Target Validation Information
TTD ID T13260
Target Name Aromatase (CYP19A1)
Type of Target
Successful
Drug Potency against Target Drug Info IC50 = 15 nM [35]
Aminoglutethimide Drug Info IC50 = 18500 nM [36]
Exemestane Drug Info IC50 = 5 nM [35]
Letrozole Drug Info IC50 = 0.8 nM [35]
Drug Info IC50 = 2100 nM [34]
Drug Info IC50 = 11.45 nM
Drug Info IC50 = 16.5 nM
Drug Info IC50 = 1840 nM
Drug Info IC50 = 9740 nM [5]
Drug Info IC50 = 100 nM [5]
Drug Info IC50 = 130 nM [5]
Drug Info IC50 = 5430 nM [5]
Drug Info IC50 = 2540 nM [5]
Drug Info IC50 = 2830 nM [26]
Drug Info IC50 = 1820 nM
Drug Info IC50 = 4830 nM [5]
Drug Info IC50 = 4060 nM [5]
Drug Info IC50 = 4600 nM [5]
Drug Info IC50 = 350 nM [22]
Drug Info IC50 = 55 nM [22]
Drug Info IC50 = 8400 nM [29]
Drug Info IC50 = 0.5 nM [3]
Drug Info IC50 = 15 nM [25]
Drug Info IC50 = 760 nM [22]
Drug Info IC50 = 170 nM [22]
Drug Info IC50 = 3 nM [25]
Drug Info IC50 = 4600 nM [2]
Drug Info Ki = 52.7 nM [22]
Drug Info IC50 = 3700 nM [15]
Drug Info IC50 = 2760 nM
Drug Info IC50 = 20 nM [25]
Drug Info IC50 = 1100 nM [34]
Drug Info IC50 = 7370 nM [5]
Drug Info Ki = 120 nM [27]
Drug Info IC50 = 3551 nM [11]
Drug Info IC50 = 3400 nM [15]
Drug Info IC50 = 17 nM [9]
Drug Info IC50 = 16800 nM [12]
Drug Info IC50 = 300 nM [24]
Drug Info IC50 = 9700 nM [2]
Drug Info IC50 = 770 nM [7]
Drug Info IC50 = 11000 nM [18]
(+/-)-7-methoxy-2-(4-methoxyphenyl)chroman-4-one Drug Info IC50 = 1860 nM [14]
(+/-)-7-methoxy-2-phenylchroman-4-one Drug Info IC50 = 8000 nM [15]
(2S)-5,7,2',4'-tetrahydroxyflavanone Drug Info IC50 = 2200 nM [2]
(2S)-abyssinone II Drug Info IC50 = 400 nM [2]
(2S)-euchrenone a7 Drug Info IC50 = 3400 nM [2]
1-(1-Benzyl-2-biphenyl-4-yl-ethyl)-1H-imidazole Drug Info IC50 = 950 nM [19]
1-(2-(benzo[b]thiophen-4-yl)ethyl)-1H-imidazole Drug Info IC50 = 3560 nM [22]
1-(2-phenoxybenzyl)-1H-imidazole Drug Info IC50 = 389.2 nM
1-(3-(4-fluorophenyl)propyl)-1H-imidazole Drug Info IC50 = 310 nM [25]
1-(3-Methoxy-naphthalen-2-yl)-1H-imidazole Drug Info IC50 = 129 nM [8]
1-(4-Cyanobenzyl)-5-methyl-1H-imidazole Drug Info IC50 = 15 nM [16]
1-(4-Nitro-2-phenylsulfanylbenzyl)-1H-imidazole Drug Info IC50 = 5.59 nM
1-(7-Methoxy-2-phenyl-chroman-4-yl)-1H-imidazole Drug Info IC50 = 90 nM [4]
1-(9-phenyl-9H-fluoren-9-yl)-1H-1,2,4-triazole Drug Info IC50 = 4000 nM [22]
1-(9-Phenyl-9H-fluoren-9-yl)1H-imidazole Drug Info IC50 = 74 nM [25]
1-(9H-fluoren-9-yl)-1H-imidazole Drug Info IC50 = 2850 nM [22]
1-(biphenyl-3-ylmethyl)-1H-1,2,4-triazole Drug Info IC50 = 210 nM [24]
1-Bromo-4-imidazol-1-ylmethyl-xanthen-9-one Drug Info IC50 = 89 nM [34]
1-Ethyl-5-(imidazol-1-yl-phenyl-methyl)-1H-indole Drug Info IC50 = 205 nM [1]
1-Imidazol-1-ylmethyl-4-nitro-xanthen-9-one Drug Info IC50 = 970 nM [34]
1-Imidazol-1-ylmethylxanthen-9-one Drug Info IC50 = 150 nM
1-Naphthalen-2-yl-1H-imidazole Drug Info IC50 = 2821 nM [8]
1-[(7-Fluoronaphth-2-yl)methyl]-1H-imidazole Drug Info IC50 = 160 nM [25]
