research Thiohydrazides in the Synthesis of Functionalized Extranuclear Heterosteroids
New steroid derivatives show promise as anticancer agents, even against resistant cells.
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240-270 / 1000+ resultsresearch Estranys matins de febrer: Pauline Fondevila
Trienones are more effective at inhibiting the enzyme linked to hair loss than dienones.
![Benzo[c]quinolizin-3-ones: A Novel Class of Potent and Selective Nonsteroidal Inhibitors of Human Steroid 5α-Reductase 1](/images/research/ff6e6cbe-cb9c-4d11-87ef-671d28ffd4fa/small/15506.jpg)
research Benzo[c]quinolizin-3-ones: A Novel Class of Potent and Selective Nonsteroidal Inhibitors of Human Steroid 5α-Reductase 1
Benzo[c]quinolizin-3-ones are effective nonsteroidal inhibitors of human steroid 5α-reductase 1.
![Verification of the Major Metabolic Oxidation Path for the Naphthoyl Group in Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells (CRTh2) Antagonist 2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic Acid (Setipiprant/ACT-129968)](/images/research/d743d32f-3115-48ff-9697-2f2d56130701/small/14175.jpg)
research Verification of the Major Metabolic Oxidation Path for the Naphthoyl Group in Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells (CRTh2) Antagonist 2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic Acid (Setipiprant/ACT-129968)
The document confirms the structures of major metabolites of the CRTh2 antagonist Setipiprant and identifies minor metabolites.
research Ultrasound-Assisted Facile Synthesis and Anticancer Evaluation of Novel N-(2-substituted phenyl-4-oxathiazolidine-3-carbonothioyl) benzamide
Researchers made new compounds that could potentially be developed into anticancer drugs.
research Synthetic Approaches for Pharmacologically Active Decorated Six-Membered Diazines
The document concludes that specific methods for making diazine-based drugs can lead to high yields and are important for creating effective treatments for various diseases.
research Synthesis and anticancer activity of phenylpropanoid sucrose esters
Phenylpropanoid sucrose esters show potential as anticancer agents.
research Synthesis and anticancer activity evaluation of Novel 6 mercaptopurine derivatives.
Compound 1 showed promising anticancer activity.
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
Three specific 4-azasteroid-2-oximes showed strong enzyme inhibition, but less than finasteride.
research Breaking the “rule-of-five” to access Bridged Bicyclic Heteroaromatic Bioisosteres
A new method creates valuable compounds for drug discovery by breaking traditional chemical rules.
research Synthesis, Anticancer and Molecular Docking Studies of 2-(4-chlorophenyl)-5-aryl-1,3,4-Oxadiazole Analogues
The compound 4c showed strong potential as an anticancer agent.
research Thiazole: A Versatile Standalone Moiety Contributing to the Development of Various Drugs and Biologically Active Agents
Thiazole, a sulfur and nitrogen chemical, is useful in creating potential drugs for conditions like seizures, cancer, bacterial infections, tuberculosis, inflammation, malaria, viruses, Alzheimer's, diabetes, and A1-receptor issues.
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.
![Synthesis and 5α-Reductase Inhibitory Activity of 8-Substituted Benzo[ƒ]Quinolinones Derived from Palladium Mediated Coupling Reactions](/images/research/2aedba8c-b0ac-4fa3-9ac7-9f375a016bba/small/15581.jpg)
research Synthesis and 5α-reductase inhibitory activity of 8-substituted benzo[ƒ]quinolinones derived from palladium mediated coupling reactions
Some newly made compounds can block an enzyme linked to hair loss and prostate growth, with one in particular being very selective.
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
PF-998425 is a new, effective, and non-phototoxic treatment for skin conditions related to androgens.
research Towards sustainable and scalable synthesis of amitriptyline hydrochloride, minoxidil, and pyrrolidinyl diaminopyrimidine oxide
research Atroposelective Synthesis of Biaryl N‐Oxides via Cu‐Catalyzed De Novo Heteroaromatic N‐Oxide Ring Formation
A new method efficiently creates biaryl N-oxides with potential for cancer treatment and drug development.
research Novel 5α-Reductase Inhibitors: Synthesis, Structure−Activity Studies, and Pharmacokinetic Profile of Phenoxybenzoylphenyl Acetic Acids
A brominated phenoxy compound effectively inhibits a human enzyme and shows potential for clinical use.
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
Compounds 15, 20, and 25 are strong inhibitors of human steroid 5α-reductase type 2.
research Crystal Structure of 17-.BETA.-Benzoyloxy-16-.BETA.-methylpregna-4,6-diene-3,20-dione.
A new antiandrogen compound was made and its detailed three-dimensional shape was described.
research Structure optimization of tetrahydropyridoindole-based aldose reductase inhibitors improved their efficacy and selectivity
Optimizing the structure of a specific compound greatly improved its effectiveness and precision for treating diabetic complications.
research Design, synthesis and anti-tumor evaluation of novel thiohydantoin congeners as androgen receptor antagonists with in vivo study.
A new compound, 3a, effectively fights prostate cancer better than finasteride.
research Modulation of the 6-position of benzopyran derivatives and inhibitory effects on the insulin releasing process
Changing the 6-position on benzopyran molecules affects insulin release, with some compounds showing strong inhibitory effects.
![Patent Evaluation: Hexahydrobenzo[f]quinolines as 5α-Reductase Inhibitors](/images/research/1634373b-f615-46c7-a157-21394e3366be/small/21095.jpg)
research Patent Evaluation: Hexahydrobenzo[f]quinolines as 5α-reductase inhibitors
Hexahydrobenzo[f]quinolines are effective at blocking the enzyme 5α-reductase.
![Benzo[c]quinolizin-3-ones Theoretical Investigation: SAR Analysis and Application to Untested Compounds](/images/research/6712367a-949f-47c7-a756-2bfe6316fc69/small/15331.jpg)
research Benzo[c]quinolizin-3-ones Theoretical Investigation: SAR Analysis and Application to Nontested Compounds
The research found a link between certain molecular features and the biological activity of BC3, which can help identify or create new active compounds.
![Synthesis and Activity of 8-Substituted Benzo[c]quinolizin-3-ones as Dual Inhibitors of Human 5α-Reductases 1 and 2](/images/research/efc54340-66d6-4f27-9930-045ac023f903/small/15248.jpg)
research Synthesis and activity of 8-substituted benzo[c]quinolizin-3-ones as dual inhibitors of human 5α-reductases 1 and 2
New compounds were made that effectively block enzymes related to prostate issues and hair loss.
research Design and synthesis of novel androgen receptor antagonists with sterically bulky icosahedral carboranes
New compounds with carborane showed anti-androgen effects similar to flutamide.
research Estudio de la reactividad de los anillos A y C de olean-12-enos naturales para la obtención de sintones quirales
The study found ways to create important compounds for male health from olive waste.
![Synthesis of Spiro[cyclohexane-1,2'-[2H]indene] Derivatives as Inhibitors of Steroid 5α-Reductase](/images/research/d91300a7-4d66-4d2c-90ac-293b0dbc5ff5/small/21048.jpg)
research Synthesis of Spiro[cyclohexane-1,2?-[2H]indene] derivatives as inhibitors of steroid 5?-reductase
Compound 15a was effective in inhibiting 5α-reductase.
research Synthesis of Analogues of Cercidin, an Antimicrobial Compound of Cercidiphyllum japonicum : Glycosylation of Methyl Gallate with Ulosyl Bromides
Researchers created 10 new compounds similar to cercidin, which could lead to new antibiotics.