Skip to main page content (V体育官网入口)
U.S. flag

An official website of the United States government

Dot gov

The . gov means it’s official. Federal government websites often end in . gov or . mil. Before sharing sensitive information, make sure you’re on a federal government site VSports app下载. .

Https

The site is secure. The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely V体育官网. .

. 2016 Oct 21:122:520-529.
doi: 10.1016/j.ejmech.2016.06.055. Epub 2016 Jul 1.

"VSports在线直播" 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

Zhiwei Wang  1 , Huan Qi  2 , Qirong Shen  3 , Guodong Lu  3 , Mingyang Li  3 , Kai Bao  4 , Yingliang Wu  5 , Weige Zhang  6
Affiliations

"V体育官网入口" 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

Zhiwei Wang et al. Eur J Med Chem. .

Abstract

A new series of 4,5-diaryl-3H-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 IC50 value of 4. 44 μM being observed VSports手机版. 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. .

Keywords: Antiproliferative activity; Cell cycle arrest; Combretastatin A-4/oltipraz hybrids; Molecular modelling studies; Tubulin polymerization V体育安卓版. .

PubMed Disclaimer

MeSH terms

LinkOut - more resources