10-EPI-8-DEOXY-CUMAMBRIN B Drug Info IC50 = 7 nM [25]
11BETA,13-DIHYDRO-10-EPI-8-DEOXYCUMAM-BRIN B Drug Info IC50 = 2 nM [25]
2,3,4-Trimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 3570 nM
2,3,5-Trimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 2280 nM
2,3-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 980 nM
2,4-Dimethoxy-3'-amino-trans-stilbene Drug Info IC50 = 11140 nM
2,4-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 760 nM
2-(1H-Imidazol-1-yl)-1-(4-nitrophenyl)ethanone Drug Info IC50 = 190 nM
2-(3-hydroxyphenyl)-7-methoxychroman-4-one Drug Info IC50 = 3500 nM [15]
2-Imidazol-1-ylmethylxanthen-9-one Drug Info IC50 = 7900 nM
2-phenyl-2,3-dihydrobenzo[h]chromen-4-one Drug Info IC50 = 4300 nM [15]
2-Phenyl-4-[1,2,4]triazol-1-yl-chroman-7-ol Drug Info IC50 = 430 nM [4]
3,4'-(Ethane-1,2-diyl)dibenzenamine Drug Info IC50 = 3210 nM
3,4,5-Trimethoxy-3'-amino-trans-stilbene Drug Info IC50 = 16420 nM
3,4,5-Trimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 900 nM
3,4-bis(3,4-dimethoxyphenyl)furan-2(5H)-one Drug Info IC50 = 1 nM [25]
3,4-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 14510 nM
3,5-Diacetoxy-4'-amino-trans-stilbene Drug Info IC50 = 2940 nM
3,5-Diamino-4'-amino-trans-stilbene Drug Info IC50 = 8510 nM
3,5-Dihydroxyl-4'-amino-trans-stilbene Drug Info IC50 = 5000 nM
3,5-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 590 nM
3-((1H-imidazol-1-yl)methyl)-9H-xanthen-9-one Drug Info IC50 = 390 nM
3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine Drug Info IC50 = 1507 nM [11]
3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine Drug Info IC50 = 6045 nM [11]
3-(2,2-Diphenyl-vinyl)-pyridine Drug Info IC50 = 3630 nM [5]
3-(3,4-dihydronaphthalen-2-yl)pyridine Drug Info IC50 = 4073 nM [11]
3-(3-methyl-3,4-dihydronaphthalen-2-yl)pyridine Drug Info IC50 = 1787 nM [11]
3-(4-Amino-phenyl)-1-methyl-pyrrolidine-2,5-dione Drug Info IC50 = 10040 nM [29]
3-(4-Amino-phenyl)-3-methyl-pyrrolidine-2,5-dione Drug Info IC50 = 10040 nM [29]
3-(4-Amino-phenyl)-pyrrolidine-2,5-dione Drug Info IC50 = 10200 nM [29]
3-(5-Bromo-6-methoxy-naphthalen-2-yl)-pyridine Drug Info IC50 = 9107 nM [8]
3-(5-Chloro-6-methoxy-naphthalen-2-yl)-pyridine Drug Info IC50 = 1805 nM [8]
3-(6-Ethoxy-naphthalen-2-yl)-pyridine Drug Info IC50 = 6638 nM [8]
3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine Drug Info IC50 = 814 nM [11]
3-(6-methoxynaphthalen-2-yl)pyridine Drug Info IC50 = 600 nM [21]
3-(imidazolylmethyl)-4'-methoxyflavone Drug Info IC50 = 80 nM [13]
3-(imidazolylmethyl)-4'-nitroflavone Drug Info IC50 = 45 nM [13]
3-(imidazolylmethyl)-7-methoxy-4'-nitroflavone Drug Info IC50 = 470 nM [13]
3-(imidazolylmethyl)flavone Drug Info IC50 = 71 nM [13]
3-(naphthalen-2-yl)pyridine Drug Info IC50 = 5700 nM [21]
3-Amino-4'-amino-trans-stilbene Drug Info IC50 = 7470 nM
3-Fluoren-9-ylidenemethyl-pyridine Drug Info IC50 = 4810 nM [5]
3-Fluoro-4'-(pyridin-4-ylmethyl)biphenyl-4-ol Drug Info IC50 = 2693 nM [26]
