Small molecule activation by boron-containing heterocycles

2019 ◽  
Vol 48 (13) ◽  
pp. 3613-3659 ◽  
Author(s):  
Yuanting Su ◽  
Rei Kinjo

This review focuses on boron-containing heterocycles enabling the activation of σ- and π-bonds in small molecules.

2019 ◽  
Vol 48 (33) ◽  
pp. 12365-12381 ◽  
Author(s):  
Laurence J. Taylor ◽  
Deborah L. Kays

In this Perspective, we will highlight selected examples of transition metal complexes with low coordination numbers whose high reactivity has been exploited in catalysis and the activation of small molecules featuring strong bonds (N2, CO2, and CO).


2021 ◽  
Author(s):  
Yong-Peng Shen ◽  
Hong-Xue Cai ◽  
Fang-Yuan Chen ◽  
Yuan-Ru Guo ◽  
Qing-Jiang Pan

DFT calculations rationalize the capability of uranium metallocenes in activating small molecules, and the experimentally inaccessible CO2 adduct is addressed.


RSC Advances ◽  
2018 ◽  
Vol 8 (46) ◽  
pp. 26271-26276 ◽  
Author(s):  
Yiheng Wang ◽  
Zhen Hua Li ◽  
Huadong Wang

An oxygen-linked germinal frustrated Lewis pair was synthesized and its reactivities against a series of small molecules were investigated.


2019 ◽  
Vol 48 (18) ◽  
pp. 5869-5878 ◽  
Author(s):  
Elodie Anxolabéhère-Mallart ◽  
Julien Bonin ◽  
Claire Fave ◽  
Marc Robert

Substituted tetraphenyl Fe porphyrins are versatile molecular catalysts for the activation of small molecules (such as O2, H+ or CO2), which could lead to renewable energy storage, the direct production of fuels or new catalytic relevant processes.


Author(s):  
Peter Werner Roesky ◽  
Niklas Reinfandt ◽  
Nadine Michenfelder ◽  
Christoph Schoo ◽  
Ravi Yadav ◽  
...  

2020 ◽  
Vol 22 (Supplement_2) ◽  
pp. ii200-ii200
Author(s):  
Stephen Skirboll ◽  
Natasha Lucki ◽  
Genaro Villa ◽  
Naja Vergani ◽  
Michael Bollong ◽  
...  

Abstract INTRODUCTION Glioblastoma multiforme (GBM) is the most aggressive form of primary brain cancer. A subpopulation of multipotent cells termed GBM cancer stem cells (CSCs) play a critical role in tumor initiation and maintenance, drug resistance, and recurrence following surgery. New therapeutic strategies for the treatment of GBM have recently focused on targeting CSCs. Here we have used an unbiased large-scale screening approach to identify drug-like small molecules that induce apoptosis in GBM CSCs in a cell type-selective manner. METHODS A luciferase-based survival assay of patient-derived GBM CSC lines was established to perform a large-scale screen of ∼one million drug-like small molecules with the goal of identifying novel compounds that are selectively toxic to chemoresistant GBM CSCs. Compounds found to kill GBM CSC lines as compared to control cell types were further characterized. A caspase activation assay was used to evaluate the mechanism of induced cell death. A xenograft animal model using patient-derived GBM CSCs was employed to test the leading candidate for suppression of in vivo tumor formation. RESULTS We identified a small molecule, termed RIPGBM, from the cell-based chemical screen that induces apoptosis in primary patient-derived GBM CSC cultures. The cell type-dependent selectivity of RIPGBM appears to arise at least in part from redox-dependent formation of a proapoptotic derivative, termed cRIPGBM, in GBM CSCs. cRIPGBM induces caspase 1-dependent apoptosis by binding to receptor-interacting protein kinase 2 (RIPK2) and acting as a molecular switch, which reduces the formation of a prosurvival RIPK2/TAK1 complex and increases the formation of a proapoptotic RIPK2/caspase 1 complex. In an intracranial GBM xenograft mouse model, RIPGBM was found to significantly suppress tumor formation. CONCLUSIONS Our chemical genetics-based approach has identified a small molecule drug candidate and a potential drug target that selectively targets cancer stem cells and provides an approach for the treatment of GBMs.


Sign in / Sign up

Export Citation Format

Share Document