scholarly journals Green Synthesis of New Pyrrolo [1,2-a] quinoxalines as Antiproliferative Agents in GPER-expressing Breast Cancer Cells

2021 ◽  
Vol 2021 ◽  
pp. 1-8
Author(s):  
Gabriele Carullo ◽  
Sarah Mazzotta ◽  
Francesca Giordano ◽  
Francesca Aiello
Keyword(s):  
Anticancer Agents ◽  
Biological Properties ◽  
Antiproliferative Agents ◽  
Antiproliferative Effects ◽  
Anticancer Properties ◽  
Small Set ◽  
Acetyl Group ◽  
High Yields ◽  
Short Time

4,5-Dihydropyrrolo [1,2-a]quinoxalines are interesting druggable scaffolds, with multifaceted biological properties, including anticancer properties targeting the G protein-coupled estrogen receptor 1 (GPER). In this work, the synthesis and preliminary antiproliferative activity of a small set of new 4,5-dihydropyrrolo[1,2-a]quinoxalines (18-20) and pyrrolo[1,2-a]quinoxalines (21, 22) has been reported, inspired by known antiproliferative agents (G-1, G-15, and G-36). The synthesis of the pyrroloquinoxalinic core was employed following the Pictet–Spengler reaction, using the surfactant p-dodecylbenzene sulphonic acid (p-DBSA), as catalyst. It demonstrated efficiency in the catalysis of the 4-phenylpyrrole [1,2-a] quinoxaline type compound formation in mild solvents such as water, ethanol, and hydroalcoholic solutions. In addition, the reactions proceeded in a short time (between 15 and 120 minutes) at room temperature and with high yields. The in vitro MTT assays showed that the presence of isopropyl groups furnished promising antiproliferative compounds. Although, the acetyl group provided also antiproliferative effects, breaking down its responsibility in the GPER transactivation. Nevertheless, it is possible to conclude that the 4,5-dihydropyrrolo[1,2-a]quinoxalines remain a feasible scaffold to develop anticancer agents against GPER-expressing cells.

The Molecular Diversity Scope of Urazole in the Synthesis of Organic Compounds

2019 ◽  
Vol 16 (7) ◽  
pp. 953-967 ◽  
Author(s):  
Ghodsi M. Ziarani ◽  
Fatemeh Mohajer ◽  
Razieh Moradi ◽  
Parisa Mofatehnia
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Microtubule Assembly ◽  
Heterocyclic Molecules ◽  
Biological Perspective ◽  
Highly Active ◽  
Anti Inflammatory ◽  
High Yields ◽  
Short Time

Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

Development of Natural Bioactive Alkaloids: Anticancer perspective

2021 ◽  
Vol 21 ◽  
Author(s):  
Ashish Patel ◽  
Ravi Vanecha ◽  
Jay Patel ◽  
Divy Patel ◽  
Umang Shah ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Low Cost ◽  
Chemical Compounds ◽  
Cost Effective ◽  
Drug Discovery And Development ◽  
Anticancer Properties ◽  
Antimetastatic Activity ◽  
New Chemical Entities

: Cancer is a frightful disease that still poses a 'nightmare' worldwide, causing millions of casualties annually due to one of the human race's most significant healthcare challenges that requires a pragmatic treatment strategy. However, plants and plant-derived products revolutionize the field as they are quick, cleaner, eco-friendly, low-cost, effective, and less toxic than conventional treatment methods. Plants are repositories for new chemical entities and have a promising cancer research path, supplying 60% of the anticancer agents currently used. Alkaloids are important chemical compounds that serve as a rich reservoir for drug discovery and development. However, some alkaloids derived from natural herbs display anti-proliferation and antimetastatic activity on different forms of cancer, both in vitro and in vivo. Alkaloids have also been widely formulated as anticancer medications, such as camptothecin and vinblastine. Still, more research and clinical trials are required before final recommendations can be made on specific alkaloids. This review focuses on the naturally-derived bioactive alkaloids with prospective anticancer properties based on the information in the literature.

scholarly journals Effect of Roasting and Brewing on the Antioxidant and Antiproliferative Activities of Tartary Buckwheat