3-Indan-(1E)-ylidenemethyl-pyridine Drug Info IC50 = 2040 nM [5]
3-Indan-(1Z)-ylidenemethyl-pyridine Drug Info IC50 = 3550 nM [5]
3-Methoxyl-4'-amino-trans-stilbene Drug Info IC50 = 3080 nM
3-Nitro-4'-nitro-trans-stilbene Drug Info IC50 = 8330 nM
3-[3-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 3680 nM [5]
3-[3-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 2800 nM [5]
3-[4-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 230 nM [5]
3-[4-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 1810 nM [5]
3-[4-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 180 nM [5]
3-[4-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 4720 nM [5]
3-[4-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 12630 nM [5]
3-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 7830 nM [5]
3-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 4260 nM [5]
3-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 4050 nM [5]
3-[5-Ethoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 7080 nM [5]
3-[5-Ethoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 7680 nM [5]
3-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 2490 nM [5]
3-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 4310 nM [5]
3-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 5570 nM [5]
3-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 6360 nM [5]
3-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 3930 nM [5]
4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diol Drug Info IC50 = 2440 nM [26]
4'-bromo-3-(imidazolylmethyl)-7-methoxyflavone Drug Info IC50 = 4100 nM [13]
4'-bromo-3-(imidazolylmethyl)flavone Drug Info IC50 = 440 nM [13]
4'-cyano-3-(imidazolylmethyl)-7-methoxyflavone Drug Info IC50 = 1800 nM [13]
4'-cyano-3-(imidazolylmethyl)flavone Drug Info IC50 = 69 nM [13]
4-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one Drug Info IC50 = 2100 nM [22]
4-((1H-imidazol-1-yl)methyl)benzonitrile Drug Info IC50 = 15 nM [16]
4-(1-Imidazol-1-yl-vinyl)-benzonitrile Drug Info IC50 = 0.7 nM [31]
4-(3,4,5-Trimethoxyphenethyl)aniline Drug Info IC50 = 2790 nM
4-(3,4-Dimethoxyphenethyl)aniline Drug Info IC50 = 670 nM
4-ANDROSTENE-3-17-DIONE Drug Info Ki = 20 nM [30]
4-Bromo-1-imidazol-1-ylmethyl-xanthen-9-one Drug Info IC50 = 940 nM [34]
4-Fluoren-9-ylidenemethyl-pyridine Drug Info IC50 = 2740 nM [5]
4-Imidazol-1-yl-2-phenyl-chroman-7-ol Drug Info IC50 = 40 nM [4]
4-Imidazol-1-ylmethyl-1-nitro-xanthen-9-one Drug Info IC50 = 40 nM [34]
4-Imidazol-1-ylmethyl-2-nitroxanthen-9-one Drug Info IC50 = 53 nM
4-Imidazol-1-ylmethyl-3-nitroxanthen-9-one Drug Info IC50 = 1900 nM
4-Imidazol-1-ylmethylthioxanthen-9-one Drug Info IC50 = 3.98 nM
4-Imidazol-1-ylmethylxanthen-9-one Drug Info IC50 = 17 nM
4-Indan-(1E)-ylidenemethyl-pyridine Drug Info IC50 = 6700 nM [5]
4-Indan-(1Z)-ylidenemethyl-pyridine Drug Info IC50 = 12730 nM [5]
4-[(3'-Hydroxybiphenyl-4-yl)methyl]pyridine Drug Info IC50 = 663 nM [26]
