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Design, synthesis and evaluation of antiproliferative activity of fluorinated betulinic acid.

Abstract：

:Betulinic acid (BA), a pentacyclic triterpenoid, exhibits broad spectrum antiproliferative activity, but generally with only modest potency. To improve BA's pharmacological properties, fluorine was introduced as a single atom at C-2, creating two diastereomers, or in a trifluoromethyl group at C-3. We evaluated the impact of these groups on antiproliferative activity against five human tumor cell lines. A racemic 2-F-BA (compound 6) showed significantly improved antiproliferative activity, while each diastereomer exhibited similar effects. We also demonstrated that 2-F-BA is a topoisomerase (Topo) I and IIα dual inhibitor in cell-based and cell-free assays. A hypothetical mode of binding to the Topo I-DNA suggested a difference between the hydrogen bonding of BA and 2-F-BA to DNA, which may account for the difference in bioactivity against Topo I.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Li J,Chang LC,Hsieh KY,Hsu PL,Capuzzi SJ,Zhang YC,Li KP,Morris-Natschke SL,Goto M,Lee KH

doi

10.1016/j.bmc.2019.05.016

subject

Has Abstract

pub_date

2019-07-01 00:00:00

pages

2871-2882

issue

13

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(19)30523-1

journal_volume

27

pub_type

杂志文章

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