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:5.99.1.3 (
topoisomerase
)
9,911
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Unlike other
DNA topoisomerase II
(topo II) inhibitors, our recently identified acridone derivative E17 exerted strong cytotoxic activity by inhibiting topo II without causing topo II degradation and DNA damage, which promoted us to explore more analogues of E17 by expanding its chemical diversification and enrich the structure-activity relationship (SAR) outcomes of acridone-oriented chemotypes. To achieve this goal, 42 novel acridone derivatives were synthesized and evaluated for their antiproliferative efficacies. SAR investigations revealed that orientation and spatial topology of R
3
substituents make greater contributions to the bioactivity, exemplified by compounds E24,
E25
and E27, which has provided valuable information for guiding further development of acridone derivatives as promising drug candidates.
...
PMID:Structure-activity relationship of novel acridone derivatives as antiproliferative agents. 3319 Oct 85
