Jinlian Wei

Higher Fsp ³ often correlates with clinical success, driving the replacement of flat arenes with saturated carbocycles. Stereodefined 1,1,3‐trisubstituted cyclobutane and 1,2,4‐trisubstituted bicyclo[2.1.1]hexane (BCH) serve as bioisosteres for para ‐ and 1,2,4‐trisubstituted benzenes, respectively. Yet, general stereoselective routes to these frameworks remain underdeveloped. In this study, we report a photocatalytic transannular functional group migration (TFGM) strategy that enables highly diastereoselective synthesis of 1,1,3‐trisubstituted cyclobutanes from alkylidene cyclobutanes and diverse radical precursors at room temperature. The reaction proceeds through a rigid BCH‐type transition state, delivering exclusive cis ‐selectivity. The mild conditions accommodate broad functional group tolerance and support the migration of various groups, including heteroarenes, nitrile, aldehyde, oxime, and alkene derivatives. This platform further provides general and modular entry to 1,2,4‐trisubstituted BCHs via a base‐promoted 5‐exo‐tet cyclization and cross‐coupling sequence. The resulting BCH scaffolds are effective bioisosteres of 1,2,4‐trisubstituted benzenes, demonstrated by BCH‐Olaparib and BCH‐Fluzoparib—analogues of the anticancer drugs Olaparib and Fluzoparib. These analogues retain potent activity comparable to Olaparib in a panel of cancer cell lines (enhanced in breast and liver cells), and the preferred enantiomer of BCH‐Olaparib surpasses Olaparib in PARP1 inhibition, validating 1,2,4‐trisubstituted BCHs as faithful benzenoid bioisosteres for drug innovation.

Higher Fsp ³ often correlates with clinical success, driving the replacement of flat arenes with saturated carbocycles. Stereodefined 1,1,3‐trisubstituted cyclobutane and 1,2,4‐trisubstituted bicyclo[2.1.1]hexane (BCH) serve as bioisosteres for para ‐ and 1,2,4‐trisubstituted benzenes, respectively. Yet, general stereoselective routes to these frameworks remain underdeveloped. In this study, we report a photocatalytic transannular functional group migration (TFGM) strategy that enables highly diastereoselective synthesis of 1,1,3‐trisubstituted cyclobutanes from alkylidene cyclobutanes and diverse radical precursors at room temperature. The reaction proceeds through a rigid BCH‐type transition state, delivering exclusive cis ‐selectivity. The mild conditions accommodate broad functional group tolerance and support the migration of various groups, including heteroarenes, nitrile, aldehyde, oxime, and alkene derivatives. This platform further provides general and modular entry to 1,2,4‐trisubstituted BCHs via a base‐promoted 5‐exo‐tet cyclization and cross‐coupling sequence. The resulting BCH scaffolds are effective bioisosteres of 1,2,4‐trisubstituted benzenes, demonstrated by BCH‐Olaparib and BCH‐Fluzoparib—analogues of the anticancer drugs Olaparib and Fluzoparib. These analogues retain potent activity comparable to Olaparib in a panel of cancer cell lines (enhanced in breast and liver cells), and the preferred enantiomer of BCH‐Olaparib surpasses Olaparib in PARP1 inhibition, validating 1,2,4‐trisubstituted BCHs as faithful benzenoid bioisosteres for drug innovation.

Cyclocybe cylindracea , commonly known as “Chaxingu” in China, is an edible and medicinal mushroom that has attracted increasing interest because of its bioactive polysaccharides. Cyclocybe cylindracea polysaccharides (CCPs) have been reported to exhibit antioxidant, immunomodulatory, antitumor, anti‐aging, hypoglycemic, hypolipidemic, anti‐inflammatory, and gut microbiota‐modulating activities. A structured literature search was conducted across major scientific databases, and eligible studies were screened according to predefined inclusion and exclusion criteria. This review summarizes recent advances in the extraction, purification, structural characterization, biological activities, structure–activity relationships, applications, and safety evaluation of CCPs. Particular attention is given to the effects of extraction and purification methods on polysaccharide yield, purity, molecular weight, monosaccharide composition, structural features, and biological functions. Current evidence indicates that CCPs have potential as functional food ingredients, health products, and pharmaceutical adjuvants. Nevertheless, further studies are required to clarify their fine structures, active fractions, structure–activity relationships, bioavailability, in vivo mechanisms, safety, and clinical efficacy. This review provides a focused reference for future research, quality control, and value‐added development of CCPs.