AI Article Synopsis
- Researchers created hybrids of vinca alkaloids and phomopsin A to target different sites on tubulin, a protein important for cell structure and division.
- These hybrids were synthesized using a quick method that combines specific chemical parts of the compounds.
- In studies, these hybrids closely matched existing treatments for tubulin and showed strong effectiveness in stopping microtubule assembly, proving to be harmful to cancer cells in four different types.
Article Abstract
Hybrids of vinca alkaloids and phomopsin A have been elaborated with the aim of interfering with the "vinca site" and the "peptide site" of the vinca domain in tubulin. They were synthesized by an efficient one-pot procedure that directly links the octahydrophomopsin lateral chain to the velbenamine moiety of 7'-homo-anhydrovinblastine. In their modeled complexes with tubulin, these hybrids were found to superimpose nicely on the tubulin-bound structures of vinblastine and phomopsin A. This good matching can account for the fact that two of them are very potent inhibitors of microtubules assembly and are cytotoxic against four cancer cell lines.
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| http://dx.doi.org/10.1021/jm500530v | DOI Listing |
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