Silicon switch: Carbon–silicon Bioisosteric replacement as a strategy to modulate the selectivity, physicochemical, and drug‐like properties in anticancer pharmacophores

Abstract

Cancer is a generic term used for different types of rapid and abnormal cell growth beyond their usual boundaries, affecting different parts of the body and spreading to different organs. As such, cancer is one of the most prevalent and devastating conditions, and a leading cause of death worldwide, claiming about 10 million lives in 2020, according to recent data from the World Health Organization (WHO) (Ferlay et al., 2020). Recent studies have also indicated that lung, colon and rectum, liver, stomach, and breast cancer are among the deadliest types of cancers worldwide (La Vecchia et al., 2022;Mabry et al., 2022;Mattiuzzi & Lippi, 2019;Wen & Shen, 2022). Furthermore, it is estimated that ~400,000 children under 14 years of age are diagnosed with cancer each year across the globe, with lymphomas, retinoblastoma, renal tumors, leukemias, and soft tissue sarcomas being among the major forms of childhood cancers (Ferlay et al., 2020;Libes et al., 2023;Lupo et al., 2021;Ross & Olshan, 2004). Despite significant advances in the development of selective and targeted therapies, including tumor-targeting chemotherapies (

Regioselective Fluorohydrin Synthesis from Allylsilanes and Evidence for a Silicon–Fluorine Gauche Effect

“…Given not only the value of fluorine-containing compounds for drug discovery − but also an emerging interest in organosilanes for this purpose, silicon-substituted fluorohydrins could present a novel platform for designing conformationally restricted biologically active structures. Alternatively, oxidative desilylation would generate 2-fluoro-1,3-propanediols, which have proven to be useful for studying enzymatic reactions involving glycerol , as well as starting points to access fluorinated carbohydrate analogues of medicinal value .…”

Advances in disilylation reactions to access cis/trans-1,2-disilylated and gem-disilylated alkenes

“…9–12 Carbon/silicon exchange, particularly in drug design, will enhance chemical diversity and modify the physiological and biological properties of bioactive molecules. 13,14 In materials science, the heat resistance, photostability, and transparency of organosilicon materials also make silicon highly attractive. 15,16 Additionally, silicon compounds exhibit versatility in synthetic conversions, with silyl groups serving as temporary functional groups amenable to further functionalization.…”

Photoredox Synthesis of Silicon-Containing Isoindolin-1-ones and Deuterated Analogues Through Hydrosilylation and Deuterium-silylation

“…As the second-largest element of the earth’s crust, silicon has been widely installed into many organic molecules, and the resulting organosilicon compounds have widespread applications in material science and organic synthesis . In addition, owing to the low toxicity and high lipophilicity nature of silicon, organosilicon derivatives also play an important role in medicinal chemistry . Along this line, the incorporation of silicon moieties into medicinally important scaffolds would offer an innovative avenue for drug discovery.…”