scholarly journals Efficient cleavage of tertiary amide bonds via radical–polar crossover using a copper(ii) bromide/Selectfluor hybrid system

2020 ◽  
Vol 11 (45) ◽  
pp. 12323-12328
Author(s):  
Zhe Wang ◽  
Akira Matsumoto ◽  
Keiji Maruoka

A novel approach for the efficient cleavage of the amide bonds in tertiary amides is reported.

2018 ◽  
Author(s):  
Benjamin Stenton ◽  
Bruno Oliveira ◽  
João Conde ◽  
Magda Negrão ◽  
Miguel Godinho Ferreira ◽  
...  

<p>Creating ways to control drug activation at specific tissues while sparing healthy tissues remains a major challenge. The administration of exogenous triggers offers the possibility for precise and traceless drug activation. However, ensuring localization of the trigger as well as the prodrug at the diseased tissue is complex while essential for therapeutic efficacy and to avoid side-toxicity. Cisplatin remains a first line option to treat 20% of all cancer patients and while clearing after 30 min from blood it concentrates in tumor tissues. Here, we demonstrate the use of the platinum-mediated bond cleavage of protected tertiary amides, which can occur in a catalytic manner under bioorthogonal conditions. Protected analogues of cytotoxic drugs 5-fluorouracil (5-FU) and monomethyl auristatin E (MMAE) were successfully activated using non-toxic amounts of platinum salts in cells. An otherwise fully stable and non-internalizing ADC built using a bifunctional linker featuring a tertiary amide protected MMAE was also bioorthogonally decaged in the presence of platinum salts for extracellular drug release. Finally, cisplatin-mediated activation of a prodrug 5-FU was shown in a colorectal zebrafish xenograft model leading to a significant tumor reduction. Considering cisplatin’s continued use as a first-choice treatment for many solid cancers and especially in colorectal cancer, we anticipate that our platinum-mediated decaging strategy will enhance cancer therapy by allowing tumor specific prodrug activation.</p>


2018 ◽  
Author(s):  
Benjamin Stenton ◽  
Bruno Oliveira ◽  
João Conde ◽  
Magda Negrão ◽  
Miguel Godinho Ferreira ◽  
...  

<p>Creating ways to control drug activation at specific tissues while sparing healthy tissues remains a major challenge. The administration of exogenous triggers offers the possibility for precise and traceless drug activation. However, ensuring localization of the trigger as well as the prodrug at the diseased tissue is complex while essential for therapeutic efficacy and to avoid side-toxicity. Cisplatin remains a first line option to treat 20% of all cancer patients and while clearing after 30 min from blood it concentrates in tumor tissues. Here, we demonstrate the use of the platinum-mediated bond cleavage of protected tertiary amides, which can occur in a catalytic manner under bioorthogonal conditions. Protected analogues of cytotoxic drugs 5-fluorouracil (5-FU) and monomethyl auristatin E (MMAE) were successfully activated using non-toxic amounts of platinum salts in cells. An otherwise fully stable and non-internalizing ADC built using a bifunctional linker featuring a tertiary amide protected MMAE was also bioorthogonally decaged in the presence of platinum salts for extracellular drug release. Finally, cisplatin-mediated activation of a prodrug 5-FU was shown in a colorectal zebrafish xenograft model leading to a significant tumor reduction. Considering cisplatin’s continued use as a first-choice treatment for many solid cancers and especially in colorectal cancer, we anticipate that our platinum-mediated decaging strategy will enhance cancer therapy by allowing tumor specific prodrug activation.</p>


Author(s):  
Michael G. Karnavas

The investigation of war crimes has proved to be a challenging task for the Defence at the International Criminal Tribunal for the former Yugoslavia (ICTY). At the Court’s infancy, civil trained defence counsel with no experience in adversarial party-driven procedures were unfamiliar with aspects of case preparation and trial advocacy, such as gathering evidence by conducting their own investigation, or cross-examination through leading questions based on a coherent theory of the case. These adversarial modalities also came with specific ethical duties. This chapter offers some practical advice and best practices relevant to Defence Counsel practising in national jurisdictions of the former Yugoslavia region and elsewhere, where adversarial modalities similar to those found in the ICTY procedure have been adopted in reforming their criminal procedures—transitioning them from civil law to a more hybrid system.


