scholarly journals Enabling technologies for the preparation of multifunctional “bullets” for nanomedicine

2018 ◽  
pp. 134-143
Author(s):  
K. Martina ◽  
L. Serpe ◽  
R. Cavalli ◽  
G. Cravotto
Keyword(s):  
Ultrasound Irradiation ◽  
Stimuli Responsive ◽  
Enabling Technology ◽  
Drug Formulations ◽  
Transdisciplinary Approach ◽  
Drug Candidates ◽  
The Past ◽  
New Drug ◽  
Enabling Technologies ◽  
Diagnostic Agents

Recent advances in nanotechnology, including modern enabling techniques that can improve synthetic preparation and drug formulations, have opened up new frontiers in nanomedicine with the development of nanoscale carriers and assemblies. The use of delivery platforms has attracted attention over the past decade as researchers shift their focus away from the development of new drug candidates, and toward new means with which to deliver therapeutic and/or diagnostic agents. This work will explore a transdisciplinary approach for the production of a number of nanomaterials, nanocomplexes and nanobubbles and their application in a variety of potential biological and theranostic protocols. Particular attention will be paid to nanobubbles, stimuli responsive nanoparticles and cyclodextrin grafted nanosystems produced under non-conventional conditions, such as microwave and ultrasound irradiation. Besides nanoparticles preparation, ultrasound can also act as an enabling technology when activating sensitive nanobubbles and nanoparticles.

scholarly journals 3-Phenylcoumarins as a Privileged Scaffold in Medicinal Chemistry: The Landmarks of the Past Decade

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6755
Author(s):  
Maria J. Matos ◽  
Eugenio Uriarte ◽  
Lourdes Santana
Keyword(s):  
Medicinal Chemistry ◽  
Review Paper ◽  
Relevant Literature ◽  
Natural Origin ◽  
Drug Candidates ◽  
Heterocyclic Molecules ◽  
The Past ◽  
New Drug ◽  
Privileged Scaffold

3-Phenylcoumarins are a family of heterocyclic molecules that are widely used in both organic and medicinal chemistry. In this overview, research on this scaffold, since 2010, is included and discussed, focusing on aspects related to its natural origin, synthetic procedures and pharmacological applications. This review paper is based on the most relevant literature related to the role of 3-phenylcoumarins in the design of new drug candidates. The references presented in this review have been collected from multiple electronic databases, including SciFinder, Pubmed and Mendeley.

Enabling technologies for ice giant exploration

2020 ◽  
Vol 378 (2187) ◽  
pp. 20190488 ◽  
Author(s):  
Thomas R. Spilker
Keyword(s):  
New Technology ◽  
Giant Planet ◽  
Development Work ◽  
Enabling Technology ◽  
Power Sources ◽  
The Past ◽  
Engineering Development ◽  
Enabling Technologies ◽  
The Cost ◽  
Development Tasks

Future missions to an ice giant planet, especially orbital missions, are technologically challenging. But with one exception, radioisotope power sources (RPSs), the technologies that would enable such missions are currently available. RPSs are not a new technology, but devices used in the past that are appropriate to an ice giant mission are no longer available without engineering development work (currently unfunded), and it is uncertain whether the new NASA unit under development will be available for flight in time to take advantage of the best transfer trajectories of the next 15 years. This paper describes technologies already in hand that enable an ice giant mission, but for them to be useful they must be maintained. If an enabling technology is lost a replacement must be developed, potentially impacting the cost and schedule of a mission. In addition to the enabling technologies, there are a number of technologies that, while not enabling, could greatly enhance the science return and science value of a mission, making the programmatic aspects of approval an easier task and the funding of those development tasks a high priority. This article is part of a discussion meeting issue ‘Future exploration of ice giant systems'.

Fluorocarbon Precursor for High Aspect Ratio via Milling in Focused Ion Beam Modification of Integrated Circuits

2004 ◽  
Author(s):  
Valery Ray
Keyword(s):  
Side Effects ◽  
Aspect Ratio ◽  
Integrated Circuits ◽  
High Aspect Ratio ◽  
Focused Ion Beam ◽  
Ion Beam ◽  
Enabling Technology ◽  
Si Substrate ◽  
Ion Beam Modification ◽  
The Past

