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research Novel synthesis of nicotinamide derivatives of cytotoxic properties
This study screened synthesized pyridinecarboxamides for antitumor properties and found that many, particularly 5c and 7a, showed moderate in vitro activity against various human tumor cell lines.
research Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production
This study found that a specific amino-pyridine compound showed potent androgen receptor antagonist activity, stimulating hair growth in mice and reducing sebum production in a hamster model.
research Selective Sensing of Darolutamide and Thalidomide in Pharmaceutical Preparations and in Spiked Biofluids
This study introduced a new spectrofluorometric method using a synthesized organic fluorophore to effectively analyze darolutamide and thalidomide in pharmaceutical preparations and biofluids.
research 5α-Reductase inhibitors, antiviral and anti-tumor activities of some steroidal cyanopyridinone derivatives
This study found that some synthesized heterocyclic derivatives showed promising 5α-reductase inhibitor, antiviral, and anti-tumor activities, surpassing several reference drugs in effectiveness.
research Advancing mitochondrial therapeutics: Synthesis and pharmacological evaluation of pyrazole-based inhibitors targeting the mitochondrial pyruvate carrier
This study reported the development of new pyrazole-based MPC inhibitors that effectively inhibit mitochondrial pyruvate transport, showing potential as therapeutic candidates for conditions like metabolic dysfunction-associated steatohepatitis without activating PPARγ.
research Novel Dual Soft Drug Strategy Enables Development of Topical Androgen Receptor Antagonists with Enhanced Efficacy and Optimized Safety for Androgenetic Alopecia
In this study, candidate compound 39 demonstrated potent androgen receptor antagonism and faster hair-growth efficacy in a mouse model compared to pyrilutamide, while maintaining favorable safety and pharmacokinetic profiles, suggesting potential for topical use in androgenic alopecia.
research N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase
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.
research Synthesis and anticancer activity evaluation of Novel 6 mercaptopurine derivatives.
This study synthesized and evaluated five 6-mercaptopurine derivatives for anticancer activity against three cancer cell lines, detailing the promising results of compound 1.
research Development of Novel Mitochondrial Pyruvate Carrier Inhibitors to Treat Hair Loss
This study found that novel MPC inhibitor analogues with specific chemical modifications promoted significant hair growth in shaved mice when applied topically.
research Palladium nanoparticles on a pyridinium supported ionic liquid phase: a recyclable and low-leaching palladium catalyst for aminocarbonylation reactions
In this study, researchers developed a new Supported Ionic Liquid Phase palladium catalyst that showed effectiveness in aminocarbonylation reactions for synthesizing pharmaceutical compounds like CX-546 and a precursor of Finasteride, though results were sensitive to substrate variations and prompted palladium leaching concerns.
research Design and synthesis of novel Azasteroids and Pseudoazulenyl nitrones
This review explores the synthesis and potential of azasteroids as novel drugs, discussing challenges in their production and reporting no new clinical results.
research Synthesis and Evaluation of 2‘-Substituted 4-(4‘-Carboxy- or 4‘-carboxymethylbenzylidene)-N-acylpiperidines: Highly Potent and in Vivo Active Steroid 5α-Reductase Type 2 Inhibitors
This study found that several synthesized compounds were potent inhibitors of human steroid 5alpha-reductase type 2 and reduced prostate weights in treated rats, with compound 15 showing promise for potency in humans.
research 576 INTASYL PH-762: Intratumoral immunotherapy targeting PD-1
PH-762 shows promise in treating skin cancer by effectively targeting and silencing PD-1 in tumors with minimal side effects.
research Synthesis and structure–activity investigation of iodinated arylhydantoins and arylthiohydantoins for development as androgen receptor radioligands
This study found that arylhydantoin and arylthiohydantoin derivatives with hydroxybutyl or methyl side-chains showed superior androgen receptor binding affinity and may serve as promising radioiodinated AR ligands.
research Novel DualSoftDrug Strategy Enables Developmentof Topical Androgen Receptor Antagonists with Enhanced Efficacy andOptimized Safety for Androgenetic Alopecia
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.
