Antivascular and anticancer activity of dihalogenated A-ring analogues of combretastatin A-4

作者:Beale Thomas M; Myers Rebecca M*; Shearman James W; Charnock Jones D Stephen; Brenton James D; Gergely Fanni V; Ley Steven V
来源:Medchemcomm, 2010, 1(3): 202-208.
DOI:10.1039/c0md00095g

摘要

The generally accepted view is that the 3,4,5-trimethoxy-substituted aromatic A-ring of combretastatin A-4 (CA-4) and its analogues should be conserved in order to maintain biological activity through enforcing an active molecular conformation. Contrary to this, we have found that substituting the larger meta-methoxy groups of CA-4 with smaller halogen atoms results in compounds that are equipotent or more potent than CA-4 itself in vitro.

  • 出版日期2010-9