A series of novel hydantoins was designed and synthesized as structural alternatives to hydroxamate inhibitors of TACE. 5-Mono- and di-substituted hydantoins exhibited activity with IC50 values of 11-60 nM against porcine TACE in vitro and excellent selectivity against other MMPs.
Department of Urology, Guangzhou Women and Children's Medical Center, National Children's Medical Center for South Central Region, Guangzhou Medical University, Guangzhou, Guangdong, China.
Cancer cells acquire the ability to reprogram their phenotype in response to targeted therapies, yet the transition from dormancy to proliferation in drug-resistant cancers remains poorly understood. In prostate cancer, we utilized high-plasticity mouse models and enzalutamide-resistant (ENZ-R) cellular models to elucidate NR2F1 as a key factor in lineage transition and ENZ resistance. Depletion of NR2F1 drives ENZ-R cells into a relative dormancy state, characterized by reduced proliferation and heightened drug resistance, while NR2F1 overexpression yields contrasting outcomes.
Objective: We aimed to examine trends in novel antiandrogen receptor signal inhibitor (ARSI) usage and medical costs by collecting real-world big data included in The National Database of Health Insurance Claims and Specific Health Checkups of Japan (NDB) Open Data, covering most of the clinical practices throughout Japan.
Methods: Usage data for outpatient prescriptions from 2016 to 2021 were extracted from the NDB Open Data. Among the 459,610 million tablets/capsules prescribed, prostate cancer-specific agents (bicalutamide, estramustine phosphate, flutamide, abiraterone, enzalutamide, apalutamide, and darolutamide) were selected to investigate the trends of usage and medical costs.
The investigation focused on high-risk prostate cancer patients receiving neoadjuvant therapy before surgical procedures to assess clinical outcomes and factors influencing pathological responses.
76 patients were analyzed after receiving either androgen deprivation therapy with apalutamide or abiraterone, revealing significant differences in rates of pathological complete response and biochemical recurrence duration.
Results showed that the apalutamide group had higher rates of complete response (51.5% vs. 25.6%) and longer biochemical recurrence duration (261 days vs. 76 days), with lower post-treatment PSA levels being a key predictor of favorable outcomes.
Wound healing is a complex biological process crucial for tissue repair, especially in chronic wounds where healing is impaired. Liposomes have emerged as promising vehicles for delivering therapeutics to facilitate wound repair. Liposomes have been explored as effective carriers for therapeutic agents.
Laboratory for Chiral Technologies, Division of Organic Chemistry and Biochemistry, Ruđer Bošković Institute, Bijenička Cesta 54, 10000 Zagreb, Croatia.
Hydantoins, a class of five-membered heterocyclic compounds, exhibit diverse biological activities. The aim of this study was to synthesize and characterize a series of novel 3,5-disubstituted hydantoins and to investigate their antiproliferative activity against human cancer cell lines. The new hydantoin derivatives - were prepared as racemic mixtures of - and -isomers via a base-assisted intramolecular amidolysis of C-3 functionalized β-lactams.