Abstract Gas Assisted Etching (GAE) is the enabling technology for High Aspect Ratio (HAR) circuit access via milling in Focused Ion Beam (FIB) circuit modification. Metal interconnect layers of microelectronic Integrated Circuits (ICs) are separated by Inter-Layer Dielectric (ILD) materials, therefore HAR vias are typically milled in dielectrics. Most of the etching precursor gases presently available for GAE of dielectrics on commercial FIB systems, such as XeF2, Cl2, etc., are also effective etch enhancers for either Si, or/and some of the metals used in ICs. Therefore use of these precursors for via milling in dielectrics may lead to unwanted side effects, especially in a backside circuit edit approach. Making contacts to the polysilicon lines with traditional GAE precursors could also be difficult, if not impossible. Some of these precursors have a tendency to produce isotropic vias, especially in Si. It has been proposed in the past to use fluorocarbon gases as precursors for the FIB milling of dielectrics. Preliminary experimental evaluation of Trifluoroacetic (Perfluoroacetic) Acid (TFA, CF3COOH) as a possible etching precursor for the HAR via milling in the application to FIB modification of ICs demonstrated that highly enhanced anisotropic milling of SiO2 in HAR vias is possible. A via with 9:1 aspect ratio was milled with accurate endpoint on Si and without apparent damage to the underlying Si substrate.

Antitubercular Marine Natural Products

2018 ◽  
Vol 25 (20) ◽  
pp. 2304-2328 ◽  
Author(s):  
Lishu Wang ◽  
Jungfeng Wang ◽  
Juan Liu ◽  
Yonghong Liu
Keyword(s):  
Natural Products ◽  
Marine Natural Products ◽  
Antitubercular Activity ◽  
Marine Resources ◽  
Drug Candidates ◽  
New Drug ◽  
Chemical Constitution

Due to the importance of nature as a source of new drug candidates, the purpose of this article is to emphasize the marine natural products, which exhibit antitubercular activity, published between January 2000 and May 2016, with 138 quotations to 250 compounds obtained from marine resources. These metabolites are organized by chemical constitution and named as simple alkyl lipids derivatives, aromatics derivatives, peptides, alkaloids, terpenoids, steroids, macrolides, and polycyclic polyketides.

Click Reactions in Chemistry of Triterpenes - Advances Towards Development of Potential Therapeutics

2018 ◽  
Vol 25 (5) ◽  
pp. 636-658 ◽  
Author(s):  
Jan Pokorny ◽  
Lucie Borkova ◽  
Milan Urban
Keyword(s):  
Biological Activities ◽  
Synthetic Approach ◽  
Clinical Use ◽  
New Approach ◽  
Click Reactions ◽  
Drug Candidates ◽  
The Past ◽  
Low Toxicity ◽  
New Compounds ◽  
Potential Therapeutics

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.

Current Approaches to Drug Discovery for Chagas Disease: Methodological Advances

2019 ◽  
Vol 22 (8) ◽  
pp. 509-520
Author(s):  
Cauê B. Scarim ◽  
Chung M. Chin
Keyword(s):  
Drug Discovery ◽  
Chagas Disease ◽  
Drug Candidates ◽  
Lead Compounds ◽  
New Drug ◽  
Compound Libraries ◽  
Screening Assays ◽  
Cruzi Infection

Background: In recent years, there has been an improvement in the in vitro and in vivo methodology for the screening of anti-chagasic compounds. Millions of compounds can now have their activity evaluated (in large compound libraries) by means of high throughput in vitro screening assays. Objective: Current approaches to drug discovery for Chagas disease. Method: This review article examines the contribution of these methodological advances in medicinal chemistry in the last four years, focusing on Trypanosoma cruzi infection, obtained from the PubMed, Web of Science, and Scopus databases. Results: Here, we have shown that the promise is increasing each year for more lead compounds for the development of a new drug against Chagas disease. Conclusion: There is increased optimism among those working with the objective to find new drug candidates for optimal treatments against Chagas disease.

Molecular Topological Properties of Alkylating Agents Based Anticancer Drug Candidates Via Some Ve-degree Topological Indices

2020 ◽  
Vol 16 (2) ◽  
pp. 190-195 ◽  
Author(s):  
Süleyman Ediz ◽  
Murat Cancan
Keyword(s):  
Anticancer Drugs ◽  
Anticancer Drug ◽  
Alkylating Agents ◽  
Topological Indices ◽  
Pharmacological Properties ◽  
Topological Properties ◽  
Drug Candidates ◽  
New Drug ◽  
Atom Bond ◽  
Dual Target

Background: Reckoning molecular topological indices of drug structures gives the data about the underlying topology of these drug structures. Novel anticancer drugs have been leading by researchers to produce ideal drugs. Materials and Methods: Pharmacological properties of these new drug agents explored by utilizing simulation strategies. Topological indices additionally have been utilized to research pharmacological properties of some drug structures. Novel alkylating agents based anticancer drug candidates and ve-degree molecular topological indices have been introduced recently. Results and Conclusion: In this study we calculate ve-degree atom-bond connectivity, harmonic, geometric-arithmetic and sum-connectivity molecular topological indices for the newly defined alkylating agents based dual-target anticancer drug candidates.