RSC Advances ◽  
2014 ◽  
Vol 4 (73) ◽  
pp. 38761-38768 ◽  
Author(s):  
X. Y. Xu ◽  
B. Yan

Multi-component sol–gel derived alumina and titania hybrid materials are assembled by the functionalization of both lanthanide complexes and a special metal organic framework compound: Al-MIL-53-COOH through coordination bonds. Multi-color luminescence and white colored light can be tuned by controlling the different units in the hybrid system.


2020 ◽  
Vol 6 (3) ◽  
pp. 747-756 ◽  
Author(s):  
Haiman Wang ◽  
Zhuang Miao ◽  
Yafeng Li ◽  
Weihua He ◽  
Youpeng Qu ◽  
...  

A MES-centered hybrid system was developed with well-matched current generation, efficient organic matter removal and subsequent nitrogen removal.


2019 ◽  
Vol 9 (3) ◽  
pp. 506 ◽  
Author(s):  
Yi-Huan Lee ◽  
Yan-Nian Zhuang ◽  
Hsin-Ta Wang ◽  
Ming-Feng Wei ◽  
Wen-Chi Ko ◽  
...  

In this study, we report a novel approach to fabricate an organic/inorganic magnetic hybrid system capable of self-healing, wherein a polycaprolactone-poly(furfuryl glycidyl ether) copolymer (PCLF) serving as the structure template was first synthesized, followed by the incorporation of iron oxide nanoparticles-decorated multiwalled carbon nanotubes (IONPs-MWCNTs) and 1,1′-(methylenedi-4,1-phenylene)bismaleimide (BMI) into the polymer matrix to form a covalently crosslinked hybrid network via a Diels−Alder (DA) reaction. For this system, the reactive combination of diene and dienophile from furan/maleimide, MWCNT/furan, and MWCNT/maleimide could facilely induce multiple DA reactions that imparted a versatile route to efficiently introduce IONPs-MWCNTs into the organic polymer hosts, resulting in a uniform distribution of IONPs-MWCNTs that led to a hybrid system with superparamagnetic properties. Beside the magnetic behavior, such material synergistically exhibited a superior ability for healing scratch defects via a retro-DA reaction. Therefore, this crosslinked PCLF/BMI/IONPs-MWCNTs hybrid system which exhibits multifunctional properties including superparamagnetic behavior and self-repairability can serve as an intelligent material for developing advanced electromagnetic applications.


2015 ◽  
Vol 17 (18) ◽  
pp. 12051-12055 ◽  
Author(s):  
Kaibiao Zhang ◽  
Hong Zhang ◽  
Chikang Li

Noble metal nanoparticles can modify the optical properties of graphene.


RSC Advances ◽  
2014 ◽  
Vol 4 (77) ◽  
pp. 40828-40836 ◽  
Author(s):  
Piao Xu ◽  
Guangming Zeng ◽  
Danlian Huang ◽  
Liang Liu ◽  
Cui Lai ◽  
...  

A novel approach for phenol removal using Fe3O4 nanoparticles and oxalate was proposed via a radical mechanism.


Nanoscale ◽  
2019 ◽  
Vol 11 (35) ◽  
pp. 16284-16292 ◽  
Author(s):  
Ashley M. Hancock ◽  
Sophie A. Meredith ◽  
Simon D. Connell ◽  
Lars J. C. Jeuken ◽  
Peter G. Adams

Self-assembled proteoliposomes allow highly efficient energy transfer from the spectrally-complementary chromophore Texas Red to the plant light-harvesting protein LHCII, increasing the effective absorption range of this bio-hybrid system.


Sign in / Sign up

Export Citation Format

Share Document