scholarly journals Evaluation of Substituted Pyrazole-Based Kinase Inhibitors in One Decade (2011–2020): Current Status and Future Prospects

Molecules ◽  
2022 ◽  
Vol 27 (1) ◽  
pp. 330
Author(s):  
Mohammed I. El-Gamal ◽  
Seyed-Omar Zaraei ◽  
Moustafa M. Madkour ◽  
Hanan S. Anbar

Pyrazole has been recognized as a pharmacologically important privileged scaffold whose derivatives produce almost all types of pharmacological activities and have attracted much attention in the last decades. Of the various pyrazole derivatives reported as potential therapeutic agents, this article focuses on pyrazole-based kinase inhibitors. Pyrazole-possessing kinase inhibitors play a crucial role in various disease areas, especially in many cancer types such as lymphoma, breast cancer, melanoma, cervical cancer, and others in addition to inflammation and neurodegenerative disorders. In this article, we reviewed the structural and biological characteristics of the pyrazole derivatives recently reported as kinase inhibitors and classified them according to their target kinases in a chronological order. We reviewed the reports including pyrazole derivatives as kinase inhibitors published during the past decade (2011–2020).

EMJ Urology ◽  
2021 ◽  
pp. 72-82
Author(s):  
Mohammad Faruquz Zaman ◽  
Noor Buchholz ◽  
Christian Bach

Objectives: To evaluate an overview of the past, present, and future of robotic surgery. To provide insight and focus on the current status of the field of robotic systems for urological surgery with outcomes and discuss future perspectives in terms of other operative techniques and new robotic platforms. Evidence acquisition: The authors undertook a non-systematic literature review using PubMed, Medline, and Google search. They used the search terms “robotic uro-surgery”, “laparoscopic”, “minimally invasive surgery”, “future of robotics”, “global robotic market growth”, “geographical distribution”, and “cost-effectiveness”. Evidence synthesis: Robotic surgery has embraced and extended almost all aspects of uro-surgical fields since its introduction three decades ago. There are definite advantages of robots to the surgeons and patients. It has become new standard of care for many surgical procedures. Innovation and technological advances are continuing and new with more precise robots are emerging. The major downside is cost. Despite the high cost, robot market is growing. Conclusion: Over the past decade, minimally invasive approaches have virtually revolutionised surgery and robotic surgery has accelerated these changes. Without doubt, robotic urologic surgery is here to stay and will expand further in all surgical disciplines. Utilisation of robotics should be coupled with a reduction in costs to healthcare systems, and improved clinical outcomes for the general population rather than a privileged few. Therefore, making this expensive technology more affordable must be part of the equation.


2020 ◽  
Vol 16 (4) ◽  
pp. 431-453
Author(s):  
Xiao-hua Cai ◽  
Hong-yan Zhang ◽  
Bing Xie

Matrine-family alkaloids as tetracycloquinolizindine analogues from Traditional Chinese Medicine Sophora flavescens Ait, Sophora subprostrata and Sophora alopecuroides L possess various pharmacological activities and have aroused great interests over the past decades. Especially, a lot of matrine derivatives have been designed and synthesized and their biological activities investigated, and encouraging results have continuously been achieved in recent several years. These studies are helpful to develop more potent candidates or therapeutic agents and disclose their molecular targets and mechanisms. This paper reviews recent advances in the bioactive modifications of matrine-family alkaloids from derivatization of the C-13, C-14 or C-15 position, opening D ring, fusing D ring and structural simplification.


2017 ◽  
Vol 2 (4) ◽  
pp. 71
Author(s):  
Mardawig Alebouyeh

The pediatric hematology and oncology (PHO) services in Iran have steadily improved during the past 10 years.Today, we have specialized PHO services in almost all major cities throughout the country, where 43 board-certified or eligible pediatric hematologist-oncologists are currently giving care to children suffering from cancer or hematological disorders. In this paper, the state of Pediatric hematology-oncology in Iran will be presented.


Author(s):  
Vanessa Nadig ◽  
Ken Herrmann ◽  
Felix M. Mottaghy ◽  
Volkmar Schulz

AbstractPurpose Since the 1990s, PET has been successfully combined with MR or CT systems. In the past years, especially PET systems have seen a trend towards an enlarged axial field of view (FOV), up to a factor of ten. Methods Conducting a thorough literature research, we summarize the status quo of contemporary total-body (TB) PET/CT scanners and give an outlook on possible future developments. Results Currently, three human TB PET/CT systems have been developed: The PennPET Explorer, the uExplorer, and the Biograph Vision Quadra realize aFOVs between 1 and 2 m and show a tremendous increase in system sensitivity related to their longer gantries. Conclusion The increased system sensitivity paves the way for short-term, low-dose, and dynamic TB imaging as well as new examination methods in almost all areas of imaging.


