74901-08-9Relevant articles and documents
Diazaborines Are a Versatile Platform to Develop ROS-Responsive Antibody Drug Conjugates**
Aguiar, Sandra I.,André, Ana S.,António, Jo?o P. M.,Bernardes, Gon?alo J. L.,Carvalho, Joana Inês,Dias, Joana N. R.,Faustino, Hélio,Gois, Pedro M. P.,Lopes, Ricardo M. R. M.,Veiros, Luis F.,da Silva, Frederico A.
, p. 25914 - 25921 (2021/11/09)
Antibody–drug conjugates (ADCs) are a new class of therapeutics that combine the lethality of potent cytotoxic drugs with the targeting ability of antibodies to selectively deliver drugs to cancer cells. In this study we show for the first time the synthesis of a reactive-oxygen-species (ROS)-responsive ADC (VL-DAB31-SN-38) that is highly selective and cytotoxic to B-cell lymphoma (CLBL-1 cell line, IC50 value of 54.1 nM). The synthesis of this ADC was possible due to the discovery that diazaborines (DABs) are a very effective ROS-responsive unit that are also very stable in buffer and in plasma. DFT calculations performed on this system revealed a favorable energetic profile (ΔGR=?74.3 kcal mol?1) similar to the oxidation mechanism of aromatic boronic acids. DABs’ very fast formation rate and modularity enabled the construction of different ROS-responsive linkers featuring self-immolative modules, bioorthogonal functions, and bioconjugation handles. These structures were used in the site-selective functionalization of a VL antibody domain and in the construction of the homogeneous ADC.
Covalently functionalized carbon nanoparticles with a chiral Mn-Salen: A new nanocatalyst for enantioselective epoxidation of alkenes
Zammataro, Agatino,Gangemi, Chiara Maria Antonietta,Pappalardo, Andrea,Toscano, Rosa Maria,Puglisi, Roberta,Nicotra, Giuseppe,Fragalà, Maria Elena,Tuccitto, Nunzio,Sfrazzetto, Giuseppe Trusso
, p. 5255 - 5258 (2019/05/08)
A new protocol to obtain carbon nanoparticles (CNPs) covalently functionalized with a chiral Mn-Salen catalyst is described here. The new nanocatalyst (CNPs-Mn-Salen) was tested in the enantioselective epoxidation of some representative alkenes (CN-chromene, 1,2-dihydronaphthalene and cis-β-ethyl styrene), obtaining better enantiomeric excess values than that of the catalyst single molecule, highlighting the role of the nanostructure in the enantioselectivity.
Nerve Gas Simulant Sensing by a Uranyl–Salen Monolayer Covalently Anchored on Quartz Substrates
Trusso Sfrazzetto, Giuseppe,Millesi, Salvatrice,Pappalardo, Andrea,Tomaselli, Gaetano A.,Ballistreri, Francesco P.,Toscano, Rosa Maria,Fragalà, Ignazio,Gulino, Antonino
, p. 1576 - 1583 (2017/02/10)
A uranyl complex monolayer that easily allows the optical detection of a nerve gas simulant, namely, dimethyl methylphosphonate, is reported. Both UV/Vis spectroscopy and photoelectron data confirm that the functional hybrid material coordinates a Lewis base by means of the P=O group, which interacts with the uranium equatorial site available for complexation.