4-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine Drug Info IC50 = 3070 nM [26]
4-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 3400 nM [5]
4-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 1990 nM [5]
4-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 1550 nM [5]
4-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 800 nM [5]
4-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 3960 nM [5]
4-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 3720 nM [5]
4-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 280 nM [5]
4-[6-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 770 nM [5]
4-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 1280 nM [5]
4-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 1710 nM [5]
5-Indan-(1E)-ylidenemethyl-1H-imidazole Drug Info IC50 = 955 nM [6]
5-Indan-(1Z)-ylidenemethyl-1H-imidazole Drug Info IC50 = 130 nM [6]
5-[5-Bromo-indan-(1E)-ylidenemethyl]-1H-imidazole Drug Info IC50 = 27 nM [6]
5-[5-Bromo-indan-(1Z)-ylidenemethyl]-1H-imidazole Drug Info IC50 = 100 nM [6]
5-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyrimidine Drug Info IC50 = 7450 nM [5]
5-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyrimidine Drug Info IC50 = 790 nM [5]
5-[5-Methoxy-indan-(1E)-ylidenemethyl]-thiazole Drug Info IC50 = 4330 nM [5]
6-Imidazol-1-yl-isoquinoline Drug Info IC50 = 3060 nM [22]
7,4'-Dihydroxyflavone Drug Info IC50 = 2 nM [25]
7-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one Drug Info IC50 = 680 nM [22]
7-((1H-imidazol-1-yl)methyl)-4H-chromen-4-one Drug Info IC50 = 100 nM [22]
7-((1H-imidazol-1-yl)methyl)isoquinoline Drug Info IC50 = 1380 nM [22]
7-hydroxy-2-phenylchroman-4-one Drug Info IC50 = 3800 nM [15]
7-[1,2,4]Triazol-4-ylmethyl-chromen-4-one Drug Info IC50 = 3700 nM [34]
ALBANOL A Drug Info IC50 = 7500 nM [2]
ALPHA-NAPHTHOFLAVONE Drug Info IC50 = 70 nM [25]
APIGENIN Drug Info IC50 = 900 nM [25]
Benzyl-biphenyl-4-ylmethyl-imidazol-1-yl-amine Drug Info IC50 = 1200 nM [19]
biochanin A Drug Info IC50 = 10.2 nM [25]
Chrysin Drug Info IC50 = 1 nM [25]
flavone Drug Info IC50 = 8 nM [25]
Gamma-mangostin Drug Info IC50 = 4970 nM [17]
GARCINONE D Drug Info IC50 = 5200 nM [17]
Isogemichalcone C Drug Info IC50 = 7100 nM [2]
ISOLICOFLAVONOL Drug Info IC50 = 100 nM [2]
LIAROZOLE Drug Info IC50 = 5 nM [25]
LIQUIRTIGENIN Drug Info IC50 = 340 nM [18]
LUDARTIN Drug Info IC50 = 55 nM [25]
MDL-18962 Drug Info IC50 = 56.2 nM [32]
MONODICTYOCHROMONE B Drug Info IC50 = 16500 nM [20]
MR-16089 Drug Info IC50 = 40 nM [25]
MR-20492 Drug Info IC50 = 200 nM [25]
MR-20494 Drug Info IC50 = 110 nM [25]
MR-20496 Drug Info Ki = 10.3 nM [33]
N-(2-hexyloxy-4-nitrophenyl)methanesulfonamide Drug Info IC50 = 2670 nM [10]
N-(2-nonyloxy-4-nitrophenyl)methanesulfonamide Drug Info IC50 = 910 nM [10]
N-(2-Propyloxy-4-nitrophenyl)methanesulfonamide Drug Info IC50 = 2510 nM [10]
N-[2-(4'-Nitrophenyl)ethyl]-imidazole Drug Info IC50 = 160 nM [25]
NARINGENIN Drug Info IC50 = 2.9 nM [25]
