Naphtho[2,3-f]indole-5,10-dione aminoalkyl derivatives: a new class of topoisomerase I inhibitors.
Naphtho[2,3-f]indole-5,10-dione aminoalkyl derivatives in cytotoxic concentrations inhibit topoisomerase I, which is an important factor of antitumor activity of compounds of this chemical class. The degree of topoisomerase I inhibition with naphtho[2,3-f]indole-5,10-dione derivatives depends on the structure and position of active (aminoalkyl) groups. The mechanism of topoisomerase I inhibition with aminoalkylnaph-tho[2,3-f]indole-5,10-diones differs from specific blocking of the catalytic activity of the enzyme and depends on interactions of these compounds with DNA.
Dezhenkova
L G
LG
G. F. Gauze Institute for Search for New Antibiotics, Russian Academy of Medical Sciences.
Susova
O Y
OY
Shchekotikhin
A E
AE
Preobrazhenskaya
M N
MN
Shtil
A A
AA
D000880:Anthraquinones / Q000494:pharmacology*; D004996:Ethidium / Q000494:pharmacology; D011758:Pyrroles / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors
C533991:4,11-dimethoxynaphtho(2,3-f)indole-5,10-dione; D000880:Anthraquinones; D011758:Pyrroles; D059004:Topoisomerase I Inhibitors; D004996:Ethidium