New Pd/Pt(ii) complexes as unsymmetrical ylide-based chemotherapeutic agents: synthesis, characterization, biological activity, electrochemical, and X-ray studies

2018 ◽  
Vol 42 (11) ◽  
pp. 8968-8978 ◽  
Author(s):  
Seyyed Javad Sabounchei ◽  
Khadijeh Badpa ◽  
Davood Nematollahi ◽  
Mahnaz Sharafi-kolkeshvandi ◽  
Leila Hosseinzadeh ◽  
...  
Keyword(s):  
Biological Activity ◽  
Chemotherapeutic Agents ◽  
Cellular Imaging ◽  
X Ray ◽  
Cytotoxic Studies

New P,C-coordinated Pd/Pt-complexes were characterized successfully and the cytotoxic studies showed that they can be used as non-toxic labels for cellular imaging.

scholarly journals New Haloterpenes from the Marine Red Alga Laurencia papillosa: Structure Elucidation and Biological Activity

Marine Drugs ◽  
2021 ◽  
Vol 19 (1) ◽  
pp. 35
Author(s):  
Mohamed Shaaban ◽  
Ghada S. E. Abou-El-Wafa ◽  
Christopher Golz ◽  
Hartmut Laatsch
Keyword(s):  
Biological Activity ◽  
Crude Extract ◽  
Structure Elucidation ◽  
Antimicrobial Activities ◽  
Red Alga ◽  
Spectroscopic Methods ◽  
X Ray Diffraction ◽  
X Ray ◽  
Chemical Structures ◽  
Terpene Derivatives

Analysis of the air-dried marine red alga Laurencia papillosa, collected near Ras-Bakr at the Suez gulf (Red Sea) in Egypt delivered five new halogenated terpene derivatives: aplysiolic acid (1), 7-acetyl-aplysiol (2), aplysiol-7-one (3), 11,14-dihydroaplysia-5,11,14,15-tetrol (5a), and a new maneonene derivative 6, named 5-epi-maneolactone. The chemical structures of these metabolites were characterized employing spectroscopic methods, and the relative and absolute configurations were determined by comparison of experimental and ab initio-calculated NMR, NOE, ECD, and ORD data, and by X-ray diffraction of 2 and 6. The antimicrobial activities of the crude extract and compounds 1–3, 5a and 6 were studied.

Isoselenocyanates: Synthesis and Their Use for Preparing Selenium-Based Heterocycles

Synthesis ◽  
2021 ◽  
Author(s):  
Stefan H. Bossmann ◽  
Raul Neri
Keyword(s):  
Biological Activity ◽  
Infectious Diseases ◽  
Cancer Cells ◽  
Multicomponent Reactions ◽  
Oxidative Cyclization ◽  
Biologically Active ◽  
Organoselenium Compounds ◽  
X Ray ◽  
Synthetic Work

AbstractIsoselenocyanates (ISCs) are a class of organoselenium compounds that have been recognized as potential chemotherapeutic and chemopreventative agents against cancer(s) and infectious diseases. ISC compounds are chemically analogous to their isosteric relatives, isothiocyanates (ITCs); however, they possess increased biological activity, such as enhanced cytotoxicity against cancer cells. ISCs not only serve as significant products, but also as precursors and essential intermediates for a variety of organoselenium compounds, such as selenium-containing heterocycles, which are biologically active. While syntheses of ISCs have become less difficult to accomplish, the syntheses of selenium-containing heterocycles are often difficult due to the use of highly toxic selenium reagents. Because of this, ISCs can serve as versatile reagents for the preparation of these heterocycles. In this review, the classical and recent syntheses of ISCs will be discussed, along with notable and recent synthetic work employing ISCs to access novel selenium-containing heterocycles.1 Introduction1.1 Selenium and Health2 Isoselenocyanates2.1 Preparation of Isoselenocyanates3 Selenium-Containing Heterocycles3.1 Notable Synthetic Work3.2 Recent Synthetic Work3.2.1 Synthesis of N-(3-Methyl-4-phenyl-3H-selenazol-2-ylidene)benzamide­ Derivatives3.2.2 Synthesis and X-ray Studies of Diverse Selenourea Derivatives3.2.3 Synthesis of Heteroarene-Fused [1,2,4]Thiadiazoles/Selenadiazoles via Iodine-Promoted [3+2] Oxidative Cyclization3.2.4 2-Amino-1,3-selenazole Derivatives via Base-Promoted Multicomponent Reactions4 Conclusion

