866261-63-4Relevant academic research and scientific papers
Pt(IV) complexes conjugating with chalcone analogue as inhibitors of microtubule polymerization exhibited selective inhibition in human cancer cells
Huang, Xiaochao,Huang, Rizhen,Wang, Zhimei,Li, Lingxue,Gou, Shaohua,Liao, Zhixin,Wang, Hengshan
, p. 435 - 450 (2018)
Six novel of Pt(IV) complexes comprising chalcone analogues were synthesized and evaluated for anti-proliferative activity using MTT assay. In vitro evaluation revealed that all Pt(IV) complexes showed better and more potent activity against three human cancer cells including CDDP resistant cells than that of their corresponding mother Pt(II) species. Among them, two representative complexes, 14 and 17, exhibited better cell selectivity between cancer cells and normal cells than CDDP. Molecular docking study indicated that complexes 14 and 17 could bind to the colchicine site of tubulin. Moreover, complexes 14 and 17 also remarkably displayed inhibition of cell migration against HUVEC cells in vitro. Molecular mechanism studies suggested that 14 and 17 induced production of reactive oxygen species (ROS), cell cycle arrest at the G2/M phase, and mitochondria-mediated apoptosis by regulating the expression of Bcl-2 family members.
The synthesis and evaluation of new butadiene derivatives as tubulin polymerization inhibitors
Pang, Yanqing,Yan, Jun,An, Baijiao,Huang, Ling,Li, Xingshu
, p. 3059 - 3067 (2017/05/29)
A series of new butadiene derivatives was synthesized and evaluated as tubulin polymerization inhibitors for the treatment of cancer. The optimal butadiene derivative, 9a, exhibited IC50 values of 0.056–0.089?μM for five human cancer cell lines. This paper included a mechanistic study of the antiproliferative activity, including a tubulin polymerization assay, an examination of morphological alterations of cancer cells, an analysis of cell cycle arrest and an apoptosis assay.
Synthesis and biological evaluation of a series of tangeretin-derived chalcones
Quintin, Jerome,Desrivot, Julie,Thoret, Sylviane,Menez, Patrick Le,Cresteil, Thierry,Lewin, Guy
body text, p. 167 - 169 (2009/04/10)
A series of chalcones polyoxygenated on the ring A (with pentamethoxy or 2′-hydroxy-3′,4′,5′,6′-tetramethoxy substitution patterns) was synthesized from tangeretin, a natural Citrus flavonoid. These chalcones were evaluated for their antiproliferative, ac
