1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase.
The synthesis of a series of novel 1-[(benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles is described. The compounds were tested for human placental aromatase inhibition in vitro, using [1beta-3H]-androstenedione as the substrate for the aromatase enzyme, the percentage inhibition and IC50 data is included.
Vinh
T K
TK
Welsh School of Pharmacy, Cardiff University, UK.
Ahmadi
M
M
Delgado
P O
PO
Perez
S F
SF
Walters
H M
HM
Smith
H J
HJ
Nicholls
P J
PJ
Simons
C
C
D000616:Aminoglutethimide / Q000494:pharmacology; D000735:Androstenedione / Q000378:metabolism; D001141:Aromatase / Q000378:metabolism; D047072:Aromatase Inhibitors; D001572:Benzofurans / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D007659:Ketones / Q000138:chemical synthesis; D010920:Placenta / Q000201:enzymology; D011247:Pregnancy; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000737:chemistry*; D014230:Triazoles / Q000737:chemistry*
D047072:Aromatase Inhibitors; D001572:Benzofurans; D004791:Enzyme Inhibitors; D007659:Ketones; D013777:Tetrazoles; D014230:Triazoles; D000616:Aminoglutethimide; D000735:Androstenedione; D001141:Aromatase