Quest for novel chemical entities through incorporation of silicon in drug scaffolds

R Ramesh, DS Reddy - Journal of Medicinal Chemistry, 2017 - ACS Publications
In order to optimize a lead molecule for further development, bioisosteric replacements are
generally adopted as one of the strategies. Silicon appears to be the right choice as a …

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

J Fotie, CM Matherne… - Chemical Biology & Drug …, 2023 - Wiley Online Library
Bioisosterism is one of the leading strategies in medicinal chemistry for the design and
modification of drugs, consisting in replacing an atom or a substituent with a different atom or …

Base-modified nucleosides as chemotherapeutic agents: past and future

MP Burke, KM Borland… - Current Topics in Medicinal …, 2016 - ingentaconnect.com
Nucleoside and nucleobase antimetabolites have substantially impacted treatment of cancer
and infections. Their close resemblance to natural analogs gives them the power to interfere …

Antiproliferative effects of selective adenosine receptor agonists and antagonists on human lymphocytes: evidence for receptor-independent mechanisms

AC Schiedel, SK Lacher, C Linnemann, PA Knolle… - Purinergic …, 2013 - Springer
The effects of standard adenosine receptor (AR) agonists and antagonists on the
proliferation of human T lymphocytes, unstimulated and phytohemagglutinin-stimulated …

The role of silicon in drug discovery: a review

JL Panayides, DL Riley, F Hasenmaile… - RSC Medicinal …, 2024 - pubs.rsc.org
This review aims to highlight the role of silicon in drug discovery. Silicon and carbon are
often regarded as being similar with silicon located directly beneath carbon in the same …

Synthesis and in vitro growth inhibitory activity of novel silyl-and trityl-modified nucleosides

JL Panayides, V Mathieu, LMY Banuls… - Bioorganic & medicinal …, 2016 - Elsevier
Seventeen silyl-and trityl-modified (5′-O-and 3′, 5′-di-O-) nucleosides were synthesized
with the aim of investigating the in vitro antiproliferative activities of these nucleoside …

Synthesis and SAR of 2′, 3′-bis-O-substituted N6, 5′-bis-ureidoadenosine derivatives: Implications for prodrug delivery and mechanism of action

JR Shelton, CE Cutler, MS Browning, J Balzarini… - Bioorganic & medicinal …, 2012 - Elsevier
A series of 2′, 3′-bis-O-silylated or-acylated derivatives of lead compound 3a (2′, 3′-
bis-O-tert-butyldimethylsilyl-5′-deoxy-5′-(N-methylcarbamoyl) amino-N6-(N …

Novel 5-Arylcarbamoyl-2-methylisoxazolidin-3-yl-3-phosphonates as Nucleotide Analogues

K Kokosza, J Balzarini… - … , Nucleotides and Nucleic …, 2014 - Taylor & Francis
A series of 5-substituted 3-phosphonylated isoxazolidines have been obtained via
cycloaddition of N-methyl-C-(diethoxyphosphoryl) nitrone with N-heteroaromatic …

Arylurea Derivatives: A Class of Potential Cancer Targeting Agents

JN Chen, DW Wu, T Li, KJ Yang… - Current topics in …, 2017 - ingentaconnect.com
Arylurea derivatives, an important class of small molecules, have received considerable
attention in recent years due to their wide range of biological applications. Various …

Synthesis and Conformational Analysis of 2‐O‐Silyl Protected Nucleosides from Unprotected Nucleobases and Sugar Epoxides

A Ahmed, F Rasool, G Singh, M Katoch… - European Journal of …, 2020 - Wiley Online Library
Synthesis of orthogonally protected 2‐silyl nucleosides were achieved by trans opening of
sugar epoxides with nucleobases catalyzed by trimethylsilyltrifluoromethanesulfonate using …