Facile design of thio-perylenediimides with controllable fluorescent, photodynamic and photothermal effects towards cancer theranostics

2021 ◽  
Author(s):  
Chang Liu ◽  
Chendong Ji ◽  
Zongyang Fan ◽  
Ruihao Ma ◽  
Meizhen Yin

A series of thionated perylenediimides with modulating phototheranostic modalities have been synthesized by one-pot method for multiple anti-cancer applications. Compared to the initial and 4-tert-butyl phenol-substituted fluorescent perylenediimide, the obtained...

RSC Advances ◽  
2016 ◽  
Vol 6 (35) ◽  
pp. 29757-29768 ◽  
Author(s):  
Raja Modhugoor Devendiran ◽  
Senthil kumar Chinnaiyan ◽  
Narra Kishore Yadav ◽  
Ganesh Kumar Moorthy ◽  
Giriprasath Ramanathan ◽  
...  

The one pot aqueous green synthesis of gold nanoparticles (GNPs) decorated with folic acid and loaded with doxorubicin suitable for anti-cancer drug delivery was potentially promising as a new therapeutic system for cancer treatment.


2020 ◽  
Vol 20 (11) ◽  
pp. 1340-1351 ◽  
Author(s):  
Ponnurengam M. Sivakumar ◽  
Matin Islami ◽  
Ali Zarrabi ◽  
Arezoo Khosravi ◽  
Shohreh Peimanfard

Background and objective: Graphene-based nanomaterials have received increasing attention due to their unique physical-chemical properties including two-dimensional planar structure, large surface area, chemical and mechanical stability, superconductivity and good biocompatibility. On the other hand, graphene-based nanomaterials have been explored as theranostics agents, the combination of therapeutics and diagnostics. In recent years, grafting hydrophilic polymer moieties have been introduced as an efficient approach to improve the properties of graphene-based nanomaterials and obtain new nanoassemblies for cancer therapy. Methods and results: This review would illustrate biodistribution, cellular uptake and toxicity of polymergraphene nanoassemblies and summarize part of successes achieved in cancer treatment using such nanoassemblies. Conclusion: The observations showed successful targeting functionality of the polymer-GO conjugations and demonstrated a reduction of the side effects of anti-cancer drugs for normal tissues.


2019 ◽  
Vol 19 (2) ◽  
pp. 265-275 ◽  
Author(s):  
Faeze Khalili ◽  
Sara Akrami ◽  
Malihe Safavi ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Mina Saeedi ◽  
...  

Background: This paper reports synthesis, cytotoxic activity, and apoptosis inducing effect of a novel series of styrylimidazo[1,2-a]pyridine derivatives. Objective: In this study, anti-cancer activity of novel styrylimidazo[1,2-a]pyridines was evaluated. Methods: Styrylimidazo[1,2-a]pyridine derivatives 4a-o were synthesized through a one-pot three-component reaction of 2-aminopyridines, cinnamaldehydes, and isocyanides in high yield. All synthesized compounds 4a-o were evaluated against breast cancer cell lines including MDA-MB-231, MCF-7, and T-47D using MTT assay. Apoptosis was evaluated by acridine orange/ethidium bromide staining, cell cycle analysis, and TUNEL assay as the mechanism of cell death. Results: Most of the synthesized compounds exhibited more potent cytotoxicity than standard drug, etoposide. Induction of apoptosis by the most cytotoxic compounds 4f, 4g, 4j, 4n, and 4m was confirmed through mentioned methods. Conclusion: In conclusion, these results confirmed the potency of styrylimidazo[1,2-a]pyridines for further drug discovery developments in the field of anti-cancer agents.


2021 ◽  
Author(s):  
Goutam Brahmachari ◽  
Indrajit Karmakar ◽  
Pintu Karmakar

A one-pot procedure for the synthesis of biologically relevant coumarin-hydrazones by a three-component reaction between 4-hydrocoumarins, primary aromatic amines and tert-butyl nitrite under ball-milling in the absence of any catalyst/additive...