research Bicalutamide
research Experimental Assessment of 3-meta-Pyridine-1,2,4-Oxadiazole Deoxycholic Acid Derivative as a Prototype of 5-α-Reductase Inhibitors in silico and in vivo Models
This study found that a new deoxycholic acid derivative may offer a similar prostatoprotective effect to finasteride with lower toxicity in rat models.
research Design, Synthesis, and Evaluation of Aryl Hydantoins and Ureas as Antischistosomal Agents
This study identified AH01 derivatives and related compounds with high antischistosomal efficacy and reduced antiandrogenic effects, suggesting potential new directions for schistosomiasis drug development.
research Novel DualSoftDrug Strategy Enables Developmentof Topical Androgen Receptor Antagonists with Enhanced Efficacy andOptimized Safety for Androgenetic Alopecia
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.
research Synthesis and structure–activity studies of side-chain derivatized arylhydantoins for investigation as androgen receptor radioligands
This study identified the N-(iodopropenyl) derivative 13 as a promising candidate for development as a radioiodinated androgen receptor ligand due to its binding affinity.
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
This study suggests that PF-0998425 is an effective androgen receptor antagonist for sebum control and androgenetic alopecia with rapid metabolism reducing the risk of systemic side effects.
research Proxalutamide Significantly Accelerates Viral Clearance and Reduces Time to Clinical Remission in Patients with Mild to Moderate COVID-19: Results from a Randomized, Double-Blinded, Placebo-Controlled Trial
In this study, Proxalutamide significantly increased the rate of viral clearance and reduced clinical remission time in patients with mild to moderate COVID-19 compared to placebo.
research Proxalutamide (GT0918) Reduces the Rate of Hospitalization in mild-to-moderate COVID-19 Female Patients: A Randomized Double-Blinded Placebo-Controlled Two-Arm Parallel Trial
This study found that proxalutamide treatment significantly reduced 30-day hospitalization rates in women with mild-to-moderate COVID-19 compared to placebo, with no safety issues identified.
research Synthesis and Structure–Activity Relationships of the First Ferrocenyl-Aryl-Hydantoin Derivatives of the Nonsteroidal Antiandrogen Nilutamide
Scientists made the first metal-based compounds from a nonsteroidal antiandrogen drug, which showed potential in fighting both hormone-dependent and independent prostate cancer cells.
research Novel DualSoftDrug Strategy Enables Developmentof Topical Androgen Receptor Antagonists with Enhanced Efficacy andOptimized Safety 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.
research A Transition State Analogue of 5′-Methylthioadenosine Phosphorylase Induces Apoptosis in Head and Neck Cancers
This study found that the combination of MT-DADMe-ImmA and MTA selectively induced apoptosis in head and neck squamous cell carcinoma cell lines FaDu and Cal27, but not in normal fibroblasts or MTAP-deficient breast cancer cells.
research Tuning Scaffold Properties of New 1,4-Substituted Pyrrolo[3,2-c]quinoline Derivatives Endowed with Anticancer Potential, New Biological and In Silico Insights
In this study, the synthesis and testing of new pyrroloquinoline derivatives identified compound 7p, which showed low micromolar cytotoxic activity against MCF-7 and HeLa cells, highlighting its potential for development into a potent anticancer agent.
research Analysis of metabolic characteristics of epristeride in zebrafish based on LC-Q-TOF MS and its potential applications in doping control
This study used a zebrafish model and advanced mass spectrometry to identify 11 metabolites of epristeride, revealing significant effects on purine metabolism and aromatic amino acid biosynthesis, which may aid in developing anti-doping detection methods.
research Neoadjuvant therapy with Disitamab vedotin in treating muscle-invasive bladder cancer: A case report
In this study, a 68-year-old man with muscle-invasive bladder cancer and renal insufficiency achieved a partial radiological response to neoadjuvant therapy with gemcitabine and Disitamab Vedotin, without significant adverse events, highlighting a potential alternative for cisplatin-ineligible patients.