research Proteolysis‐targeting chimeras in cancer therapy: Targeted protein degradation for next‐generation treatment
PROTACs offer a new, precise way to treat cancer by breaking down harmful proteins.
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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 Enriching Proteolysis Targeting Chimeras with a Second Modality: When Two Are Better Than One
Adding a second method to PROTACs could improve cancer treatment.
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
The new compound is a promising, less toxic alternative to finasteride for treating prostate issues.
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.
![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.
research Nano-PROTACs: state of the art and perspectives
Nano-PROTACs could improve drug targeting and delivery by using nanotechnology.
research Thiohydrazides in the Synthesis of Functionalized Extranuclear Heterosteroids
New steroid derivatives show promise as anticancer agents, even against resistant cells.
![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 Synthesis of N-Substituted 3-Oxo-17b- carboxamide-4-aza-5a-androstanes and the Tautomerism of 3-Oxo-4-aza-5-androstenes
Researchers made two new compounds that could be used for medicine.
research Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors
3-tetrazolo steroidal analogs can strongly inhibit the enzyme linked to hair loss.
research PROTACs in cancer therapy: targeted degradation of GPX4, PARP and epigenetic regulators
PROTACs show promise in cancer treatment by effectively degrading specific harmful proteins.
research Activity of steroid 4 and derivatives 4a–4f as inhibitors of the enzyme 5α-reductase 1
Compounds 4, 4b, and 4c effectively inhibit an enzyme linked to testosterone conversion without significant toxicity.
research Selective Delivery of Tofacitinib Citrate to Hair Follicles Using Lipid-Coated Calcium Carbonate Nanocarrier Controls Chemotherapy-Induced Alopecia Areata
A new treatment using nanoparticles can effectively prevent and reduce hair loss caused by chemotherapy.
research Peptide-Based PROTACs: Transitioning from Static Paradigm to a Dynamic Landscape within Targeted Protein Degradation
Peptide-based PROTACs show promise in targeting hard-to-treat proteins, especially for cancer therapy.
research Pharmacological Profile of 9,11-Dehydrocortexolone 17α-Butyrate (CB-03-04), a New Androgen Antagonist with Antigonadotropic Activity
CB-03-04 shows promise as a treatment for prostate issues due to its strong anti-androgen effects.
![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](/images/research/d19df8a7-8de6-4430-8a0d-4ffa1f502985/small/15608.jpg)
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
New compounds were made that effectively block a specific enzyme related to androgen conditions.
research N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase
Scientists found new, better-working inhibitors for a hormone-related enzyme.
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.
research In vivo evaluation of the efficacy, toxicity and biodistribution of PLGA-DMSA nanoparticles loaded with itraconazole for treatment of paracoccidioidomycosis
Itraconazole-loaded nanoparticles are more effective and less toxic for treating fungal infections than conventional oral itraconazole.
research In‐silico Screening of ATP‐competitive Inhibitory Activities of Phytochemicals against Janus Kinase 3 and Its In‐vitro Evaluation
Poncirin is a promising inhibitor of Janus Kinase 3, potentially better than tofacitinib.
research Synthesis and structure–activity studies of side-chain derivatized arylhydantoins for investigation as androgen receptor radioligands
The nature of the side chain in RU 58841 derivatives greatly affects its AR affinity, with the N-(iodopropenyl) derivative 13 showing the highest AR binding affinity, suggesting its potential for developing high-affinity radioiodinated AR radioligands.
research 3,3-Diphenylpentane skeleton as a steroid skeleton substitute: Novel inhibitors of human 5α-reductase 1
A new compound effectively inhibits human 5α-reductase 1.
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 Preclinical Pharmacology, Antitumor Activity, and Development of Pharmacodynamic Markers for the Novel, Potent AKT Inhibitor CCT128930
CCT128930 is a promising new drug that effectively targets and inhibits a cancer-related protein, showing potential for cancer treatment.
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 Steroid 5α-Reductase Inhibitors
New steroidal compounds could be effective for treating conditions related to 5α-reductase enzyme activity.
research Dual inhibitors of urease and carbonic anhydrase-II from Iris species
Some natural compounds from Iris plants can block enzymes related to certain disorders, with a few affecting both targeted enzymes.
![Synthesis, Biological Evaluation, and Molecular Docking of 4-Amino-2H-benzo[h]chromen-2-one Analogs Containing the Piperazine Moiety](/images/research/2ecf4eed-7dbe-4f1a-83db-739625546cdd/small/31808.jpg)
research Synthesis, biological evaluation and molecular docking of 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs containing the piperazine moiety
Analog 23 is a promising compound for prostate cancer treatment.
research Rapid Characterization of the Functional and Pharmacological Consequences of Cantú Syndrome KATPChannel Mutations in Intact Cells
Kir6.1 mutations in Cantú syndrome increase channel sensitivity and hyperpolarization, while SUR2B mutations do not.