1999 ◽  
Vol 23 (6) ◽  
pp. 368-369
Author(s):  
Issa Yavari ◽  
Abbas Ali Esmaili ◽  
Sakineh Asghari ◽  
Hamid Reza Bijanzadeh

The highly reactive 1:1 intermediate produced in the reaction between tert-butyl isocyanide and dialkyl acetylenedicarboxylates is trapped by dialkyl 2-bromomalonates to yield the title compounds in fairly high yields.


2021 ◽  
pp. 174751982098753
Author(s):  
Xiaofang Wu ◽  
Lei Zhou ◽  
Fangshao Li ◽  
Jing Xiao

A PCl3-mediated conversion of tert-butyl esters into esters and amides in one-pot under air is developed. This novel protocol is highlighted by the synthesis of skeletons of bioactive molecules and gram-scale reactions. Mechanistic studies revealed that this transformation involves the formation of an acid chloride in situ, which is followed by reactions with alcohols or amines to afford the desired products.


2015 ◽  
Vol 51 (68) ◽  
pp. 13309-13312 ◽  
Author(s):  
Shao-Jen Wang ◽  
Yung-Te Hou ◽  
Lin-Chi Chen

A novel selective decoy oligodeoxynucleotide (dODN)–doxorubicin (DOX) complex is reported for cancer theranostics.


2021 ◽  
Author(s):  
Sameh Rizk ◽  
Mohamed Megahed ◽  
Monda Badawy ◽  
Mohamed Aly

Abstract New anticancer agents are highly needed to overcome cancer cell resistance. Synthesis of newly pyrazole, derivatives via heterocyclic ring opening of azacoumarin promoted with grinding and ultrasonic reaction conditions. Efficient solvent less one pot synthesis can be well progressed to afford the good yield of new heterocyclic products that were characterized by IR, 1H-NMR, MS and micro-analytical data. Anticancer evaluation for the synthesized compounds exhibited good cytotoxiciy. The anti-liver cancer activity of all compounds was screened in vitro against hepatocellular carcinoma (HCC) cell lines (HepG-2) by viability assay. The synthesized compounds were evaluated for their anticancer activity and found to exhibit promising activities. All new compounds were tested for possible anti-cancer activity against HepG-2 cell lines in comparison to the reference drug doxorubicin (DOX). Compound 8 was the most active against the liver carcinoma cell line (HepG-2) giving promising half-maximal inhibitory concentration (IC50) value of 27.5 ± 1.3 μg/mL, compared with DOX with IC50 value of 0.36 ± 0.02 μg/mL. However it has weak cytotoxic effects against normal rat hepatocytes with 50% cytotoxic concentration (CC50) = 1820.5 µg/ml (= > 500 µg/ml). Compound 8 was selected to be tested in combination with ionizing gamma radiation. Gene expression levels of the cell cycle inhibitor p21 and caspase-3 was quantified. As well as, Oxidative stress was quantified by measuring the concentration of malondialdehyde (MDA), and antioxidant activity of reduced gluthatione (GSH). This study concluded that the new derivative of the azacomarin compound has an effective anti-cancer effect and it was found that using the new compound with ionizing radiation at a dose of 8 Gy improves the effectiveness of the compound on liver cancer cells.


ChemInform ◽  
2010 ◽  
Vol 29 (1) ◽  
pp. no-no
Author(s):  
G. BARBARO ◽  
A. BATTAGLIA ◽  
A. GUERRINI ◽  
C. BERTUCCI
Keyword(s):  
One Pot ◽  

2020 ◽  
Author(s):  
Barbara Souza ◽  
Jin-Chong Tan

We report two solvent-free mechanochemical methods to achieve one‑pot encapsulation of anti-cancer drug 5‑Fluorouracil (5‑FU) in the iron-based MIL‑100 metal-organic framework (MOF). We compare the structural and physicochemical properties of drug@MIL‑100 systems derived from <i>in situ </i>manual and vortex grinding, where the former exhibits a slower drug release due to stronger guest-host interactions.


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