Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:5.99.1.2 (
topoisomerase
)
9,166
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Isoaurostatin A (IAS-A) isolated from Thermomonospora alba showed weak inhibition against
topoisomerase
(topo) I (IC(50)=307microM). To get more strong inhibition, derivatives of
IAS
-A were prepared and their structure-activity relationships against topo I and II were investigated. The addition of hydroxyl group on aromatic rings increased the activities, 3-(3,4,5-trihydroxybenzylidene)-5-hydroxy-3H-benzofuran-2-one (IAS-9) showed strong inhibition (IC(50)=3microM) against topo I. And also, the increasing of hydroxyl group increased growth inhibition against a variety of cancer cells, and
IAS
-9 showed most potent inhibition. Unlike camptothecin and etoposide,
IAS
-9 neither stabilized DNA-topo cleavable complex nor intercalated into DNA, and it inhibited topo I and II noncompetitively. The inhibitory activities also increased by opening of lactone ring in the molecule of
IAS
-9.
...
PMID:Inhibitory activities against topoisomerase I and II by isoaurostatin derivatives and their structure-activity relationships. 1580 69
