scholarly journals Insight into the antitumor actions of sterically hindered platinum(ii) complexes by a combination of STD NMR and LCMS techniques

Metallomics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 427-434
Author(s):  
Zhimei Wang ◽  
Lei Fang ◽  
Jian Zhao ◽  
Shaohua Gou

The introduction of suitable steric hindrance groups to platinum(ii) complexes is beneficial for drug delivery and overcoming the drawbacks of the current platinum(ii) complexes.

2019 ◽  
Author(s):  
Idriss Curbet ◽  
Sophie Colombel-Rouen ◽  
Romane Manguin ◽  
Anthony Clermont ◽  
Alexandre Quelhas ◽  
...  

<div> <div> <div> <div> <p>The synthesis of conjugated triynes by molybdenum-catalyzed alkyne metathesis is reported. Strategic to the success of this approach is the utilization of sterically-hindered diynes that allowed for the site- selective alkyne metathesis to produce the desired con- jugated triyne products. The steric hindrance of alkyne moiety was found to be crucial in preventing the for- mation of diyne byproducts. This novel synthetic strategy was amenable to self- and cross-metathesis providing straightforward access to the corresponding symmetrical and dissymmetrical triynes with high selectivity. </p> </div> </div> </div> </div>


2021 ◽  
Vol 17 ◽  
Author(s):  
Shadma Wahab ◽  
Md. Parwez Ahmad ◽  
Arshad Hussain ◽  
Shaik Fayazuddin Abdul Qadir

: Nanotechnology is a multidisciplinary domain that involves overlapping of areas such as nonanomaterials, nanoelectronics, and nanobiotechnology. Herbal medicine is a significant component of traditional medicine and has been a treatment part of many diseases. Asian peoples are using these herbal medicines for decades. Still, herbal extracts' therapeutic efficacy and pharmaceutical application are associated with many factors such as poor bioavailability, low solubility, permeability, and lack of targeting potential. In the present work, we have reviewed thriving strategies for the targeted drug delivery of phytoconstituents and critically explain the most recent progressions on emerging novel nanophytomedicine-based materials as herbal medicines carriers. Nanotechnology-based clinical trial studies targeting herbal bioactive compounds were discussed. Advancements in nanotechnology-based drug delivery systems intended to enhance cellular uptake, improved pharmacokinetics and effectiveness of herbal drugs have facilitated the powerful targeting of specific agents against diseases. This review provides insight into current progress and future opportunities for nanomedicines as potential curative targets for the delivery of herbal bioactive compounds. This information could be used as platforms for the future expansion of multi-functional nano constructs for the advanced detection of diseases and functional drug delivery of phytoconstituents.


Author(s):  
Mohammad Ghanaatpishe ◽  
Hosam K. Fathy

This paper examines the shaping of a drug's delivery—in this case, nicotine—to maximize its efficacy. Previous research: (i) furnishes a pharmacokinetic–pharmacodynamic (PKPD) model of this drug's metabolism; (ii) shows that the drug-delivery problem is proper, meaning that its optimal solution is periodic; (iii) shows that the underlying PKPD model is differentially flat; and (iv) exploits differential flatness to solve the problem by optimizing the coefficients of a truncated Fourier expansion of the flat output trajectory. In contrast, the work in this article provides insight into the structure of the theoretical solution to this optimal periodic control (OPC) problem. First, we argue for the existence of a bijection between feasible periodic input and state trajectories of the problem. Second, we exploit Pontryagin's maximum principle to show that the optimal periodic solution has a bang–singular–bang structure. Building on these insights, this article proposes two different numerical methods for solving this OPC problem. One method uses nonlinear programming (NLP) to optimize the states at which the optimal solution transitions between the different solution arcs. The second method approximates the control input trajectory as piecewise constant and optimizes the discrete values of the input sequence. The paper concludes by discussing the computational costs of these two algorithms as well as the importance of the associated insights into the structure of the optimal solution trajectory.


2019 ◽  
Vol 9 (1-s) ◽  
pp. 408-415 ◽  
Author(s):  
Rupalben Kaushalkumar Jani ◽  
Gohil Krupa

In nanomedicines, currently a wide array of reported nanoparticle systems is being explored by targeting schemes which suggests great potential of targeted delivery to revolutionize cancer therapeutics. This review  gives insight into recent  challenges in modification of nanoparticle systems for enhanced cancer therapy  acknowledged by researchers to date and also outlines different major targeting strategies of nanoparticle systems that have been utilized for the delivery of therapeutics or imaging agents, targeting ligand and cross-linking agent to cancer  which was divided into three sections: 1) Angiogenesis associated targeting, 2) Uncontrolled cell proliferation targeting and 3) Tumor cell targeting. Keywords: nanoparticles, tumor cells, active targeting, targeting strategies, targeting ligands


1976 ◽  
Vol 29 (12) ◽  
pp. 2621 ◽  
Author(s):  
RK Norris ◽  
D Randles

The reactions of a series of α-substituted p-nitrobenzyl chlorides, p- NO2C6H4CH(Cl)R (R = Me, Et, Prt, But), with the lithium salt of 2- nitropropane in dimethyl sulphoxide and dimethylformamide have been studied. When R = Me or Et, competing SRN1 and SN2 processes take place, giving C- and O-alkylated products respectively. In the more sterically hindered cases where R = Pri or But, the only reaction taking place has been shown to be an SRN1 reaction with exclusive O-alkylation. These observations indicate that the SRN1 reaction is prone to steric hindrance, and that radical alkylation of the ambident nitronate ion occurs on the more accessible oxygen atom in sterically hindered situations.


2016 ◽  
Vol 52 (77) ◽  
pp. 11539-11542 ◽  
Author(s):  
Maciej Krzeszewski ◽  
Paweł Świder ◽  
Łukasz Dobrzycki ◽  
Michał K. Cyrański ◽  
Witold Danikiewicz ◽  
...  

Sterically hindered tetraaryl-pyrrolo[3,2-b]pyrroles undergo oxidative aromatic coupling, forming a fluorene scaffold linked via a spiro carbon atom with a novel π-conjugated scaffold.


Author(s):  
Joseph T. Keyes ◽  
Bruce R. Simon ◽  
Jonathan P. Vande Geest

Drug-eluting stents (DESs) perform their antiproliferative effects through the use of localized drug delivery. The delivery may be computationally modeled to determine efficacy of the DES-tissue system and utilizes coupled convective and diffusive transport. Since the movement of solutes through the wall is via the coupled effects of convective and diffusive transport, the relative influence of these factors provides insight into the governing forces of localized DES drug delivery [1].


Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 522
Author(s):  
Zhen Li ◽  
Shunqi Mei ◽  
Yajie Dong ◽  
Fenghua She ◽  
Yongzhen Li ◽  
...  

Nanofibrous biomaterials have huge potential for drug delivery, due to their structural features and functions that are similar to the native extracellular matrix (ECM). A wide range of natural and polymeric materials can be employed to produce nanofibrous biomaterials. This review introduces the major natural and synthetic biomaterials for production of nanofibers that are biocompatible and biodegradable. Different technologies and their corresponding advantages and disadvantages for manufacturing nanofibrous biomaterials for drug delivery were also reported. The morphologies and structures of nanofibers can be tailor-designed and processed by carefully selecting suitable biomaterials and fabrication methods, while the functionality of nanofibrous biomaterials can be improved by modifying the surface. The loading and releasing of drug molecules, which play a significant role in the effectiveness of drug delivery, are also surveyed. This review provides insight into the fabrication of functional polymeric nanofibers for drug delivery.


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