111 citations
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August 2002 in “Journal of Medicinal Chemistry” This study reports that 2-(1-Adamantyl)-4H-thiochromen-4-on-6-O-sulfamate is the most potent steroid sulfatase inhibitor identified so far, exhibiting 170-fold higher activity than the lead compound estrone sulfamate.
27 citations
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July 2008 in “The Journal of Steroid Biochemistry and Molecular Biology” The new compounds may be more effective and cheaper than current treatments for conditions like baldness.
27 citations
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September 1994 in “The journal of investigative dermatology/Journal of investigative dermatology” This study found that relatively low concentrations of 1,25(OH)2D3 stimulated human hair follicle and fiber growth, while higher concentrations inhibited growth in a whole-organ culture system.
27 citations
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October 2001 in “Journal of Medicinal Chemistry” This study identified eight isoflavone derivatives as potential nonsteroidal inhibitors of rat 5α-reductase using a pharmacophore model in virtual screening.
20 citations
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January 2003 in “Chemical and Pharmaceutical Bulletin” This study reports that five new progesterone derivatives demonstrated inhibitory activity against the 5α-reductase enzyme and binding affinity for the androgen receptor in an in vitro hamster model.
20 citations
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February 2002 in “Expert Opinion on Therapeutic Patents” This review discusses the potential uses of 5α-reductase inhibitors for conditions ranging from benign prostatic hyperplasia to skin disorders like acne and male pattern baldness, but it reports no new clinical results.
19 citations
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March 2010 in “Steroids” This study found that specific steroids, particularly 5 and 7b, decreased growth of prostate and seminal vesicles and bound to the androgen receptor, showing comparable pharmacological activity to finasteride.
18 citations
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October 2010 in “Bioorganic & Medicinal Chemistry Letters” This study found that a new hybrid compound designed from finasteride and epristeride was a potent inhibitor of 5α-reductase with a mechanism similar to finasteride.
18 citations
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December 2005 in “Journal of Medicinal Chemistry” In this study, novel substituted benzoyl benzoic acids and phenylacetic acids were potent and selective inhibitors of human steroid 5alpha-reductase type 2, with one compound showing promising bioavailability in rats for potential clinical evaluation.
17 citations
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June 2012 in “European journal of medicinal chemistry” This study found that compounds 21–23 and 25 exhibited strong 5α-reductase II inhibition in vitro and significantly reduced rat prostate weight, performing comparably to finasteride.
17 citations
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December 2004 in “Bioorganic & Medicinal Chemistry Letters” This study identified N-acyl arylsulfonamides, particularly N-(Boc-piperidine-4-carbonyl)-benzenesulfonamides, as steroid sulfatase inhibitors with improved cellular potency compared to previous compounds.
17 citations
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June 1996 in “The Journal of Steroid Biochemistry and Molecular Biology” In this study, FCE 28260 showed greater potency than finasteride in inhibiting 5α-reductase enzymes and reducing prostate DHT levels in rats.
16 citations
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September 2018 in “Journal of Molecular Liquids” This study investigated a nanostructured system using PS-b-PAA diblock copolymer for incorporating the hydrophobic photosensitizer ClAlPc, finding it effective in causing cellular damage in Caco-2 cells under light while demonstrating no cytotoxicity without light, suggesting its potential use in photodynamic therapy.
13 citations
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January 2005 in “Chemical and Pharmaceutical Bulletin” This study reported that newly synthesized progesterone derivatives significantly reduced prostate weight in testosterone-treated hamsters, with 5alpha-reductase inhibitory activity dependent on the size of the substituent at C-17.
13 citations
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August 2007 in “Bioorganic & medicinal chemistry letters” This study developed a new competitive 5alpha-reductase inhibitor with an IC(50) of 0.84 microM using a novel chemical structure.
11 citations
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May 2010 in “Journal of Medicinal Chemistry” This study introduced a novel nonsteroidal androgen receptor antagonist that effectively controls sebum production in the golden Syrian hamster ear model through targeted follicular delivery.
8 citations
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July 2019 in “Pure and Applied Chemistry” This study identified natural compounds from Iris plants that showed potential as inhibitors of urease and carbonic anhydrase-II enzymes, suggesting their possible use in treating related disorders.
5 citations
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January 2018 This study optimized a screening assay to identify molecules that inhibit or enhance TRPM5 ion channel activity, which may have implications for treating dysfunctions linked to cardiac arrhythmias and diabetes.
4 citations
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August 2010 in “Acta Biologica Hungarica” This study found that novel compounds moderately inhibited 5α-reductase type 1 activity compared to finasteride, offering valuable data on structure-activity relationships.
2 citations
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September 2022 in “Cellular and molecular biology” In this study, Agaricus bisporus derived β-Glucan particles demonstrated antimicrobial, antioxidant, and anticancer effects against cervical cancer HeLa cells, suggesting potential as a therapeutic option.
1 citations
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December 2022 in “International Journal of Science for Global Sustainability” This study found that Mitracarpus hirtus extracts showed potential antifungal activity against Tinea capitis in vitro, with ethylacetate extracts demonstrating the highest inhibitory effects.
In this study, exposure to high concentrations of all-trans retinoic acid caused apoptotic cell death in mouse hair follicle stem cells, suggesting its potential for removing unwanted hair.
In this study, the researchers reported that the optimized compound 39 demonstrated potent AR antagonism and favorable pharmacokinetics in a hair-growth mouse model, achieving similar efficacy to pyrilutamide with faster onset and preserved safety, offering promise for next-generation topical AR antagonist development.
This study found that the optimized topical AR antagonist 39, derived from 14-P1, demonstrated potent AR antagonism and comparable efficacy to pyrilutamide in a hair-growth mouse model, with a faster onset and favorable safety profile.
In this study, researchers optimized the soft drug AR antagonist 14-P1 to create candidate 39, which demonstrated effective AR antagonism and safety in a hair-growth mouse model, showing similar efficacy to pyrilutamide but with quicker onset and a lower risk of systemic toxicity.
In a hair-growth mouse model, this study reported that the novel AR antagonist candidate 39, derived from structural optimization of 14-P1, achieved similar efficacy to pyrilutamide with faster response and maintained safety, demonstrating potent AR antagonism and favorable pharmacokinetics with lower systemic toxicity risk.
This study found that the optimized AR antagonist compound 39 showed potent hair growth activity with improved safety in mice, suggesting potential for better topical treatments for androgenetic alopecia.
In a mouse hair-growth model, this study found that the optimized compound 39 matched the efficacy of pyrilutamide for androgenic alopecia, with faster response and maintained safety, suggesting it as a promising topical AR antagonist with reduced systemic toxicity risk.
In this study, a dual soft drug design strategy improved the AR antagonist candidate 39, showing potent AR antagonism and good safety in a mouse hair-growth model, with similar efficacy to pyrilutamide but faster response.
This study found that the optimized AR antagonist candidate 39, in a hair-growth mouse model, achieved similar efficacy to pyrilutamide with faster onset and favorable safety, suggesting a promising approach for developing topical treatments with low systemic toxicity for androgenetic alopecia.