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Journal of Enzyme Inhibition Volume 2, 1988 - Issue 3
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Research Article

Structure-Activity Relationships for Non-Steroidal Inhibitors of Aromatase

L. Banting Welsh School of Pharmacy, UWIST Cathays Park, Cardiff, CFI 3XF, UK
,
H. J. Smith Welsh School of Pharmacy, UWIST Cathays Park, Cardiff, CFI 3XF, UK
,
M. James Welsh School of Pharmacy, UWIST Cathays Park, Cardiff, CFI 3XF, UK
,
G. Jones Welsh School of Pharmacy, UWIST Cathays Park, Cardiff, CFI 3XF, UK
,
W. Nazareth Welsh School of Pharmacy, UWIST Cathays Park, Cardiff, CFI 3XF, UK
,
P. J. Nicholls Welsh School of Pharmacy, UWIST Cathays Park, Cardiff, CFI 3XF, UK
,
M. J. E. Hewlins University College, PO Box 78, Cardiff, CF1 lXL, UK
&
M. G. Rowlands Drug Development Section, Institute of Cancer Research, Sutton, Surrey, SM2 5PX, UK
 show all
Pages 215-229 | Received 15 Nov 1987, Published online: 27 Sep 2008

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Robert W Brueggemeier. (2002) Aromatase inhibitors in breast cancer therapy. Expert Review of Anticancer Therapy 2:2, pages 181-191.
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H John Smith, Paul J Nicholls, Claire Simons & Regis Le Lain. (2001) Inhibitors of steroidogenesis as agents for the treatment of hormone-dependent cancers. Expert Opinion on Therapeutic Patents 11:5, pages 789-824.
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Safa Moslemi & Gilles-Eric Seralini. (1997) Inhibition and inactivation of equine aromatase by steroidal and non-steroid al compounds. A comparison with human aromatase inhibition. Journal of Enzyme Inhibition 12:4, pages 241-254.
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Sabbir Ahmed. (1997) The Mechanism of a P-450 Enzyme-Aromatase; a Molecular Modelling Perspective for the Removal of the C(19) Methyl and Aromatisation of the Steroid a Ring. Journal of Enzyme Inhibition 12:1, pages 59-70.
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B. A. J. Evans, S. C. Stillman, I. A. Hughes, P. J. Nicholls & H. J. Smith. (1993) Screening and Determination of Kinetic Parameters of Aromatase Inhibitors Using Human Genital Skin Fibroblasts. Journal of Enzyme Inhibition 7:3, pages 203-212.
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R. Whomsley, H. J. Smith, P. J. Nicholls, W. Nazareth & M. Ahmadi. (1993) Some 1-, and 3-Substituted 3-(4 - Aminophenyl)Pyrrolidine-2,5-Diones as Selective Inhibitors of Aromatase. Journal of Enzyme Inhibition 6:4, pages 317-330.
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Patrick Van Roey, Keith A. Bullion, Yoshio Osawa, Leslie J. Browne, Robert M. Bowman & Dietmar G. Braun. (1991) Structure-Activity Studies of Non-Steroidal Aromatase Inhibitors: The Crystal and Molecular Structures of CGS 16949A and CGS 18320B. Journal of Enzyme Inhibition 5:2, pages 119-132.
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Robert W. Brueggemeier. (1990) Biochemical and Molecular Aspects of Aromatase. Journal of Enzyme Inhibition 4:2, pages 101-111.
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Articles from other publishers (30)