Cucurbitacins as Anticancer Agents: A Patent Review

2019 ◽  
Vol 14 (2) ◽  
pp. 133-143 ◽  
Author(s):  
Hidayat Hussain ◽  
Ivan R. Green ◽  
Muhammad Saleem ◽  
Khanzadi F. Khattak ◽  
Muhammad Irshad ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Wide Spectrum ◽  
Biological Effects ◽  
Therapeutic Effects ◽  
Cytotoxic Effects ◽  
Natural Sources ◽  
Oh Groups ◽  
Drug Candidates ◽  
The Past ◽  
Wide Range

Background: Cucurbitacins belong to a group of tetracyclic triterpenoids that display a wide range of biological effects. In the past, numerous cucurbitacins have been isolated from natural sources and many active compounds have been synthesized using the privileged scaffold in order to enhance its cytotoxic effects. Objective: his review covers patents on the therapeutic effects of natural cucurbitacins and their synthetic analogs published during the past decade. By far, the majority of patents published are related to cancer and Structure-Activity Relationships (SAR) of these compounds are included to lend gravitas to this important class of natural products. Methods: The date about the published patents was downloaded via online open access patent databases. Results: Cucurbitacins display significant cytotoxic properties, in particular cucurbitacins B and D which possess very potent effects towards a number of cancer cells. Numerous cucurbitacins isolated from natural sources have been derivatized through chemical modification at the C(2)-OH and C(25)- OH groups. Most importantly, an acyl ester of the C(25)-OH and, iso-propyl, n-propyl and ethyl ether groups of the C(2)-OH demonstrated the most increased cytotoxic activity. Conclusion: The significant cytotoxic effects of natural and semi-synthetic cucurbitacins make them attractive as new drug candidates. Moreover, cucurbitacins have the capability to form conjugates with other anticancer drugs which will synergistically enhance their anticancer effects. The authors believe that in order to get lead compounds, there should be a greater focus on the synthesis of homodimers, heterodimers, and halo derivatives of cucurbitacins. In the opinion of the authors the analysis of the published patents on the cucurbitacins indicates that these compounds can be developed into a regimen to treat a wide spectrum of cancers.

Investigations on T cell transmigration in a human skin-on-chip (SoC) model

Lab on a Chip ◽  
2021 ◽  
Vol 21 (8) ◽  
pp. 1527-1539
Author(s):  
Xiaoou Ren ◽  
Anthony E. Getschman ◽  
Samuel Hwang ◽  
Brian F. Volkman ◽  
Thomas Klonisch ◽  
...  
Keyword(s):  
T Cell ◽  
T Lymphocytes ◽  
Human Skin ◽  
Drug Candidates ◽  
New Drug ◽  
Human T Lymphocytes ◽  
Quantitative Studies ◽  
Inflammatory Skin ◽  
Skin Conditions ◽  
On Chip

Our skin-on-chip (SoC) model uniquely enabled quantitative studies of transendothelial and transepithelial migration of human T lymphocytes under mimicked inflammatory skin conditions and was used to test new drug candidates.

scholarly journals Advances in Molecularly Imprinted Polymers as Drug Delivery Systems

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3589
Author(s):  
Rui Liu ◽  
Alessandro Poma
Keyword(s):  
Drug Delivery ◽  
Molecularly Imprinted Polymers ◽  
Drug Loading ◽  
Stimuli Responsive ◽  
Molecularly Imprinted ◽  
Imprinted Polymers ◽  
Drug Delivery Vehicles ◽  
The Past ◽  
Drug Molecules ◽  
Delivery Vehicles

Despite the tremendous efforts made in the past decades, severe side/toxic effects and poor bioavailability still represent the main challenges that hinder the clinical translation of drug molecules. This has turned the attention of investigators towards drug delivery vehicles that provide a localized and controlled drug delivery. Molecularly imprinted polymers (MIPs) as novel and versatile drug delivery vehicles have been widely studied in recent years due to the advantages of selective recognition, enhanced drug loading, sustained release, and robustness in harsh conditions. This review highlights the design and development of strategies undertaken for MIPs used as drug delivery vehicles involving different drug delivery mechanisms, such as rate-programmed, stimuli-responsive and active targeting, published during the course of the past five years.

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