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Synthesis and Biological Evaluation of Amino-Pyridines as Androgen Receptor Antagonists for Stimulating Hair Growth and Reducing Sebum Production

research Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production

17 citations , August 2007 in “Bioorganic & Medicinal Chemistry Letters”

A compound made by Pfizer can potentially stimulate hair growth and reduce oil production, making it a good candidate for topical use.

research Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists

3 citations , May 2017 in “Bioorganic & medicinal chemistry letters”

New compounds were made that are promising for prostate cancer therapy.

Synthesis and Biological Evaluation of 4-(4-(Alkyl- and Phenylaminocarbonyl)benzoyl)benzoic Acid Derivatives as Non-Steroidal Inhibitors of Steroid 5α-Reductase Isozymes 1 and 2

research Synthesis and Biological Evaluation of 4-(4-(Alkyl-and Phenylaminocarbonyl)benzoyl)benzoic Acid Derivatives as Non-steroidal Inhibitors of Steroid 5α-Reductase Isozymes 1 and 2

8 citations , March 2002 in “Archiv Der Pharmazie”

The compound 4c effectively inhibits the enzyme linked to hair loss.

research Synthesis, Characterization and Evaluation of 5α, 6β-Dihalo Androsterone Derivatives as 5α-Reductase Inhibitors

May 2022 in “Current Enzyme Inhibition”

Compound 7b is a promising candidate for treating benign prostatic hyperplasia and prostate cancer.

research Design and synthesis of novel androgen receptor antagonists with sterically bulky icosahedral carboranes

45 citations , August 2005 in “Bioorganic & medicinal chemistry”

New compounds with carborane showed anti-androgen effects similar to flutamide.

research Cortexolone 17a-propionate: A new antiandrogen acting on hair dermal papilla cells for the treatment of androgenic alopecia

March 2014 in “Journal of The American Academy of Dermatology”

Cortexolone 17a-propionate may be an effective new treatment for hair loss.

research Synthesis of a 4-azasteroid hormones compound

January 2009 in “Xiandai huagong”

Finasteride was successfully synthesized from Pregnadienolone acetate.

New Progesterone Esters as 5α-Reductase Inhibitors

research New Progesterone Esters as 5.ALPHA.-Reductase Inhibitors.

22 citations , January 2001 in “Chemical & Pharmaceutical Bulletin”

Some new progesterone derivatives are better at blocking testosterone conversion than a common drug.

research Synthesis and Pharmacological Evaluation of New 16-Methyl Pregnane Derivatives.

18 citations , January 2002 in “Chemical & pharmaceutical bulletin/Chemical and pharmaceutical bulletin”

New pregnane derivatives were more effective than finasteride at inhibiting a key enzyme for male pattern baldness.

research Synthesis and 5α-Reductase Inhibitory Activity of C21 Steroids Having 1,4-diene or 4,6-diene 20-ones and 4-Azasteroid 20-Oximes

186 citations , December 2011 in “Molecules”

Three specific 4-azasteroid-2-oximes showed strong enzyme inhibition, but less than finasteride.

research The First Syntheses of 16β-Chloro- and 16β-Bromo-cyproterone Acetate

3 citations , January 2003 in “Synthetic Communications”

Scientists made two new chemicals that might help treat diseases caused by male hormones.

research BindingDB Entry 50021519: Discovery of (2S)-N-(6-Cyano-5-(trifluoromethyl)pyridin-3-yl)-3-(6-(4-cyanophenyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)-2-hydroxy-2-methylpropanamide as a Highly Potent and Selective Topical Androgen Receptor Antagonist for Androgenetic Alopecia Treatment.

January 2025

Highly Efficient Nucleophilic Addition of Alkyl Grignard Reagents to 17-Ketosteroids in the Presence of Cerium(III) Chloride: Synthesis of 17α-Propyl-17β-Hydroxy-4-Androsten-3-One, an Androgen Receptor Antagonist

research Highly efficient nucleophilic addition of alkyl Grignard reagents to 17-ketosteroids in the presence of cerium(III) chloride: Synthesis of 17α-propyl-17β-hydroxy-4-androsten-3-one, an androgen receptor antagonist

14 citations , February 1994 in “Tetrahedron Letters”

Adding cerium(III) chloride to Grignard reagents improves the making of compounds that could treat prostate issues and hair loss.

(1R,2S)-4-(2-Cyano-Cyclohexyl-Oxy)-2-Trifluoromethyl-Benzonitrile, A Potent Androgen Receptor Antagonist For Stimulating Hair Growth And Reducing Sebum Production

research (1R,2S)-4-(2-Cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production

14 citations , August 2007 in “Bioorganic & Medicinal Chemistry Letters”

The compound (1R,2S)-4-(2-Cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile can stimulate hair growth and reduce oil production when applied topically.

research An improved synthesis of finasteride from 4-androsten-3,17-dione

December 2010 in “Asian Journal of Research in Chemistry”

The new method makes finasteride cheaper and easier to produce.

