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EnglishA novel series of tubulin polymerization inhibitors, based on the 1-(3’,4’,5’-trimethoxyphenyl)-2-aryl-1H-imidazole scaffold and designed as cis-restricted combretastatin A-4 analogues, was synthesized with the goal of evaluating the effects of various patterns of substitution on the phenyl at the 2-position of the imidazole ring on biological activity. A chloro and ethoxy group at the meta- and para-positions, respectively, produced the most active compound in the series (4o), with IC50 values of 0.4-3.8 nM against a panel of seven cancer cell lines. Except in HL-60 cells, 4o had greater antiproliferative than CA-4, indicating that the 3’-chloro-4’-ethoxyphenyl moiety was a good surrogate for the CA-4 B-ring. Experiments carried out in a mouse syngenic model demonstrated high antitumor activity of 4o, which significantly reduced the tumor mass at a dose thirty times lower than that required for CA-4P, which was used as a reference compound. Altogether, our findings suggest that 4o is a promising anticancer drug candidate that warrants further preclinical evaluation.
| Titolo: | Design and Synthesis of Potent in Vitro and in Vivo Anticancer Agents Based on 1-(3’,4’,5’-Trimethoxyphenyl)-2-Aryl-1H-Imidazole | |
| Autori: | BARALDI, Pier Giovanni (Secondo) | |
| Data di pubblicazione: | 2016 | |
| Rivista: | ||
| Handle: | http://hdl.handle.net/11392/2343844 | |
| Appare nelle tipologie: | 03.1 Articolo su rivista |
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| File | Descrizione | Tipologia | Licenza | |
|---|---|---|---|---|
| SREP26602.pdf | Full text ed | Full text (versione editoriale) |  | Open Access Visualizza/Apri |
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