Second-Generation Inhibitors for the Metalloprotease Neprilysin Based on Bicyclic Heteroaromatic Scaffolds: Synthesis, Biological Activity, and X-Ray Crystal-Structure Analysis

2005 ◽  
Vol 88 (4) ◽  
pp. 731-750 ◽  
Author(s):  
Stefan Sahli ◽  
Brian Frank ◽  
W. Bernd Schweizer ◽  
François Diederich ◽  
Denise Blum-Kaelin ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Biological Activity ◽  
Structure Analysis ◽  
Second Generation ◽  
Crystal Structure Analysis ◽  
X Ray

scholarly journals Synthesis of Exosome-Based Fluorescent Gold Nanoclusters for Cellular Imaging Applications

2021 ◽  
Vol 22 (9) ◽  
pp. 4433
Author(s):  
Eun Sung Lee ◽  
Byung Seok Cha ◽  
Seokjoon Kim ◽  
Ki Soo Park
Keyword(s):  
Photoelectron Spectroscopy ◽  
Low Cost ◽  
Stokes Shift ◽  
Gold Nanoclusters ◽  
Human Colon ◽  
Cellular Imaging ◽  
Metal Nanoclusters ◽  
Human Colon Cancer ◽  
X Ray ◽  
High Concentrations

In recent years, fluorescent metal nanoclusters have been used to develop bioimaging and sensing technology. Notably, protein-templated fluorescent gold nanoclusters (AuNCs) are attracting interest due to their excellent fluorescence properties and biocompatibility. Herein, we used an exosome template to synthesize AuNCs in an eco-friendly manner that required neither harsh conditions nor toxic chemicals. Specifically, we used a neutral (pH 7) and alkaline (pH 11.5) pH to synthesize two different exosome-based AuNCs (exo-AuNCs) with independent blue and red emission. Using field-emission scanning electron microscopy, energy dispersive X-ray microanalysis, nanoparticle tracking analysis, and X-ray photoelectron spectroscopy, we demonstrated that AuNCs were successfully formed in the exosomes. Red-emitting exo-AuNCs were found to have a larger Stokes shift and a stronger fluorescence intensity than the blue-emitting exo-AuNCs. Both exo-AuNCs were compatible with MCF-7 (human breast cancer), HeLa (human cervical cancer), and HT29 (human colon cancer) cells, although blue-emitting exo-AuNCs were cytotoxic at high concentrations (≥5 mg/mL). Red-emitting exo-AuNCs successfully stained the nucleus and were compatible with membrane-staining dyes. This is the first study to use exosomes to synthesize fluorescent nanomaterials for cellular imaging applications. As exosomes are naturally produced via secretion from almost all types of cell, the proposed method could serve as a strategy for low-cost production of versatile nanomaterials.

scholarly journals Arsenoplatin-Ferritin Nanocage: Structure and Cytotoxicity

2021 ◽  
Vol 22 (4) ◽  
pp. 1874
Author(s):  
Giarita Ferraro ◽  
Alessandro Pratesi ◽  
Damiano Cirri ◽  
Paola Imbimbo ◽  
Daria Maria Monti ◽  
...  
Keyword(s):  
Biological Activity ◽  
Diffraction Data ◽  
Inductively Coupled Plasma ◽  
Emission Spectroscopy ◽  
Atomic Emission ◽  
Side Chain ◽  
Plasma Atomic Emission ◽  
Average Amount ◽  
X Ray ◽  
Inductively Coupled

Arsenoplatin-1 (AP-1), the prototype of a novel class of metallodrugs containing a PtAs(OH)2 core, was encapsulated within the apoferritin (AFt) nanocage. UV-Vis absorption spectroscopy and inductively coupled plasma-atomic emission spectroscopy measurements confirmed metallodrug encapsulation and allowed us to determine the average amount of AP-1 trapped inside the cage. The X-ray structure of AP-1-encapsulated AFt was solved at 1.50 Å. Diffraction data revealed that an AP-1 fragment coordinates the side chain of a His residue. The biological activity of AP-1-loaded AFt was comparatively tested on a few representative cancer and non-cancer cell lines. Even though the presence of the cage reduces the overall cytotoxicity of AP-1, it improves its selectivity towards cancer cells.