Foods ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 1331
Author(s):  
Ji-yeon Ryu ◽  
Yoonseong Choi ◽  
Kun-Hwa Hong ◽  
Yong Suk Chung ◽  
Somi Kim Cho
Keyword(s):  
Breast Cancer Cells ◽  
Room Temperature ◽  
Tartary Buckwheat ◽  
Flavonoid Content ◽  
Total Polyphenol ◽  
Antiproliferative Effects ◽  
Long Time ◽  
Short Time ◽  
Antiproliferative Activities

We evaluated the effect of the roasting and brewing conditions of Tartary buckwheat (TB), which is widely used in infusion teas, on its antioxidant and antiproliferative activities in vitro. TB was roasted at 210 °C for 10 min and brewed at a high temperature for a short time (HTST; 85–90 °C, 3 min) or at room temperature for a long time (RTLT; 25–30 °C, 24 h). Roasted TB (RTB) tea brewed at RTLT had the highest total polyphenol content (TPC) and total flavonoid content (TFC) among the four TB teas for different roasting and brewing conditions. Moreover, RTB brewed at RTLT showed the greatest 2,2-diphenyl-1-picrylhydrazyl-, 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)-, and alkyl-scavenging activities. The TB tea brewed at RTLT had higher Fe2+-chelating activity than that brewed at HTST, irrespective of roasting. Moreover, RTB tea brewed at RTLT inhibited the proliferation of human pancreatic and breast cancer cells. Overall, RTB-RTLT displayed the largest effect on antioxidant and antiproliferative effects. Finally, rutin was found to possess the most pronounced effect on the antioxidant and antiproliferative activities of the TB teas. These results indicate that the antioxidant and antiproliferative activities of RTB are enhanced by RTLT brewing.

scholarly journals An Ethanolic Extract of Boehmeria caudata Aerial Parts Displays Anti-inflammatory and Anti-tumor Activities

2020 ◽  
Vol 7 (01) ◽  
pp. e17-e25 ◽  
Author(s):  
Paula Pereira de Paiva ◽  
Fabiana Regina Nonato ◽  
Ana Lúcia Tasca Gois Ruiz ◽  
Ilza Maria de Oliveira Sousa ◽  
Rafael Rosolen Teixeira Zafred ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Ethanolic Extract ◽  
Experimental Models ◽  
New Drugs ◽  
Antiproliferative Effects ◽  
Aerial Parts ◽  
Anti Inflammatory ◽  
Inflammatory Action ◽  
Effective Source

AbstractThe tumor microenvironment presents several therapeutic targets, with inflammation being one of them. In search of new drugs, plants have shown to be an effective source of potent anti-inflammatory and anticancer agents. This study aimed to evaluate the antitumoral and inflammatory activities of Boehmeria caudata aerial parts extract. Bioguided in vitro antiproliferative screening showed that phenanthroquinolizidine obtained from the aerial B. caudata ethanolic extract had a straight relationship with activity. Moreover, the orally administered ethanolic extract reduced Ehrlich solid tumor growth and displayed an anti-inflammatory effect in both evaluated experimental models (carrageenan-induced paw edema and croton oil-induced ear edema). These results suggest that the antitumor activity of the ethanolic extract could be explained by antiproliferative effects associated with anti-inflammatory action.

Mushroom small RNAs as potential anticancer agents: a closer look at Cantharellus cibarius proapoptotic and antiproliferative effects in colon cancer cells

2019 ◽  
Vol 10 (5) ◽  
pp. 2739-2751 ◽  
Author(s):  
Marta K. Lemieszek ◽  
Patrícia S. Marques ◽  
Miguel Ribeiro ◽  
Daniela Ferreira ◽  
Guilhermina Marques ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Small Rnas ◽  
Colon Cancer Cells ◽  
Antiproliferative Effects ◽  
Anticancer Properties

Screening aimed at the evaluation of the presence of small RNAs with anticancer properties in Boletus spretus, B. pinophilus and Cantharellus cibarius, was conducted.

scholarly journals Anticancer Ruthenium(III) Complexes and Ru(III)-Containing Nanoformulations: An Update on the Mechanism of Action and Biological Activity

