scholarly journals Diarylureas as Antitumor Agents

2021 ◽  
Vol 11 (1) ◽  
pp. 374
Author(s):  
Alessia Catalano ◽  
Domenico Iacopetta ◽  
Maria Stefania Sinicropi ◽  
Carlo Franchini
Keyword(s):  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Anticancer Agent ◽  
Kinase Inhibitors ◽  
Antitumor Agents ◽  
Serine Threonine Kinase ◽  
Threonine Kinase ◽  
The Past ◽  
To Come ◽  
Come Into The Market

The diarylurea is a scaffold of great importance in medicinal chemistry as it is present in numerous heterocyclic compounds with antithrombotic, antimalarial, antibacterial, and anti-inflammatory properties. Some diarylureas, serine-threonine kinase or tyrosine kinase inhibitors, were recently reported in literature. The first to come into the market as an anticancer agent was sorafenib, followed by some others. In this review, we survey progress over the past 10 years in the development of new diarylureas as anticancer agents.

scholarly journals Diarylureas: Repositioning from Antitumor to Antimicrobials or Multi-Target Agents against New Pandemics

Antibiotics ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 92 ◽  
Author(s):  
Alessia Catalano ◽  
Domenico Iacopetta ◽  
Michele Pellegrino ◽  
Stefano Aquaro ◽  
Carlo Franchini ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Kinase Inhibitors ◽  
Viral Infections ◽  
Drug Repositioning ◽  
Biological Activities ◽  
Antiviral Treatment ◽  
Far East ◽  
Mild Disease ◽  
To Come ◽  
The Uk

Antimicrobials have allowed medical advancements over several decades. However, the continuous emergence of antimicrobial resistance restricts efficacy in treating infectious diseases. In this context, the drug repositioning of already known biological active compounds to antimicrobials could represent a useful strategy. In 2002 and 2003, the SARS-CoV pandemic immobilized the Far East regions. However, the drug discovery attempts to study the virus have stopped after the crisis declined. Today’s COVID-19 pandemic could probably have been avoided if those efforts against SARS-CoV had continued. Recently, a new coronavirus variant was identified in the UK. Because of this, the search for safe and potent antimicrobials and antivirals is urgent. Apart from antiviral treatment for severe cases of COVID-19, many patients with mild disease without pneumonia or moderate disease with pneumonia have received different classes of antibiotics. Diarylureas are tyrosine kinase inhibitors well known in the art as anticancer agents, which might be useful tools for a reposition as antimicrobials. The first to come onto the market as anticancer was sorafenib, followed by some other active molecules. For this interesting class of organic compounds antimicrobial, antiviral, antithrombotic, antimalarial, and anti-inflammatory properties have been reported in the literature. These numerous properties make these compounds interesting for a new possible pandemic considering that, as well as for other viral infections also for CoVID-19, a multitarget therapeutic strategy could be favorable. This review is meant to be an overview on diarylureas, focusing on their biological activities, not dwelling on the already known antitumor activity. Quite a lot of papers present in the literature underline and highlight the importance of these molecules as versatile scaffolds for the development of new and promising antimicrobials and multitarget agents against new pandemic events.

Pyridine moiety: An insight into recent advances in treatment of cancer

2021 ◽  
Vol 21 ◽  
Author(s):  
Rakesh Sahu ◽  
Rakhi Mishra ◽  
Rajnish Kumar ◽  
Salahuddin ◽  
Chandana Majee ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Antitumor Agents ◽  
Pyridine Moiety ◽  
Structure Activity ◽  
Wide Range ◽  
Global Health Issue ◽  
Effective Drugs ◽  
Published Research ◽  
Insight Into

: The incidence of cancer is increasing worldwide, affecting a vast majority of the human population. As new different anticancer agents are being developed now, the requirement is to deal somehow with them and evaluate their safety. Among them, pyridine based drugs are contributing a lot, as it is one of the imperative pharmacophores occurring synthetically as well as naturally in heterocyclic compounds, and having a wide range of therapeutic applications in the area of drug discovery, thereby offering many chances for further improvement in antitumor agents via acting onto numerous receptors of extreme prominence. Many pyridine derivatives have been reported to inhibit enzymes, receptors and many other targets for controlling and curing the global health issue of cancer. Nowadays, in combination with other moieties, researchers are focusing on the development of pyridine-based new derivatives for cancer treatment. Therefore, this review sheds light on the recent therapeutic expansions of pyridine together with its molecular docking, structure-activity-relationship, availability in the market, and a summary of recently patented and published research works that shall jointly help the scientists to produce effective drugs with the desired pharmacological activity.

scholarly journals ROLE OF SERIN/ THREONINE KINASE INHIBITOR IN THERAPY NON-ALCOHOLIC STEATOHEPATITIS AND ALCOHOLIC HEPATITIS

2019 ◽  
Vol 6 (3) ◽  
pp. 101-109
Author(s):  
Novriantika Lestari
Keyword(s):  
Signal Transduction ◽  
Liver Fibrosis ◽  
Kinase Inhibitors ◽  
Kinase Inhibitor ◽  
Binding Activity ◽  
Serine Threonine Kinase ◽  
Threonine Kinase ◽  
Receptor Binding Activity ◽  
Marked Accumulation

