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research Natural Product-InspiredBis(trifluoromethyl) PhenylHydroxycinnamate Derivatives as Promising Nonsteroidal Inhibitorsof Human Steroid 5α-Reductase Type-1: Synthesis, InVitro, and In Silico Studies

August 2025 in “OPAL (Open@LaTrobe) (La Trobe University)”

Certain hydroxycinnamate derivatives may effectively inhibit enzymes linked to hair loss with low toxicity.

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

research 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

December 2023 in “Journal of Medicinal Chemistry”

A new topical treatment for hair loss shows strong hair growth effects with low toxicity.

research Four-amino acid segment in steroid 5 alpha-reductase 1 confers sensitivity to finasteride, a competitive inhibitor.

83 citations , April 1992 in “Journal of Biological Chemistry”

Four-amino acid part makes enzyme sensitive to finasteride.

research Treatment of Tourette’s Syndrome With Finasteride

42 citations , December 2007 in “American Journal of Psychiatry”

Finasteride may effectively reduce Tourette's syndrome symptoms and improve life quality.

research 5α-reduced progestogens ameliorate mood-related behavioral pathology, neurotoxicity, and microgliosis associated with exposure to HIV-1 Tat

47 citations , January 2016 in “Brain Behavior and Immunity”

5α-reduced progestogens may reduce mood issues and brain damage linked to HIV-1 Tat.

research The Neurosteroidogenic Enzyme 5α-Reductase Mediates Psychotic-Like Complications of Sleep Deprivation

27 citations , January 2017 in “Neuropsychopharmacology”

The enzyme 5α-reductase is key in causing psychotic-like effects from sleep deprivation.

research PRMT5 inhibition has a potent anti-tumor activity against adenoid cystic carcinoma of salivary glands

7 citations , January 2025 in “Journal of Experimental & Clinical Cancer Research”

PRMT5 inhibitors effectively fight adenoid cystic carcinoma in salivary glands.

research Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors

17 citations , December 2015 in “Bioorganic & Medicinal Chemistry”

3-tetrazolo steroidal analogs can strongly inhibit the enzyme linked to hair loss.

research 5α-Reductases In Human Physiology: an Unfolding Story

44 citations , July 2012 in “Endocrine Practice”

We need to learn more about 5α-reductases and neuroactive steroids to safely make drugs targeting these enzymes.

research Synthesis of avicequinone c and analogs toward the study of 5α-reductase inhibitory activity

January 2015

2-Hydroxy-1,4-naphthoquinone is a strong 5α-reductase inhibitor.

Synthesis, Biological Evaluation, and Molecular Docking of 4-Amino-2H-benzo[h]chromen-2-one Analogs Containing the Piperazine Moiety

research Synthesis, biological evaluation and molecular docking of 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs containing the piperazine moiety

7 citations , August 2019 in “Bioorganic & medicinal chemistry”

Analog 23 is a promising compound for prostate cancer treatment.

research Inhibition of 17α-hydroxylase/C17,20 lyase reduces gating deficits consequent to dopaminergic activation

19 citations , September 2013 in “Psychoneuroendocrinology”

Blocking CYP17A1 enzyme may help improve certain brain function issues related to dopamine.

5α-Reductase Inhibition Prevents the Luteal Phase Increase in Plasma Allopregnanolone Levels and Mitigates Symptoms in Women with Premenstrual Dysphoric Disorder

research 5α-Reductase Inhibition Prevents the Luteal Phase Increase in Plasma Allopregnanolone Levels and Mitigates Symptoms in Women with Premenstrual Dysphoric Disorder

110 citations , August 2015 in “Neuropsychopharmacology”

High-dose dutasteride reduces PMDD symptoms by stabilizing neurosteroid levels.

Blockade of Androgen Markers Using a Novel Betasitosterol, Thioctic Acid, and Carnitine-Containing Compound in Prostate and Hair Follicle Cell-Based Assays

research Blockade of Androgen Markers Using a Novel Betasitosterol, Thioctic Acid and Carnitine-containing Compound in Prostate and Hair Follicle Cell-based Assays

3 citations , March 2016 in “Phytotherapy Research”

The new compound was more effective than finasteride in reducing markers of hair loss and prostate issues in cell tests.

