Hydantoins are an important class of heterocycles with applications in pharmacy, agriculture, and as intermediates in organic synthesis. Traditional synthetic procedures to access hydantoins are target oriented with multiple synthetic steps and often use reagents that are not commercially available or sustainable. Herein, an efficient process is described for accessing hydantoins starting from commercially available amines using consecutive gas-liquid transformations (oxygen, carbon dioxide). This semi-continuous process produced ten benzylic/aliphatic hydantoins in good overall yields (52-84 %).
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http://dx.doi.org/10.1002/chem.201602609 | DOI Listing |
J Transl Med
January 2025
Cancer Institute, Xuzhou Medical University, 209 Tongshan Road, Xuzhou, 221004, Jiangsu, China.
Background: The sustained activation of androgen receptor splice variant-7 (AR-V7) is a key factor in the resistance of castration-resistant prostate cancer (CRPC) to second-generation anti-androgens such as enzalutamide (ENZ). The AR/AR-V7 protein is regulated by the E3 ubiquitin ligase STUB1 and a complex involving HSP70, but the precise mechanism remains unclear.
Methods: High-throughput RNA sequencing was used to identify differentially expressed circular RNAs (circRNAs) in ENZ-resistant and control CRPC cells.
Commun Biol
January 2025
Division of Biological Science, Graduate School of Science and Technology, Nara Institute of Science and Technology (NAIST), Ikoma, Japan.
Monocarpic plants flower only once and then produce seeds. Many monocarpic plants require a cold treatment known as vernalization before they flower. This requirement delays flowering until the plant senses warm temperatures in the spring.
View Article and Find Full Text PDFNihon Hinyokika Gakkai Zasshi
January 2025
Department of Urology, Osaka Medical and Pharmaceutical University Faculty of Medicine.
A 70-years-old man with metastatic hormone-sensitive prostate cancer received the apalutamide, an oral androgen receptor signaling inhibitor. On day10 after drug initiation, fever and skin rash appeared on his whole-body surface. He stopped taking the drug on day18 and skin symptoms temporarily improved about 7 days after discontinuation.
View Article and Find Full Text PDFMini Rev Med Chem
January 2025
Drug Discovery and Research Laboratory, Department of Pharmacy, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India.
Hydantoin, a five-membered heterocyclic scaffold, is regarded as a crucial scaffold in medicinal chemistry. Hydantoins have been useful in synthesizing medicines like nilutamide, enzalutamide, and apalutamide. Thiohydantoin and selenohydantoin have been discovered as two separate types of hydantoin.
View Article and Find Full Text PDFBMJ Case Rep
January 2025
Internal Medicine, All India Institute of Medical Sciences - Rishikesh, Rishikesh, Uttarakhand, India.
Phenytoin is one of the most used antiepileptic drugs. Isoniazid, a first-line antitubercular drug, blocks the CYP2C19 enzyme, preventing phenytoin from being metabolised. Concomitant use of phenytoin and isoniazid predisposes to phenytoin toxicity.
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