2021 ◽  
Vol 22 (9) ◽  
pp. 4294
Author(s):  
Marcin Ożarowski ◽  
Tomasz M. Karpiński ◽  
Aleksandra Zielińska ◽  
Eliana B. Souto ◽  
Karolina Wielgus

As the major nonpsychotropic constituent of Cannabis sativa, cannabidiol (CBD) is regarded as one of the most promising therapeutic agents due to its proven effectiveness in clinical trials for many human diseases. Due to the urgent need for more efficient pharmacological treatments for several chronic diseases, in this review, we discuss the potential beneficial effects of CBD for Alzheimer’s disease, epilepsy, multiple sclerosis, and neurological cancers. Due to its wide range of pharmacological activities (e.g., antioxidant, anti-inflammatory, and neuroprotective properties), CBD is considered a multimodal drug for the treatment of a range of neurodegenerative disorders, and various cancer types, including neoplasms of the neural system. The different mechanisms of action of CBD are here disclosed, together with recent progress in the use of this cannabis-derived constituent as a new therapeutic approach.


2020 ◽  
Vol 20 (13) ◽  
pp. 1300-1310 ◽  
Author(s):  
M. İhsan Han ◽  
Ş. Güniz Küçükgüzel

This review explains the effects of naproxen and the naproxen moiety in important biological activities. Naproxen, 2-(6-methoxynaphthalen-2-yl)propionic acid, is one of the most utilized propionic acid derivatives to the cure of many injuries or pains. Naproxen is a non-steroidal antiinflammatory drug (NSAID), which is generally used among the NSAIDs. Even though it has gastrointestinal side effects, naproxen has been safely used for many years because of the good cardiovascular sight. In the past years, except for anti-inflammatory effects, other pharmacological activities of naproxen, especially anticancer and antimicrobial activities, gain the attention of researchers. Naproxen shows its activity by inhibiting the COX-2 enzyme. There is significant interest in the possibility that COX-2 inhibitors might retard or prevent the development of various cancer types, which is often characterized by COX-2 expression. The activities of both naproxen and new molecules derived from naproxen were frequently investigated.


2003 ◽  
Vol 1 (1) ◽  
pp. 87-90 ◽  
Author(s):  
Chris Garvey

Asthma rates in the US have risen during the past 25 years, as have asthma-related morbidity and healthcare costs. Professional organizations involved in asthma care have identified the need to assure that an advanced level of asthma knowledge and skill is available to patients with asthma, their families, and insurers. This need led to development of the certification for asthma educators. The Certified Asthma Educator (AE-C) must meet specific clinical criteria and pass a standardized examination designed to evaluate knowledge and skill for providing competent asthma education and coordination. The development and current status of the Certified Asthma Educator examination process and content are discussed, as are goals of the certification


2013 ◽  
pp. 109-128 ◽  
Author(s):  
C. Rühl

This paper presents the highlights of the third annual edition of the BP Energy Outlook, which sets out BP’s view of the most likely developments in global energy markets to 2030, based on up-to-date analysis and taking into account developments of the past year. The Outlook’s overall expectation for growth in global energy demand is to be 36% higher in 2030 than in 2011 and almost all the growth coming from emerging economies. It also reflects shifting expectations of the pattern of supply, with unconventional sources — shale gas and tight oil together with heavy oil and biofuels — playing an increasingly important role and, in particular, transforming the energy balance of the US. While the fuel mix is evolving, fossil fuels will continue to be dominant. Oil, gas and coal are expected to converge on market shares of around 26—28% each by 2030, and non-fossil fuels — nuclear, hydro and renewables — on a share of around 6—7% each. By 2030, increasing production and moderating demand will result in the US being 99% self-sufficient in net energy. Meanwhile, with continuing steep economic growth, major emerging economies such as China and India will become increasingly reliant on energy imports. These shifts will have major impacts on trade balances.


1995 ◽  
Vol 32 (9-10) ◽  
pp. 267-272 ◽  
Author(s):  
A. Angelakis ◽  
E. Diamadopoulos

The basic aim of this paper is to present the existing conditions and problems of water resources management in Greece. Water demand has increased tremendously over the past 30 years. Despite adequate precipitation, water imbalance is often experienced, due to temporal and regional variations of the precipitation, the increased water demand during the summer months and the difficulty of transporting water due to the mountainous terrain. Integration of reclaimed wastewater originating from the wastewater treatment plant effluents into the water resources management is proposed. This plan exhibits the potential for reducing the pollution loads entering sea or inland waters, while at the same time providing water for irrigation.


2020 ◽  
Vol 27 (40) ◽  
pp. 6864-6887 ◽  
Author(s):  
Mohd Adil Shareef ◽  
Irfan Khan ◽  
Bathini Nagendra Babu ◽  
Ahmed Kamal

Background:: Imidazo[2,1-b]thiazole, a well-known fused five-membered hetrocycle is one of the most promising and versatile moieties in the area of medicinal chemistry. Derivatives of imidazo[2,1-b]thiazole have been investigated for the development of new derivatives that exhibit diverse pharmacological activities. This fused heterocycle is also a part of a number of therapeutic agents. Objective:: To review the extensive pharmacological activities of imidazo[2,1-b]thiazole derivatives and the new molecules developed between 2000-2018 and their usefulness. Method:: Thorough literature review of all relevant papers and patents was conducted. Conclusion:: The present review, covering a number of aspects, is expected to provide useful insights in the design of imidazo[2,1-b]thiazole-based compounds and would inspire the medicinal chemists for a comprehensive and target-oriented information to achieve a major breakthrough in the development of clinically viable candidates.


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