Synthesis and In Vitro Study of 17β-[N-Ureylene-N,N′-Disubstituted]-4-Methyl-4-Aza-5α-Androstan-3-Ones as Selective Inhibitors of Type I 5α-Reductase

research Synthesis and in vitro study of 17β-[N-ureylene-N,N′-disubstituted]-4-methyl-4-aza-5α-androstan-3-ones as selective inhibitors of type I 5α-reductase

5 citations , February 1997 in “Bioorganic & Medicinal Chemistry”

New compounds were made that effectively block a specific enzyme related to androgen conditions.

research Cyclohex-1-ene Carboxylic Acids: Synthesis and Biological Evaluation of Novel Inhibitors of Human 5α Reductase

6 citations , March 2003 in “Archiv Der Pharmazie”

Scientists made new substances that can block an enzyme linked to prostate issues and hair loss, with potential for creating a new treatment.

research PHARMACOLOGICAL BASIS FOR CLINICAL USE OF ANTIANDROGENS

January 1983 in “Elsevier eBooks”

Cyproterone acetate is used to treat conditions like prostate cancer, early puberty, excessive sexual drive, and female androgenization by affecting androgen functions and suppressing certain hormones.

Crystal Structure and Synthesis of 3β-Benzoyloxy-4-pregnen-16α,17α-epoxy-6,20-dione

research Crystal Structure and Synthesis of 3.BETA.-Benzoyloxy-4-pregnen-16.ALPHA.,17.ALPHA.-epoxy-6,20-dione

January 2004 in “Analytical Sciences: X-ray Structure Analysis Online”

The document explains how to make a compound called 3.BETA.-Benzoyloxy-4-pregnen-16.ALPHA.,17.ALPHA.-epoxy-6,20-dione and describes its crystal structure.

research Effectiveness of Anastrozole and Cyproterone Acetate in Two Brothers with Familial Male Precocious Puberty

21 citations , January 2008 in “Journal of Pediatric Endocrinology and Metabolism”

research The synthesis of (−)-4-methyl-8-chloro-trans-1,2,3,4,4a,5,6,10b-octahydrobenzo-[f]-quinolin-3-one-[3-14C] (LY300502-14C]) via a circuitous route

3 citations , October 1994 in “Journal of Labelled Compounds and Radiopharmaceuticals”

Scientists made a carbon-14 labeled version of a drug with a 48% yield and over 99% purity.

research The antiandrogen cyproterone acetate: discovery, chemistry, basic pharmacology, clinical use and tool in basic research^*

88 citations , July 2009 in “Experimental and Clinical Endocrinology & Diabetes”

research Synthesis and biological evaluation of esters of 16-formyl-17-methoxy-dehydroepiandrosterone derivatives as inhibitors of 5α-reductase type 2

5 citations , November 2015 in “Journal of Enzyme Inhibition and Medicinal Chemistry”

Certain derivatives are more effective 5α-reductase type 2 inhibitors than finasteride.

research [Proliferation behavior of the anagen hair bulb in androgenetic alopecia before and after local administration of 17 alpha- propylmesterolone–DNA flow cytophotometry studies].

December 1990 in “PubMed”

Topical 17 alpha-propylmesterolone increases hair cell growth in androgenetic alopecia.

Natural Product-Inspired Bis(Trifluoromethyl) Phenyl Hydroxycinnamate Derivatives as Promising Nonsteroidal Inhibitors of Human Steroid 5α-Reductase Type-1: Synthesis, In Vitro, and In Silico Studies

research Natural Product-Inspired Bis(trifluoromethyl) Phenyl Hydroxycinnamate Derivatives as Promising Nonsteroidal Inhibitors of Human Steroid 5α-Reductase Type-1: Synthesis, In Vitro, and In Silico Studies

August 2025 in “ACS Omega”

New compounds show promise as nonsteroidal treatments for hair loss.

research Estranys matins de febrer: Pauline Fondevila

January 2006 in “Benzina: Revista d'excepcions culturals”

Trienones are more effective at inhibiting the enzyme linked to hair loss than dienones.

research New Synthesis of Finasteride

1 citations , January 2003 in “Chinese Journal of Pharmaceuticals”

A new method to make Finasteride is more cost-effective and yields 16%.

Probing Androgen Receptor Co-Factor Selectivity Profiles: A Chemical Tool to Determine Cross-Talk Between Androgen Receptor and Beta-Catenin In Vivo

research Probing androgen receptor co-factor selectivity profiles: a chemical tool to determine cross-talk between androgen receptor and β-catenin in vivo

1 citations , January 2013 in “MedChemComm”

PF-05314882 selectively activates androgen receptors without much effect on prostate and may help in prostate cancer treatment and hair loss prevention.

Synthesis of 11α-Hydroxyprogesterone Haptens

research Synthesis of 11α-hydroxyprogesterone hartens

7 citations , June 1989 in “Steroids”

Researchers successfully made new compounds for hormone level tests, but one attempt led to an unexpected product, correcting a past error.

research Effect of Carbamates on mRNA Encoding Lipid Enzymes in Hamster Flank Organs

1 citations , February 2014 in “Archiv Der Pharmazie”

Carbamates may help treat androgen-dependent conditions by changing how certain lipid enzymes are produced.

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