Pharmacokinetic Parameters and Mechanisms of Inhibition of Rat Type 1 and 2 Steroid 5α-Reductases: Determinants for Different In Vivo Activities of GI198745 and Finasteride in the Rat

research Pharmacokinetic parameters and mechanisms of inhibition of rat type 1 and 2 steroid 5α-reductases: determinants for different in vivo activities of GI198745 and finasteride in the rat 3 3Abbreviations: r5AR1, rat 5α-reductase 1; r5AR2, rat 5α-reductase 2; and DHT, dihydrotestosterone.

22 citations , October 2001 in “Biochemical Pharmacology”

GI198745 is more potent and longer-lasting than finasteride, potentially better for treating hair loss.

research Introduction: splintering urbanism

January 2007 in “Edward Elgar eBooks”

TSPO might help treat anxiety and depression.

research The Bis(1,2,3,4-tetrahydroisoquinoline) Alkaloids Cepharanthine and Berbamine Are Ligands of SK Channels

6 citations , January 2024 in “ACS Medicinal Chemistry Letters”

Cepharanthine and berbamine may affect SK channels, influencing their therapeutic effects.

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

research Advancing mitochondrial therapeutics: Synthesis and pharmacological evaluation of pyrazole-based inhibitors targeting the mitochondrial pyruvate carrier

4 citations , December 2024 in “European Journal of Medicinal Chemistry”

New pyrazole-based inhibitors show promise for treating metabolic diseases and other conditions.

research Evaluation of Therapeutic Potential of a Selective 5α-reductase Inhibitor against Glioblastoma: Molecular Docking and In Vitro Insights

1 citations , June 2025 in “Cell Biochemistry and Biophysics”

research 11β-Hydroxylase inhibitors protect against seizures in mice by increasing endogenous neurosteroid synthesis

18 citations , April 2011 in “Neuropharmacology”

11β-Hydroxylase inhibitors help prevent seizures in mice by boosting natural neurosteroid production.

5α-Reductase Inhibitors: Progress and Therapeutic Potential

research 5α-reductase inhibitors

5 citations , January 2001 in “Advances in protein chemistry”

5α-reductase inhibitors help treat disorders caused by DHT and have potential for future therapies.

research Allopregnanolone mediates the exacerbation of Tourette-like responses by acute stress in mouse models

25 citations , June 2017 in “Scientific reports”

Stress worsens Tourette symptoms by increasing allopregnanolone levels.

research Preparation, Characterization and Molecular Docking Study of some New Pyrazole Derivatives Derived from 2-Mercaptobenzothiazole.

June 2025 in “Mağallaẗ ʻulūm al-rāfidayn”

New pyrazole derivatives may help treat hair loss, but more testing is needed.

research Rational Design and Synthesis of 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a Novel, Nonsteroidal Androgen Receptor Antagonist Devoid of Phototoxicity for Dermatological Indications

23 citations , October 2008 in “Journal of medicinal chemistry”

PF-998425 is a new, effective, and non-phototoxic treatment for skin conditions related to androgens.

In Vitro and In Vivo Effects of 17β-N-(4-Phenylcarbamoyl) Androst-4-en-3-one Derivatives as 5α-Reductase Inhibitors on Androgen-Dependent Glands

research In vitro and In vivo Effects of 17β-N-(4-phenylcarbamoyl) androst-4-en-3- one Derivatives as 5a-reductase Inhibitors on Androgen-dependent Glands

September 2020 in “Current Enzyme Inhibition”

Three compounds were found to inhibit a prostate disease-related enzyme and reduce prostate size more effectively than the current treatment, suggesting they could be used for treating benign prostatic hyperplasia.

research Synthesis and Study of Some 17a-aza-D-homo Steroids as 5α-Reductase Inhibitors

1 citations , October 2020 in “Current Drug Discovery Technologies”

The research found that compound 6, a newly created steroid, is more effective at inhibiting 5α-reductase (an enzyme) than current treatments, suggesting it could be a better option for treating urinary tract symptoms in men.

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 PD23-01 INHIBITOR OF 5A-REDUCTASE TYPES II PROMOTES THE INFILTRATION OF CD8+T CELLS IN BPH TISSUES.

March 2014 in “The Journal of Urology”

Finasteride increases CD8+ T cells in BPH tissues.

research Effect of the 5α-reductase enzyme inhibitor dutasteride in the brain of intact and parkinsonian mice

16 citations , October 2017 in “Journal of steroid biochemistry and molecular biology/The Journal of steroid biochemistry and molecular biology”

Dutasteride may protect the brain in early Parkinson's disease.

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