Thiazole in the targeted anticancer drug discovery

2019 ◽  
Vol 11 (15) ◽  
pp. 1929-1952 ◽  
Author(s):  
Adileh Ayati ◽  
Saeed Emami ◽  
Setareh Moghimi ◽  
Alireza Foroumadi
Keyword(s):  
Drug Discovery ◽  
Cancer Therapy ◽  
Mechanism Of Action ◽  
Anticancer Agents ◽  
Causes Of Death ◽  
Structure Activity ◽  
The World ◽  
Cancerous Cells ◽  
Potential Use ◽  
Anticancer Drug Discovery

Cancer is known as one of the main causes of death in the world; and many compounds have been synthesized to date with potential use in cancer therapy. Thiazole is a versatile heterocycle, found in the structure of many drugs in use as well as anticancer agents. This review provides an overview of recent advances in thiazole-bearing compounds as anticancer agents with particular emphasis on their mechanism of action in cancerous cells. Chemical designs, structure–activity relationships and relevant preclinical properties have been comprehensively described.

Recent Development of Sulfonyl or Sulfonamide Hybrids as Potential Anticancer Agents: A Key Review

2018 ◽  
Vol 18 (4) ◽  
pp. 488-505 ◽  
Author(s):  
K. P. Rakesh ◽  
Shi-Meng Wang ◽  
Jing Leng ◽  
L. Ravindar ◽  
Abdullah M. Asiri ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Anticancer Agents ◽  
Side Effect ◽  
Docking Studies ◽  
Multi Drug Resistance ◽  
Anticancer Activities ◽  
Pharmacological Activities ◽  
Synthetic Compounds ◽  
Structure Activity ◽  
Anticancer Drug Discovery

Cancer is the second leading cause of death worldwide. There is always a huge demand for novel anticancer drugs and diverse new natural or synthetic compounds are developed continuously by scientists. Presently, a large number of drugs in clinical practice have showed pervasive side effect and multidrug resistance. Sulfonyl or sulfonamide hybrids became one of the most attractive subjects due to their broad spectrum of pharmacological activities. Sulfonyl hybrids were broadly explored for their anticancer activities and it was found that they possess minimum side effect along with multi-drug resistance activity. This review describes the most recent applications of sulfonyl hybrid analogues in anticancer drug discovery and further discusses the mechanistic insights, structure-activity relationships and molecular docking studies for the potent derivatives.

Kernel Methods in Chemoinformatics

2011 ◽  
pp. 664-668
Author(s):  
Huma Lodhi
Keyword(s):  
Developing Countries ◽  
Drug Discovery ◽  
Drug Design ◽  
Kernel Methods ◽  
Cost Effective ◽  
Activity Relationship ◽  
World Population ◽  
Structure Activity ◽  
The World ◽  
Effective Drugs

Millions of people are suffering from fatal diseases such as cancer, AIDS, and many other bacterial and viral illnesses. The key issue is now how to design lifesaving and cost-effective drugs so that the diseases can be cured and prevented. It would also enable the provision of medicines in developing countries, where approximately 80% of the world population lives. Drug design is a discipline of extreme importance in chemoinformatics. Structure-activity relationship (SAR) and quantitative SAR (QSAR) are key drug discovery tasks.

scholarly journals Chemistry and pharmacological diversity of quinoxaline motifs as anticancer agents

2019 ◽  
Vol 69 (2) ◽  
pp. 177-196 ◽  
Author(s):  
Olayinka O. Ajani ◽  
Martins T. Nlebemuo ◽  
Joseph A. Adekoya ◽  
Kehinde O. Ogunniran ◽  
Tolutope O. Siyanbola ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Drug Discovery ◽  
Cell Growth ◽  
Anticancer Agents ◽  
Fast Rate ◽  
Heart Diseases ◽  
The World ◽  
Cell Growth And Proliferation ◽  
Anticancer Drug Development ◽  
Novel Therapeutic

Abstract Surpassing heart diseases, cancer is taking the lead as the deadliest disease because of its fast rate of spreading in all parts of the world. Tireless commitment to searching for novel therapeutic medicines is a worthwhile adventure in synthetic chemistry because of the drug resistance predicament and regular outbreak of new diseases due to abnormal cell growth and proliferation. Medicinal chemistry researchers and pharmacists have unveiled quinoxaline templates as precursors of importance and valuable intermediates in drug discovery because they have been established to possess diverse pharmacological potentials. Hence, this review highlights the current versatile routes to accessing functionalized quinoxaline motifs and harnessing their documented therapeutic potentials for anticancer drug development.

scholarly journals Repurposing Interleukin-6 Inhibitors to Combat COVID-19

2020 ◽  
Vol 3 (2) ◽  
pp. 52-55
Author(s):  
Shumei Kato ◽  
Razelle Kurzrock
Keyword(s):  
Acute Respiratory Distress Syndrome ◽  
Severe Acute Respiratory Syndrome ◽  
Interleukin 6 ◽  
Causes Of Death ◽  
Distress Syndrome ◽  
Cytokine Storm ◽  
Novel Treatment ◽  
The Us ◽  
The World ◽  
Potential Use

ABSTRACT Severe acute respiratory syndrome-coronavirus-2 (SARS-CoV-2) is a pandemic with major implications across the world. One of the most frequent causes of death from SARS-CoV-2 is fatal pneumonia from coronavirus disease 2019 (COVID-19), which is associated with the development of acute respiratory distress syndrome (ARDS). To date (as of April 2, 2020), other than supportive measures, there are no efficient therapeutic options for COVID-19–related ARDS, although the US Food and Drug Administration recently granted emergency authorization for the use of hydroxychoroquine/chloroquine for this indication (which is usually given with azithromycin). Although the pathogenesis for ARDS is under investigation, one of the major culprits is considered to be cytokine storm, especially from interleukin 6 (IL-6) release. Herein, we review potential use of IL-6 inhibitors, several of which are approved for other disease conditions, as potential novel treatment for the management of COVID-19–related ARDS.

Pyrrolo[2,1-a]isoquinoline scaffold in drug discovery: advances in synthesis and medicinal chemistry

2019 ◽  
Vol 11 (20) ◽  
pp. 2735-2755 ◽  
Author(s):  
Maria D Matveeva ◽  
Rosa Purgatorio ◽  
Leonid G Voskressensky ◽  
Cosimo D Altomare
Keyword(s):  
Multidrug Resistance ◽  
Drug Discovery ◽  
Tumor Cells ◽  
Mechanism Of Action ◽  
Biological Activities ◽  
Antitumor Drugs ◽  
Antitumor Activities ◽  
Structure Activity ◽  
Synthetic Approaches ◽  
Potential Exploitation

Pyrrolo[2,1- a]isoquinoline (PIq) is a nitrogen heterocyclic scaffold of diverse alkaloids endowed with several biological activities, including antiretroviral and antitumor activities. Several 5,6-dihydro-PIq (DHPIq) alkaloids, belonging to the lamellarins’ family, have proved to be cytotoxic to tumor cells, as well as reversers of multidrug resistance. In this review, we provide an overview of the main achievements over the last decade in the synthetic approaches to access libraries of PIq compounds along with a survey, as comprehensive as possible, of bioactivity, mechanism of action, pharmacophore and structure–activity relationships of synthetic analogs of DHPIq-based alkaloids. The focus is mainly on the potential exploitation of the (DH)PIq scaffold in design and development of novel antitumor drugs.

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