Liver fibrosis is a reversible response to a wound healing with marked accumulation of extracellular matrix which caused by injury to the liver. Liver fibrosis can be caused by various factors including alcohol and non-alcohol steatohepatitis. The process of fibrosis serves to localize the inflammation during chronic exposure. The hepatic stem cell (HSC) has a key role in the pathogenesis of liver fibrosis. The HSC activation is characterized by increased profibrogenic mediators including members of the TGF-? superfamily. In order to enable signal transduction, the mediator needs to bind to its receptors. The serine/ threonine kinase receptor is a receptor that binds to the TGF-? superfamily ligand, including TGF-?, BMP, activin and other mediators. The ligand receptor-binding activity will stimulate signal transduction that will translocate into the nucleus and phosphorylate various transcription factors that play a role in cell proliferation, differentiation, or apoptosis. There is currently no standard therapy for liver fibrosis. Based on the central role of the serine/ threonine kinase receptor in the pathogenesis of liver fibrosis, it is thought that the use of serine/ threonine kinase inhibitors is a promising therapy.

Recent Progress on Apoptotic Activity of Triazoles

2021 ◽  
Vol 22 ◽  
Author(s):  
Pelin Çıkla-Süzgün ◽  
Ş. Güniz Küçükgüzel
Keyword(s):  
Cancer Progression ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Rational Design ◽  
Vital Role ◽  
Anticancer Activities ◽  
The Past ◽  
Small Molecule Drugs ◽  
Apoptotic Activity ◽  
New Generation

Abstract: Apoptosis, often called programmed cell death, is a self-directed cell destruction process. It differs from classical necrosis by activation of caspases. Apoptosis is directly related to cancer progression and plays a vital role in carcinogenesis. All cytotoxic drugs and radiation therapy programs initiates apoptosis in tumor cells. Today, studies show that heterocyclic compounds that contain triazole funtionality have anticancer activities. Triazoles are 5-membered rings, which contain two carbon and three nitrogen atoms Therefore, many researchers have synthesized these small active compounds as target structures and evaluated their apoptotic activities. The present review describs more recent medicinal aspects of triazoles as anticancer agents reported during the past few years. We hope that the bioactivity of triazole derivatives will be beneficial for the rational design of new generation of small molecule drugs.

scholarly journals Schiff Base Metal Complexes as Anticancer Agents

2019 ◽  
Vol 31 (3) ◽  
pp. 493-504 ◽  
Author(s):  
G. Sridevi ◽  
S. Arul Antony ◽  
R. Angayarkani
Keyword(s):  
Schiff Base ◽  
Anticancer Agents ◽  
Anticancer Agent ◽  
Antitumor Agents ◽  
Transition Metal Complex ◽  
Bioinorganic Chemistry ◽  
Structural Data ◽  
Ligand Substitution ◽  
Schiff Base Metal Complexes

Cutting-edge practices in bioinorganic chemistry are pivotal for enhancing the layout of compounds to lessen poisonous facet effect and recognize their mechanism of action. A powerful anticancer agent should own inherent, inhibitory property and also delivery, dosage and residence time in vivo. Organic function and conformation of mutated gene may be altered by way of binding of metal ions. Upswing of activities counting on the structural data, intending in enhancing and growing different forms of metal based compounds, continuous seek of extra metal based compounds have been synthesized via revamping the prevailing chemical shape via ligand substitution. The prevailing paper addresses the trendy development in the design of novel antitumor agents primarily based on transition metal complex via highlighting the near dating among their structural alternatives and cytotoxic ability.

Breaking the DNA Damage Response via Serine/Threonine Kinase Inhibitors to Improve Cancer Treatment

2019 ◽  
Vol 26 (8) ◽  
pp. 1425-1445 ◽  
Author(s):  
Wioletta Rozpędek ◽  
Dariusz Pytel ◽  
Alicja Nowak-Zduńczyk ◽  
Dawid Lewko ◽  
Radosław Wojtczak ◽  
...  
Keyword(s):  
Dna Damage ◽  
Dna Replication ◽  
Cancer Treatment ◽  
Dna Damage Response ◽  
Ataxia Telangiectasia ◽  
Kinase Inhibitors ◽  
Serine Threonine Kinase ◽  
Threonine Kinase ◽  
Anti Cancer ◽  
Damage Response

Multiple, both endogenous and exogenous, sources may induce DNA damage and DNA replication stress. Cells have developed DNA damage response (DDR) signaling pathways to maintain genomic stability and effectively detect and repair DNA lesions. Serine/ threonine kinases such as Ataxia-telangiectasia mutated (ATM) and Ataxia-telangiectasia and Rad3-Related (ATR) are the major regulators of DDR, since after sensing stalled DNA replication forks, DNA double- or single-strand breaks, may directly phosphorylate and activate their downstream targets, that play a key role in DNA repair, cell cycle arrest and apoptotic cell death. Interestingly, key components of DDR signaling networks may constitute an attractive target for anti-cancer therapy through two distinct potential approaches: as chemoand radiosensitizers to enhance the effectiveness of currently used genotoxic treatment or as single agents to exploit defects in DDR in cancer cells via synthetic lethal approach. Moreover, the newest data reported that serine/threonine protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is also closely associated with cancer development and progression. Thereby, utilization of small-molecule, serine/threonine kinase inhibitors may provide a novel, groundbreaking, anti-cancer treatment strategy. Currently, a range of potent, highlyselective toward ATM, ATR and PERK inhibitors has been discovered, but after foregoing study, additional investigations are necessary for their future clinical use.

Sign in / Sign up

Export Citation Format

Share Document