2019 ◽  
Vol 12 (4) ◽  
pp. 146 ◽  
Author(s):  
Claudia Riccardi ◽  
Domenica Musumeci ◽  
Marco Trifuoggi ◽  
Carlo Irace ◽  
Luigi Paduano ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Anticancer Agents ◽  
Biomedical Applications ◽  
Special Focus ◽  
Anticancer Properties ◽  
Pharmacokinetic Properties ◽  
Pharmacological Potential

The great advances in the studies on metal complexes for the treatment of different cancer forms, starting from the pioneering works on platinum derivatives, have fostered an increasingly growing interest in their properties and biomedical applications. Among the various metal-containing drugs investigated thus far, ruthenium(III) complexes have emerged for their selective cytotoxic activity in vitro and promising anticancer properties in vivo, also leading to a few candidates in advanced clinical trials. Aiming at addressing the solubility, stability and cellular uptake issues of low molecular weight Ru(III)-based compounds, some research groups have proposed the development of suitable drug delivery systems (e.g., taking advantage of nanoparticles, liposomes, etc.) able to enhance their activity compared to the naked drugs. This review highlights the unique role of Ru(III) complexes in the current panorama of anticancer agents, with particular emphasis on Ru-containing nanoformulations based on the incorporation of the Ru(III) complexes into suitable nanocarriers in order to enhance their bioavailability and pharmacokinetic properties. Preclinical evaluation of these nanoaggregates is discussed with a special focus on the investigation of their mechanism of action at a molecular level, highlighting their pharmacological potential in tumour disease models and value for biomedical applications.

scholarly journals Anticancer Properties and Mechanism of Action of Oblongifolin C, Guttiferone K and Related Polyprenylated Acylphloroglucinols

2021 ◽  
Author(s):  
Christian Bailly ◽  
Gérard Vergoten
Keyword(s):  
Mechanism Of Action ◽  
Biological Properties ◽  
Structural Basis ◽  
Anticancer Activities ◽  
Potent Inducer ◽  
Anticancer Properties ◽  
Potential Development ◽  
Tumor Growth And Metastasis

AbstractPolyprenylated acylphloroglucinols represent an important class of natural products found in many plants. Among them, the two related products oblongifolin C (Ob-C) and guttiferone K (Gt-K) isolated from Garcinia species (notably from edible fruits), have attracted attention due to their marked anticancer properties. The two compounds only differ by the nature of the C-6 side chain, prenyl (Gt-K) or geranyl (Ob-C) on the phloroglucinol core. Their origin, method of extraction and biological properties are presented here, with a focus on the targets and pathways implicated in their anticancer activities. Both compounds markedly reduce cancer cell proliferation in vitro, as well as tumor growth and metastasis in vivo. They are both potent inducer of tumor cell apoptosis, and regulation of autophagy flux is a hallmark of their mode of action. The distinct mechanism leading to autophagosome accumulation in cells and the implicated molecular targets are discussed. The specific role of the chaperone protein HSPA8, known to interact with Ob-C, is addressed. Molecular models of Gt-K and Ob-C bound to HSPA8 provide a structural basis to their common HSPA8-binding recognition capacity. The review shed light on the mechanism of action of these compounds, to encourage their studies and potential development.

scholarly journals Anticancer Effects of Novel Tetrahydro-Dimethyl-Xanthene-Diones

2020 ◽  
Vol 20 (7) ◽  
pp. 909-916
Author(s):  
Alagumuthu Manikandan ◽  
Arumugam Sivakumar ◽  
Poonam S. Nigam ◽  
Ayyakannu A. Napoleon
Keyword(s):  
Mtt Assay ◽  
Anticancer Agents ◽  
Antioxidant Properties ◽  
Drug Efficacy ◽  
Anticancer Properties ◽  
Anticancer Effects ◽  
Xanthene Derivatives ◽  
Cancer Types ◽  
In Silico Molecular Docking

