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Targeting Chromatin Readers

Clinical pharmacology and therapeutics, 2013-04, Vol.93 (4), p.312-314

2013

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The discovery of potent cRaf1 kinase inhibitors

Bioorganic & medicinal chemistry letters, 2000-02, Vol.10 (3), p.223-226

2000

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6-Azasteroids : potent dual inhibitors of human type 1 and 2 steroid 5α-reductase

Journal of medicinal chemistry, 1993-12, Vol.36 (26), p.4313-4315

1993

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Unique preclinical characteristics of GG745, a potent dual inhibitor of 5AR

The Journal of pharmacology and experimental therapeutics, 1997-09, Vol.282 (3), p.1496

1997

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Asymmetric synthesis and Cram’s (chelate) rule

Pure and applied chemistry, 1991-01, Vol.63 (11), p.1591-1598

1991

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The small‐molecule MERTK inhibitor UNC2025 decreases platelet activation and prevents thrombosis

Journal of thrombosis and haemostasis, 2018-02, Vol.16 (2), p.352-363

2018

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A prodrug approach to the design of cRaf1 kinase inhibitors with improved cellular activity

Anti-cancer drug design, 2001-02, Vol.16 (1), p.1

2001

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NT-38 MerTK AS A TARGET IN GLIOBLASTOMA

Neuro-oncology (Charlottesville, Va.), 2014-11, Vol.16 (suppl 5), p.v166-v167

2014

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Discovery and development of GG745, a potent inhibitor of both isozymes of 5 alpha-reductase

Pharmaceutical biotechnology, 1998, Vol.11, p.393

1998

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Structure-activity relationship homology (SARAH): a conceptual framework for drug discovery in the genomic era

Chemistry & biology, 1999, Vol.6 (1), p.R3-R7

Frye, Stephen V

1999

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Prevention of chelation by an oxygen function through protection with a triisopropyl silyl group

Tetrahedron letters, 1986, Vol.27 (28), p.3223-3226

1986

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Chelates as intermediates in nucleophilic additions to alkoxy ketones according to Cram's rule (cyclic model)

Journal of the American Chemical Society, 1992-02, Vol.114 (5), p.1778-1784

1992

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17β-(N-tert-butylcarbamoyl)-4-aza-5α-androstan-1-en-3-one is an active site-directed slow time-dependent inhibitor of human steroid 5α-reductase 1

Biochemistry (Easton), 1994-03, Vol.33 (8), p.2291-2296

1994

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Retraction

Science (American Association for the Advancement of Science), 2002-12, Vol.298 (5602), p.2327

2002

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Synthesis of 2-aminobenzophenones via rapid halogen-lithium exchange in the presence of a 2-amino-N-methoxy-N-methylbenzamide

Journal of organic chemistry, 1991-05, Vol.56 (11), p.3750-3752

1991

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Mechanism of time-dependent inhibition of 5 alpha-reductases by delta 1-4-azasteroids: toward perfection of rates of time-dependent inhibition by using ligand-binding energies

Biochemistry (Easton), 1995-10, Vol.34 (41), p.13453-13459

1995

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Are chelates truly intermediates in Cram's chelate rule?

Journal of the American Chemical Society, 1990-08, Vol.112 (16), p.6130-6131

1990

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Inhibition of human steroid 5alpha reductases type I and II by 6-aza-steroids: structural determinants of one-step vs two-step mechanism

Biochemistry (Easton), 1996-03, Vol.35 (11), p.3457-3464

1996

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Asymmetric synthesis based on 1,3-oxathianes. IV: Mechanism of asymmetric induction in the reactions of oxathianyl ketones

Journal of the American Chemical Society, 1988, Vol.110 (2), p.484-489

1988

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Inhibition of Human Steroid 5α Reductases type I and II by 6-Aza-Steroids: Structural Determinants of One-Step vs Two-Step Mechanism

Biochemistry (Easton), 1996-03, Vol.35 (11), p.3457-3464

1996

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Nonenzymatic asymmetric synthesis of (R)-(-)- and (S)-(+)-mevalolactone in high enantiomeric purity

Journal of organic chemistry, 1985, Vol.50 (18), p.3402-3404

1985

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Asymmetric synthesis based on 1,3-oxathianes. 4. Mechanism of asymmetric induction in the reactions of oxathianyl ketones

Journal of the American Chemical Society, 1988, Vol.110 (2), p.484-489

1988

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Structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase by 6-azaandrost-4-en-3-ones: optimization of the C17 substituent

Journal of medicinal chemistry, 1995-07, Vol.38 (14), p.2621-2627

1995

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Asymmetric synthesis of (R)- and (S)-citramalate in high enantiomeric purity

Tetrahedron letters, 1985, Vol.26 (33), p.3907-3910

1985

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6-Azasteroids: structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase

Journal of medicinal chemistry, 1994-07, Vol.37 (15), p.2352-2360

1994

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Targeting Chromatin Readers

The discovery of potent cRaf1 kinase inhibitors

6-Azasteroids : potent dual inhibitors of human type 1 and 2 steroid 5α-reductase

Unique preclinical characteristics of GG745, a potent dual inhibitor of 5AR

Asymmetric synthesis and Cram’s (chelate) rule

The small‐molecule MERTK inhibitor UNC2025 decreases platelet activation and prevents thrombosis

A prodrug approach to the design of cRaf1 kinase inhibitors with improved cellular activity

NT-38 MerTK AS A TARGET IN GLIOBLASTOMA

Discovery and development of GG745, a potent inhibitor of both isozymes of 5 alpha-reductase

Structure-activity relationship homology (SARAH): a conceptual framework for drug discovery in the genomic era

Prevention of chelation by an oxygen function through protection with a triisopropyl silyl group

Chelates as intermediates in nucleophilic additions to alkoxy ketones according to Cram's rule (cyclic model)

17β-(N-tert-butylcarbamoyl)-4-aza-5α-androstan-1-en-3-one is an active site-directed slow time-dependent inhibitor of human steroid 5α-reductase 1

Retraction

Synthesis of 2-aminobenzophenones via rapid halogen-lithium exchange in the presence of a 2-amino-N-methoxy-N-methylbenzamide

Mechanism of time-dependent inhibition of 5 alpha-reductases by delta 1-4-azasteroids: toward perfection of rates of time-dependent inhibition by using ligand-binding energies

Are chelates truly intermediates in Cram's chelate rule?

Inhibition of human steroid 5alpha reductases type I and II by 6-aza-steroids: structural determinants of one-step vs two-step mechanism

Asymmetric synthesis based on 1,3-oxathianes. IV: Mechanism of asymmetric induction in the reactions of oxathianyl ketones

Inhibition of Human Steroid 5α Reductases type I and II by 6-Aza-Steroids: Structural Determinants of One-Step vs Two-Step Mechanism

Nonenzymatic asymmetric synthesis of (R)-(-)- and (S)-(+)-mevalolactone in high enantiomeric purity

Asymmetric synthesis based on 1,3-oxathianes. 4. Mechanism of asymmetric induction in the reactions of oxathianyl ketones

Structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase by 6-azaandrost-4-en-3-ones: optimization of the C17 substituent

Asymmetric synthesis of (R)- and (S)-citramalate in high enantiomeric purity

6-Azasteroids: structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase

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