Nilanjan Adhikari, Sk. Abdul Amin, Achintya Saha & Tarun Jha. (2017) Combating breast cancer with non-steroidal aromatase inhibitors (NSAIs): Understanding the chemico-biological interactions through comparative SAR/QSAR study. European Journal of Medicinal Chemistry 137, pages 365-438.
Crossref
Tarun Jha, Nilanajn Adhikari, Amit Kumar Halder & Achintya Saha. 2017. Oncology. Oncology 118 186 .
Tarun Jha, Nilanajn Adhikari, Amit Kumar Halder & Achintya Saha. 2015. Quantitative Structure-Activity Relationships in Drug Design, Predictive Toxicology, and Risk Assessment. Quantitative Structure-Activity Relationships in Drug Design, Predictive Toxicology, and Risk Assessment 400 470 .
K J Barrell, W L Woo, M Ahmadi, H J Smith & P J Nicholls. (1996) Synthesis and Biological Evaluation of 3-(Prop-2-enyl)- and 3-(Prop-2-ynyl)pyrrolidine-2,5-dione Derivatives as Potential Aromatase Inhibitors. Journal of Pharmacy and Pharmacology 48:2, pages 154-159.
Crossref
Donald J. AbrahamRobert W. Brueggemeier. 2003. Burger's Medicinal Chemistry and Drug Discovery. Burger's Medicinal Chemistry and Drug Discovery 153 218 .
Robert W. Brueggemeier, John C. Hackett & Edgar S. Diaz-Cruz. (2005) Aromatase Inhibitors in the Treatment of Breast Cancer. Endocrine Reviews 26:3, pages 331-345.
Crossref
H.S. Yathirajan, C.R. Raju, K.M. Lokanatha Rai, K. Jailakshmi, P. Nagaraja, K. Palani, M.N. Ponnuswamy & M. Nethaji. (2005) Crystal structure of bis(2-butyl-4-chloro-imidazole)5-iminoethane. Journal of Chemical Crystallography 35:3, pages 211-215.
Crossref
Sabbir Ahmed, Shaheen Adat, Annabel Murrells, Caroline P Owen & Yonas Amanuel. (2002) Design, synthesis, and evaluation of 4-(4?-aminobenzyl)-2-oxazolidinones as novel inhibitors of the cytochrome P-450 enzyme aromatase. Bioorganic Chemistry 30:5, pages 315-331.
Crossref
Robert W. Brueggemeier. (2001) Aromatase, Aromatase Inhibitors, and Breast Cancer. American Journal of Therapeutics 8:5, pages 333-344.
Crossref
Sabbir Ahmed. (2000) The Use of the Novel Substrate–Heme Complex Approach in the Derivation of a Representation of the Active Site of the Enzyme Cholesterol Side Chain Cleavage. Biochemical and Biophysical Research Communications 274:3, pages 821-824.
Crossref
Sabbir Ahmed & Yonas Amanuel. (2000) Synthesis and Biochemical Evaluation of Novel Inhibitors of Aromatase (AR) Using an Enhanced Representation of the Active Site of AR Derived from the Consideration of the Reaction Mechanism. Biochemical and Biophysical Research Communications 267:1, pages 356-361.
Crossref
Sabbir Ahmed. (1999) A novel molecular modelling study of inhibitors of the 17?-hydroxylase component of the enzyme system 17?-hydroxylase/17,20-lyase (P-450 17? ). Bioorganic & Medicinal Chemistry 7:8, pages 1487-1496.
Crossref
Sabbir Ahmed & Jason Keane. (1998) Modeling Study of Some Inhibitors of 17,20-Lyase, a Component of the Enzyme 17?-Hydroxylase/ 17,20-Lyase: A Novel Approach. Biochemical and Biophysical Research Communications 253:2, pages 273-276.
Crossref
Sabbir Ahmed. (1998) Aromatase ? its mechanism and mode of action of some inhibitors ? a molecular modelling perspective. Journal of Molecular Structure: THEOCHEM 422:1-3, pages 271-284.
Crossref
Robert W. Brueggemeier, Jill M. O'Reilly, Carl J. Lovely, Patrick J. Ward, Anne L. Quinn, David Baker, Michael V. Darby, Xin-Ju Gu & Nancy E. Gilbert. (1997) Biochemistry and pharmacology of 7α-substituted androstenediones as aromatase inhibitors. The Journal of Steroid Biochemistry and Molecular Biology 61:3-6, pages 247-254.
Crossref
S. Chen, Y.-C. Kao & C.A. Laughton. (1997) Binding characteristics of aromatase inhibitors and phytoestrogens to human aromatase. The Journal of Steroid Biochemistry and Molecular Biology 61:3-6, pages 107-115.
Crossref
Jill M. O'Reilly & Robert W. Brueggemeier. (1996) 7α-Arylaliphatic androsta-1,4-diene-3,17-diones as enzyme-activated irreversible inhibitors of aromatase. The Journal of Steroid Biochemistry and Molecular Biology 59:1, pages 93-102.
Crossref
L. Banting. 1996. 147 184 .
Sabbir Ahmed. (1995) Molecular modelling of inhibitors of 17?-Hydroxylase ? a novel approach. Bioorganic & Medicinal Chemistry Letters 5:23, pages 2795-2800.
Crossref
Sabbir Ahmed & Paul J Davis. (1995) Molecular modelling of inhibitors of aromatase ? a novel approach. Bioorganic & Medicinal Chemistry Letters 5:15, pages 1673-1678.
Crossref
Christopher Pepper, H. John Smith, Paul J. Nicholls, Kevin J. Barrell & Massoud Ahmadi. (2004) Enantioselectivity of aromatase inhibitors: Substituted 3‐(4‐aminophenyl)pyrrolidine‐2,5‐diones. Chirality 7:5, pages 376-380.
Crossref
D. Zhou, L.L. Cam, C.A. Laughton, K.R. Korzekwa & S. Chen. (1994) Mutagenesis study at a postulated hydrophobic region near the active site of aromatase cytochrome P450.. Journal of Biological Chemistry 269:30, pages 19501-19508.
Crossref
Robert W. Brueggemeier. (1994) Aromatase inhibitors ? mechanisms of steroidal inhibitors. Breast Cancer Research and Treatment 30:1, pages 31-42.
Crossref
R. Whomsley, E. Fernandez, P.J. Nicholls, H.J. Smith, P. Lombardi & V. Pestellini. (1993) Substituted 1-[(benzofuran-2-YL)-phenylmethyl]-imidazoles as potent inhibitors of aromatase in vitro and in female rats in vivo. The Journal of Steroid Biochemistry and Molecular Biology 44:4-6, pages 675-676.
Crossref
M. Lang, Ch. Batzl, P. Furet, R. Bowman, A. Häusler & A.S. Bhatnagar. (1993) Structure-activity relationships and binding model of novel aromatase inhibitors. The Journal of Steroid Biochemistry and Molecular Biology 44:4-6, pages 421-428.
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C.A. Laughton, M.J.J.M. Zvelbil & S. Neidle. (1993) A detailed molecular model for human aromatase. The Journal of Steroid Biochemistry and Molecular Biology 44:4-6, pages 399-407.
Crossref
Patrick J. Bednarski & Rolf W. Hartmann. (2006) Synthesis and Evaluation of Sulfur‐Containing Glutethimide Derivatives for Aromatase and Desmolase Inhibitory Activity. Archiv der Pharmazie 326:7, pages 391-394.
Crossref
Michael Jarman. 1992. New Approaches in Cancer Pharmacology: Drug Design and Development. New Approaches in Cancer Pharmacology: Drug Design and Development 47 62 .
. 1990. Chirality in Drug Design and Synthesis. Chirality in Drug Design and Synthesis 215 236 .
John P. Mallamo & Paul E. Juniewicz. 1989. 197 206 .

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