AI Article Synopsis
- New combretastatin analogues have been tested for their ability to inhibit tubulin polymerization, crucial for cancer treatment.
- These new compounds have a macrocyclic structure with a chain linking aromatic groups, which restricts their conformation to potentially enhance effectiveness.
- However, this conformational restriction and steric hindrance make these new analogues less effective inhibitors compared to the established compound CA-4.
Article Abstract
New analogues of combretastatins have been evaluated as inhibitors of tubulin polymerization. These compounds present a macrocyclic structure, in which the para positions of the aromatic moieties have been linked by a 5- or 6-atoms chain, in order to produce a conformational restriction. This could contribute to determine the active conformation for these ligands. Such a conformational restriction and/or the steric hindrance makes them less potent inhibitors than the model compound CA-4.
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| http://dx.doi.org/10.1016/j.bmcl.2007.08.075 | DOI Listing |
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