Background: The derivatives of xanthene are known to have promising anticancer properties, in comparison to xanthene itself. Objective: The object of our study was to develop few xanthene derivatives (a family of fifteen novel 3,4,6,7- tetrahydro-3,3-dimethyl-9-phenyl-2H-xanthene-1,8(5H, 9H)-diones encoded as 4a-4m), which were effectively prepared through regioselective synthesis approach, and to test their anticancer effects. Methods: A series of cell lines were used in this study, first to assess the cytotoxicity and then the drug efficacy of target compounds, consecutively. Prior to MTT assay, the compounds were analysed for their antioxidant properties, since oxidative stress is an important factor in the development of many cancer types. The anticancer properties of 4a-m have been assessed over in silico (molecular docking and ADMET assessments) and in vitro (MTT assay) methods. Results: Compounds 4h and 4i showed a relative percentage anticancer activity of 86.25±1.25 & 89.74±1.64 against BT474 (ER+HER2+), and 90.56±1.18 & 93.24±1.80 against MCF-7 (ER-HER2), respectively. Conclusion: The animal model and pre-clinical studies for 4h and 4i should be performed in order to develop them as future anticancer agents.

Advances on Quinazoline Based Congeners for Anticancer Potential

2021 ◽  
Vol 25 ◽  
Author(s):  
Parul Grover ◽  
Monika Bhardwaj ◽  
Garima Kapoor ◽  
Lovekesh Mehta ◽  
Roma Ghai ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Anticancer Compounds ◽  
In Vivo Models ◽  
Appropriate Treatment

: The heterocyclic compounds have a great significance in medicinal chemistry because they have extensive biological activities. Cancer is globally the leading cause of death and it is a challenge to develop an appropriate treatment for the management of cancer. Continuous efforts are being made to find a suitable medicinal agent for cancer therapy. Nitrogen-containing heterocycles have received noteworthy attention due to their wide and distinctive pharmacological activities. One of the most important nitrogen-containing heterocycles in medicinal chemistry is ‘quinazoline’ that possesses a wide spectrum of biological properties. This scaffold is an important pharmacophore and is considered a privileged structure. The various substituted quinazolines displayed anticancer activity against different types of cancer. This review highlights the recent advances in quinazoline based molecules as anticancer agents. Several in-vitro and in-vivo models used along with the results are also included. A subpart briefing natural quinazoline containing anticancer compounds is also incorporated in the review.

scholarly journals Design, Synthesis and Potential Anti-Proliferative Activity of Some Novel 4-Aminoquinoline Derivatives

2014 ◽  
Vol 64 (3) ◽  
pp. 285-297 ◽  
Author(s):  
Mostafa M. Ghorab ◽  
Mansour S. Al-Said ◽  
Reem K. Arafa
Keyword(s):  
Anticancer Agents ◽  
Proliferative Activity ◽  
Cancer Cell Line ◽  
The Novel ◽  
Design Synthesis ◽  
Reference Drug ◽  
Antiproliferative Agents ◽  
New Compounds ◽  
Mcf 7

Abstract Novel nineteen compounds based on a 4-aminoquinoline scaffold were designed and synthesized as potential antiproliferative agents. The new compounds were N-substituted at the 4-position by aryl or heteroaryl (1-9), quinolin- 3-yl (10), 2-methylquinolin-3-yl (11), thiazol-2-yl (12), and dapsone moieties (13, 14 and 18). Bis-compounds 15, 16 and 19 were also synthesized to assess their biological activity. All the newly synthesized comounds were tested for in vitro antiproliferative activity against the MCF-7 breast cancer cell line. Seventeen of the novel compounds showed higher activity than the reference drug doxorubicin. The corresponding 7-(trifluoromethyl)-N-(3,4,5-trimethoxyphenyl)quinolin-4- amine 1, N-(7-(trifluoromethyl)quinolin-4-yl)quinolin- 3- amine (10), 2-methyl-N-(7-trifluorome-thyl)quinolin-4-yl) quinolin-3-amine (11) and N-(4-(4-aminophenylsulfonyl) phenyl)-7-chloroquinolin-4-amine (13) were almost twice to thrice as potent as doxorubicin. Biological screening of the tested compounds could offer an encouraging framework in this field that may lead to the discovery of potent anticancer agents.

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