Indolequinone antitumor agents: relationship between quinone structure and rate of metabolism by recombinant human NQO1.
A series of indolequinones bearing various functional groups has been synthesized, and the effects of substituents on the metabolism of the quinones by recombinant human NAD(P)H:quinone oxidoreductase (NQO1), and on the toxicity toward nonsmall cell lung cancer cells with either high NQO1 activity (H460) or with no detectable activity (H596) were studied.
Beall
H D
HD
School of Pharmacy, University of Colorado Health Sciences Center, Denver 80262, USA.
Hudnott
A R
AR
Winski
S
S
Siegel
D
D
Swann
E
E
Ross
D
D
Moody
C J
CJ
D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism; D018288:Carcinoma, Small Cell / Q000201:enzymology / Q000473:pathology; D006801:Humans; D007700:Kinetics; D008175:Lung Neoplasms / Q000201:enzymology / Q000473:pathology; D016660:NAD(P)H Dehydrogenase (Quinone) / Q000378:metabolism*; D011809:Quinones / Q000737:chemistry* / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D011809:Quinones; D011994:Recombinant Proteins; D016660:NAD(P)H Dehydrogenase (Quinone)