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: UNIPROT:P67775 (
alpha isoform
)
797
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
On the basis of previous pharmacophore modeling studies of naphthoquinones derivatives, we have designed and synthesized a new set of pyranonaphthoquinones. These compounds were obtained through a direct and highly efficient approach based on an intramolecular domino Knoevenagel hetero Diels-Alder reaction from lawsone (
2-hydroxynaphthoquinone
) and a variety of aldehydes containing an alkene. The synthesized pyranonaphthoquinones were evaluated against the
alpha isoform
of human topoisomerase II (hTopoIIalpha). Among the 11 derivatives studied, we found that six of them act as catalytic inhibitors of the enzyme in vitro. These six derivatives strongly preclude the enzyme from decatenating or relaxing suitable substrates. Finally, we correlate their active/inactive status with docking studies of these novel compounds into the ATPase domain of hTopoIIalpha.
...
PMID:Design and synthesis of a novel series of pyranonaphthoquinones as topoisomerase II catalytic inhibitors. 1881 45
