Database :
- Academic Search Index
- Journal :
- European Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 117709993
- Full Text :
- https://doi.org/10.1016/j.ejmech.2016.06.055