Synthesis of Galactomannan Sulfate-Citrate

2022 ◽  
Vol 1049 ◽  
pp. 218-223
Author(s):  
Aleksandr S. Kazachenko ◽  
Yuriy N. Malyar ◽  
Anna S. Kazachenko
Keyword(s):  
Biological Activity ◽  
Ftir Spectroscopy ◽  
X Ray Diffraction ◽  
Absorption Bands ◽  
X Ray ◽  
Mixed Ester ◽  
First Time ◽  
Derivatives Of

Sulfated derivatives of polysaccharides have anticoagulant, hypolipedimic and other biological activity. In this work, a complex mixed ester of galactomannan, its sulfate-citrate, was obtained for the first time. The introduction of citrate and sulfate groups was proved by FTIR spectroscopy by the appearance of corresponding absorption bands. It was shown by X-ray diffraction that the introduction of the citrate group leads to the amorphization of the galactomannan structure.

Cu(II) Complexes with Heterocyclic Substituted Thiosemicarbazones:  The Case of 5-Formyluracil. Synthesis, Characterization, X-ray Structures, DNA Interaction Studies, and Biological Activity

2003 ◽  
Vol 42 (6) ◽  
pp. 2049-2055 ◽  
Author(s):  
Monica Baldini ◽  
Marisa Belicchi-Ferrari ◽  
Franco Bisceglie ◽  
Giorgio Pelosi ◽  
Silvana Pinelli ◽  
...  
Keyword(s):  
Biological Activity ◽  
Dna Interaction ◽  
X Ray ◽  
Interaction Studies

The X-ray crystal structure and biological activity of 3,5-diisopropylsalicylato Cu(II) complexes

1991 ◽  
Vol 43 (2-3) ◽  
pp. 623
Author(s):  
John D. Ranford ◽  
Peter J. Sadler ◽  
Derek A. Tocher
Keyword(s):  
Crystal Structure ◽  
Biological Activity ◽  
X Ray

Natural and synthetic naphthoquinones as potential anti-infective agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Eyra Ortiz-Pérez ◽  
Karina Vázquez ◽  
Gildardo Rivera ◽  
Cristian O. Salas ◽  
J. José Zarate-Ramos ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Effects ◽  
Plasmodium Falciparum Malaria ◽  
Toxocara Canis ◽  
Chemotherapeutic Agents ◽  
Parasitic Diseases ◽  
Antiprotozoal Activity ◽  
Wide Range ◽  
Leishmania Spp ◽  
Natural And Synthetic

Background: Naphthoquinones are a class of aromatic compounds relevant for their chemical characteristics, structural properties, and biological activity. These compounds are found in nature with a wide range of effects, highlighting their antibacterial, antifungal, and antiprotozoal properties. Additionally, naphthoquinones are used as a scaffold to obtain new derivatives with pharmacological potential, mainly compounds against parasitic diseases. Objective: The purpose of this work was to carry out a comprehensive review of naphthoquinones and their derivatives obtained from both natural and synthetic sources, also, to well as analyze their biological activity against Leishmania spp (Leishmaniasis), Trypanosoma cruzi (Chagas disease), Plasmodium falciparum (Malaria), Toxoplasma gondii (Toxoplasmosis), and Toxocara canis (Toxocariasis). All of these agents are responsible for relevant diseases worldwide. Results : Natural naphthoquinones, such as plumbagin, diospyrin, burmanin, lapachol, lawsone and psychorubrin, show an antiprotozoal activity similar or enhanced antiprotozoal activity to reference drugs. Some naphthoquinones obtained by synthesis or semi-synthesis shown better biological activity or less toxic effects than natural compounds. Conclusion: In this review, natural and synthetic naphthoquinone showed antiparasitic activity, in the most cases with improved results than current drugs currently used in clinical trials. A modification of their structure with different functional groups can enhance their biological effects, improve solubility, and reduce undesirable side effects. Therefore, naphthoquinones are important molecules in the development of new chemotherapeutic agents against parasitic diseases.

Luminescent EuIII and TbIII bimetallic complexes of N,N′-heterocyclic bases and tolfenamic acid: structures, photophysical aspects and biological activity

2020 ◽  
Vol 44 (36) ◽  
pp. 15685-15697
Author(s):  
Zafar Abbas ◽  
Prerana Singh ◽  
Srikanth Dasari ◽  
Sri Sivakumar ◽  
Ashis K. Patra
Keyword(s):  
Biological Activity ◽  
Cellular Imaging ◽  
Tolfenamic Acid ◽  
Bimetallic Complexes ◽  
Bridging Ligands ◽  
Imaging Capability ◽  
Heterocyclic Bases

The isostructural bimetallic luminescent EuIII and TbIII dimers containing N,N′-heterocyclic bases and tolfenamic acid as a bridging ligands were evaluated for their structures, cellular imaging capability and photocytotoxicity.

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