NSC-122427 Drug Info IC50 = 15500 nM [23]
NSC-12999 Drug Info Ki = 25.5 nM [22]
NSC-131736 Drug Info IC50 = 1400 nM [22]
NSC-289311 Drug Info Ki = 6.5 nM [22]
NSC-356483 Drug Info IC50 = 3100 nM [22]
NSC-356781 Drug Info IC50 = 2100 nM [22]
NSC-368272 Drug Info Ki = 5.6 nM [22]
NSC-368280 Drug Info Ki = 1.9 nM [22]
NSC-613604 Drug Info Ki = 385 nM [23]
NSC-666292 Drug Info Ki = 33.4 nM [22]
NSC-683634 Drug Info Ki = 15.1 nM [22]
NSC-75308 Drug Info IC50 = 5600 nM [22]
NSC-93358 Drug Info Ki = 266 nM [23]
NSC-94258 Drug Info IC50 = 30.5 nM [25]
NSC-94891 Drug Info IC50 = 9800 nM [23]
Rogletimide Drug Info Ki = 14000 nM [28]
Action against Disease Model Testolactone Drug Info Potency and selectivity of aromatase inhibition are parameters which ultimately influence the therapeutic efficacy of aromatase inhibitors. This report describes an in vitro model which allows an assessment of the selectivity with which aromatase inhibitors inhibit estrogen biosynthesis. Estrogen production was stimulated by incubating adult female hamster ovarian tissue with ovine LH. The production rates of estrogens (E), testosterone (T) and progesterone (P) were determined using radioimmunoassays to measure the amount of these steroids released into the incubation medi uM over a 4-hour incubation period. The selectivity of aromatase inhibition was assessed by determining the IC50S with which each inhibitor inhibited the production of E (end product), T (immediateprecursor of E) and P (early precursor of E). Selectivity was studied for each of the 4 aromatase inhibitors, CGS 16949A (a new non-steroidal compound), 4-OH-androstenedione, aminoglutethimide and testolactone. CGS 16949A was the most potent of the four, followed by 4-OH-androstenedione, aminoglutethimide and testolactone. As far as selectivity was concerned, both CGS 16949A and 4-OH-androstenedione selectively inhibited aromatase judging from the IC50s for E and P production (CGS 16949A: IC50 for E & P = 0.03 & 160 microM, resp.; 4-OH-androstenedione: IC50 for E & P = 0.88 & greater than or equal to 330 microM, resp.). Aminoglutethimide was the least selective inhibitor of aromatase (IC50 for E & P = 13 & 60 microM, resp.). For testolactone, the least potent of the four (IC50 for E = 130microM), no conclusive data were obtained concerning the selectivity of aromatase inhibition. Thus a simple, effective and reproducible method is described for assessing the selectivity with which aromatase inhibitors inhibit aromatase. [37]
References
REF 1 New selective nonsteroidal aromatase inhibitors: synthesis and inhibitory activity of 2,3 or 5-(alpha-azolylbenzyl)-1H-indoles. Bioorg Med Chem Lett. 1999 Feb 8;9(3):333-6.
REF 2 Aromatase inhibitors from Broussonetia papyrifera. J Nat Prod. 2001 Oct;64(10):1286-93.
REF 3 First dual aromatase-steroid sulfatase inhibitors. J Med Chem. 2003 Jul 17;46(15):3193-6.
REF 4 Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5215-8.
