Matrine-Family Alkaloids: Versatile Precursors for Bioactive Modifications

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.

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).


Marine Drugs ◽  
2021 ◽  
Vol 19 (11) ◽  
pp. 610
Author(s):  
Junjie Yan ◽  
Weiwei Liu ◽  
Jiatong Cai ◽  
Yiming Wang ◽  
Dahong Li ◽  
...  

Phenazines are a large group of nitrogen-containing heterocycles, providing diverse chemical structures and various biological activities. Natural phenazines are mainly isolated from marine and terrestrial microorganisms. So far, more than 100 different natural compounds and over 6000 synthetic derivatives have been found and investigated. Many phenazines show great pharmacological activity in various fields, such as antimicrobial, antiparasitic, neuroprotective, insecticidal, anti-inflammatory and anticancer activity. Researchers continued to investigate these compounds and hope to develop them as medicines. Cimmino et al. published a significant review about anticancer activity of phenazines, containing articles from 2000 to 2011. Here, we mainly summarize articles from 2012 to 2021. According to sources of compounds, phenazines were categorized into natural phenazines and synthetic phenazine derivatives in this review. Their pharmacological activities, mechanisms of action, biosynthetic pathways and synthetic strategies were summarized. These may provide guidance for the investigation on phenazines in the future.


Author(s):  
CHANDRA VELUCHAMY ◽  
RADHA PALANISWAMY

The ocean is the major essential source of structurally unique natural products that are mainly present in living organisms. The essential products extracted from marine microbes and marine algae are highly analyzed areas in instinctive product research. Marine algae are the novel food with potential nutritional values used for multiple purposes in industry and medicine. They show pharmacological activities which are helpful for the invention of bioactive compounds. Furthermore, marine algae have shown to provide an abundant source of natural bioactive compounds with antidiabetic, anti-inflammatory, antiviral, antifungal, hypolipidemic, antioxidant, anti-hypercholesterolemia, antibacterial, and antineoplastic properties. They produce new secondary metabolites that possess biological activities and have the potential to be developed as therapeutic agents. Macroalgal lectins, fucoidans, kainoids, and other substances have been routinely used in the research of biomedical and also have biological activities. The potential pharmaceutical, medicinal, and research applications of these compounds are discussed.


Molecules ◽  
2020 ◽  
Vol 25 (8) ◽  
pp. 1909 ◽  
Author(s):  
Nagaraju Kerru ◽  
Lalitha Gummidi ◽  
Suresh Maddila ◽  
Kranthi Kumar Gangu ◽  
Sreekantha B. Jonnalagadda

The analogs of nitrogen-based heterocycles occupy an exclusive position as a valuable source of therapeutic agents in medicinal chemistry. More than 75% of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties. In the forthcoming decade, a much greater share of new nitrogen-based pharmaceuticals is anticipated. Many new nitrogen-based heterocycles have been designed. The number of novel N-heterocyclic moieties with significant physiological properties and promising applications in medicinal chemistry is ever-growing. In this review, we consolidate the recent advances on novel nitrogen-containing heterocycles and their distinct biological activities, reported over the past one year (2019 to early 2020). This review highlights the trends in the use of nitrogen-based moieties in drug design and the development of different potent and competent candidates against various diseases.


2011 ◽  
Vol 2011 ◽  
pp. 1-17 ◽  
Author(s):  
Azamjon B. Soliev ◽  
Kakushi Hosokawa ◽  
Keiichi Enomoto

Research into natural products from the marine environment, including microorganisms, has rapidly increased over the past two decades. Despite the enormous difficulty in isolating and harvesting marine bacteria, microbial metabolites are increasingly attractive to science because of their broad-ranging pharmacological activities, especially those with unique color pigments. This current review paper gives an overview of the pigmented natural compounds isolated from bacteria of marine origin, based on accumulated data in the literature. We review the biological activities of marine compounds, including recent advances in the study of pharmacological effects and other commercial applications, in addition to the biosynthesis and physiological roles of associated pigments. Chemical structures of the bioactive compounds discussed are also presented.


2019 ◽  
Vol 19 (10) ◽  
pp. 809-825 ◽  
Author(s):  
Qing-Shan Li ◽  
Yao Li ◽  
Girdhar Singh Deora ◽  
Ban-Feng Ruan

Resveratrol is a non-flavonoid polyphenol containing a terpenoid backbone. It has been intensively studied because of its various promising biological properties, such as anticancer, antioxidant, antibacterial, neuroprotective and anti-inflammatory activities. However, the medicinal application of resveratrol is constrained by its poor bioavailability and stability. In the past decade, more attention has been focused on making resveratrol derivatives to improve its pharmacological activities and pharmacokinetics. This review covers the literature published over the past 15 years on synthetic analogues of resveratrol. The emphasis is on the chemistry of new compounds and relevant biological activities along with structure-activity relationship. This review aims to provide a scientific and reliable basis for the development of resveratrol-based clinical drugs.


2021 ◽  
Vol 2021 ◽  
pp. 1-19
Author(s):  
Javad Sharifi-Rad ◽  
Natália Cruz-Martins ◽  
Pía López-Jornet ◽  
Eduardo Pons-Fuster Lopez ◽  
Nidaa Harun ◽  
...  

Coumarins belong to the benzopyrone family commonly found in many medicinal plants. Natural coumarins demonstrated a wide spectrum of pharmacological activities, including anti-inflammatory, anticoagulant, anticancer, antibacterial, antimalarial, casein kinase-2 (CK2) inhibitory, antifungal, antiviral, Alzheimer’s disease inhibition, neuroprotective, anticonvulsant, phytoalexins, ulcerogenic, and antihypertensive. There are very few studies on the bioavailability of coumarins; therefore, further investigations are necessitated to study the bioavailability of different coumarins which already showed good biological activities in previous studies. On the evidence of varied pharmacological properties, the present work presents an overall review of the derivation, availability, and biological capacities of coumarins with further consideration of the essential mode of their therapeutic actions. In conclusion, a wide variety of coumarins are available, and their pharmacological activities are of current interest thanks to their synthetic accessibility and riches in medicinal plants. Coumarins perform the valuable function as therapeutic agents in a range of medical fields.


Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4677
Author(s):  
Thuraya Al-Harthy ◽  
Wajdi Zoghaib ◽  
Raid Abdel-Jalil

Fluorine-containing heterocycles continue to receive considerable attention due to their unique properties. In medicinal chemistry, the incorporation of fluorine in small molecules imparts a significant enhancement their biological activities compared to non-fluorinated molecules. In this short review, we will highlight the importance of incorporating fluorine as a basic appendage in benzothiazole and benzimidazole skeletons. The chemistry and pharmacological activities of heterocycles containing fluorine during the past years are compiled and discussed.


2018 ◽  
Vol 19 (2) ◽  
pp. 114-124 ◽  
Author(s):  
Weiyan Cheng ◽  
Chuanhui Huang ◽  
Weifeng Ma ◽  
Xin Tian ◽  
Xiaojian Zhang

Oridonin is one of the major components isolated from Isodon rubescens, a traditional Chinese medicine, and it has been confirmed to exhibit many kinds of biological activities including anticancer, anti-inflammation, antibacterial and so on. However, the poor pharmaceutical property limits the clinical applications of oridonin. So many strategies have been explored in the purpose of improving the potencies of oridonin, and structure modification is one thus way. This review outlines the landscape of the recent development of oridonin derivatives with diverse pharmacological activities, mainly focusing on the biological properties, structure-activity relationships, and mechanism of actions.


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