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Synthesis and biological evaluation of new 2-methoxyestradiol derivatives: Potent inhibitors of angiogenesis and tubulin polymerization by Moran Sun; Yixin Zhang; Jinling Qin; Mengyu Ba; Yongfang Yao; Yongtao Duan; Hongmin Liu; Dequan Yu is a Chemistry article available to read on EtoBox.
What is Synthesis and biological evaluation of new 2-methoxyestradiol derivatives: Potent inhibitors of angiogenesis and tubulin polymerization about?
Here, we report the structural optimization of a hit natural compound, 2-ME (2-methoxyestradiol), which exhibited inhibitory activity but low potency on tubulin polymerization, anti- angiogenesis, MCF-7 proliferation and metastasis in vitro and in vivo. A novel series of 3,17-modified and 17-modified analogs of 2-ME were synthesized and investigated for their antiproliferative activity against MCF-7 and another five different human cancer cell lines leading to the discovery of 9i. 9i bind to tubulin colchicine site tightly, inhibited tubulin polymerization and disrupted cellular microtubule networks. Cellular mechanism studies revealed that 9i could induce G2/M phase arrest by down-regulated expression of p-Cdc2, P21 and cell apoptosis by regulating apoptosis-related proteins (Parp, Caspase families) in a dose-dependent manner. Importantly, 9i significantly inhibited HUVEC tube formation, proliferation, migration and invasion. The inhibitory effect against angiogenesis in vivo was confirmed by zebrafish xenograft. Furthermore, 9i could effectively inhibit the proliferation and metastasis of MCF-7 cells in vitro and in zebrafish xenograft. The satisfactory physicochemical property a
Who reads Synthesis and biological evaluation of new 2-methoxyestradiol derivatives: Potent inhibitors of angiogenesis and tubulin polymerization?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Moran Sun; Yixin Zhang; Jinling Qin; Mengyu Ba; Yongfang Yao; Yongtao Duan; Hongmin Liu; Dequan Yu
- Publisher
- Elsevier BV
- Published
- 2021
- Language
- EN
- Field
- Chemistry (Physical Sciences)