REF 5 Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitor... J Med Chem. 2005 Mar 10;48(5):1563-75.
REF 6 Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase. J Med Chem. 2005 Mar 24;48(6):1796-805.
REF 7 Synthesis and characterization of azole isoflavone inhibitors of aromatase. Bioorg Med Chem. 2005 Jun 2;13(12):4063-70.
REF 8 Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart fa... J Med Chem. 2005 Oct 20;48(21):6632-42.
REF 9 Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach. J Med Chem. 2005 Nov 17;48(23):7282-9.
REF 10 Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition. J Med Chem. 2006 Feb 23;49(4):1413-9.
REF 11 Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B... J Med Chem. 2006 Apr 6;49(7):2222-31.
REF 12 Interference by naturally occurring fatty acids in a noncellular enzyme-based aromatase bioassay. J Nat Prod. 2006 Apr;69(4):700-3.
REF 13 Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme. J Med Chem. 2006 Jul 27;49(15):4777-80.
REF 14 Synthesis and biological evaluation of (+/-)-abyssinone II and its analogues as aromatase inhibitors for chemoprevention of breast cancer. J Med Chem. 2007 Jun 14;50(12):2799-806.
REF 15 New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation. Bioorg Med Chem. 2008 Feb 1;16(3):1474-80.
REF 16 Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease. J Med Chem. 1991 Feb;34(2):725-36.
REF 17 Xanthones from the botanical dietary supplement mangosteen (Garcinia mangostana) with aromatase inhibitory activity. J Nat Prod. 2008 Jul;71(7):1161-6.
REF 18 Screening of herbal constituents for aromatase inhibitory activity. Bioorg Med Chem. 2008 Sep 15;16(18):8466-70.
REF 19 CYP19 (aromatase): exploring the scaffold flexibility for novel selective inhibitors. Bioorg Med Chem. 2008 Sep 15;16(18):8349-58.
REF 20 Monodictyochromes A and B, dimeric xanthone derivatives from the marine algicolous fungus Monodictys putredinis. J Nat Prod. 2008 Nov;71(11):1793-9.
REF 21 In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-... J Med Chem. 2008 Dec 25;51(24):8077-87.
REF 22 Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors. J Med Chem. 2009 Jan 8;52(1):143-50.
REF 23 An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors. Eur J Med Chem. 2009 Oct;44(10):4121-7.
REF 24 Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template. J Med Chem. 2010 Mar 11;53(5):2155-70.
REF 25 Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19). Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64.
REF 26 Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prosta... J Med Chem. 2010 Aug 12;53(15):5749-58.
REF 27 Effects of steroid D-ring modification on suicide inactivation and competitive inhibition of aromatase by analogues of androsta-1,4-diene-3,17-dione. J Med Chem. 1989 Mar;32(3):651-8.
REF 28 Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substitu... J Med Chem. 1987 Sep;30(9):1550-4.
REF 29 Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione. J Med Chem. 1986 Apr;29(4):520-3.
REF 30 Synthesis of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their related 7-deoxy analogs as conformational and catalytic probes for the acti... J Med Chem. 1994 Jul 8;37(14):2198-205.
REF 31 Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds. J Med Chem. 1993 May 14;36(10):1393-400.
REF 32 6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase. J Med Chem. 1997 Sep 26;40(20):3263-70.
REF 33 Design and synthesis of a new type of non steroidal human aromatase inhibitors. Bioorg Med Chem Lett. 1998 May 5;8(9):1041-4.
REF 34 A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase. J Med Chem. 2001 Mar 1;44(5):672-80.
REF 35 The pharmacology of letrozole. J Steroid Biochem Mol Biol. 2003 Oct;87(1):35-45.
REF 36 Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: synthesis and inhibition of P450 aromatase. J Enzyme Inhib Med Chem. 2005 Apr;20(2):135-41.
REF 37 An in vitro method to determine the selective inhibition of estrogen biosynthesis by aromatase inhibitors. J Steroid Biochem. 1989 Jul;33(1):125-31.

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