Structure-Bioactivity Relationship Study of Xanthene Derivatives: A Brief Review

2020 ◽  
Vol 16 (8) ◽  
pp. 1071-1077
Author(s):  
Aref G. Ghahsare ◽  
Zahra S. Nazifi ◽  
Seyed M.R. Nazifi
Keyword(s):  
Biological Activities ◽  
Cyclic Compound ◽  
Research Field ◽  
Pharmaceutical Chemistry ◽  
Therapeutic Effects ◽  
Main Research ◽  
Research Fields ◽  
Xanthene Derivatives ◽  
Anti Cancer ◽  
Heterocyclic Derivatives

: Over the last decades, several heterocyclic derivatives compounds have been synthesized or extracted from natural resources and have been tested for their pharmaceutical activities. Xanthene is one of these heterocyclic derivatives. These compounds consist of an oxygen-containing central heterocyclic structure with two more cyclic structures fused to the central cyclic compound. It has been shown that xanthane derivatives are bioactive compounds with diverse activities such as anti-bacterial, anti-fungal, anti-cancer, and anti-inflammatory as well as therapeutic effects on diabetes and Alzheimer. The anti-cancer activity of such compounds has been one of the main research fields in pharmaceutical chemistry. Due to this diverse biological activity, xanthene core derivatives are still an attractive research field for both academia and industry. This review addresses the current finding on the biological activities of xanthene derivatives and discussed in detail some aspects of their structure-activity relationship (SAR).

scholarly journals Review and Prospect of Financial Geography Research

2018 ◽  
Vol 1 (1) ◽  
Author(s):  
Zhigang Wang
Keyword(s):  
Economic Geography ◽  
Research Field ◽  
Stable Operation ◽  
Financial Industry ◽  
Main Research ◽  
Research Fields ◽  
Measurement Analysis ◽  
Foreign Countries ◽  
Social And Economic Development ◽  
Financial Geography

 As an important branch of economic geography, financial geography has important significance for maintaining the stable operation of the financial industry and thus promoting social and economic development. Based on the perspective of geography, we first combed the development history and main research fields of international financial geography. According to the differences of mainstream research methods in a specific period, the development process can be divided into three stages: germination, political economics and economic geography. With the help of literature measurement analysis, the international financial geography research is divided into the classic research field focusing on the financial center, the spatial evolution of financial subjects, the financial network and regional interaction, and the emerging research fields with different scales of financialization. Then it summarizes the progress of China’s financial geography research. Although China’s financial geography started late, there is still a gap between the breadth and depth of research compared to foreign countries, but its institutional background is different from the Western institutional background. It provides a diversified explanation for its own specific financial landscape. Finally, combined with the development status of financial geography at home and abroad, the research prospects of this discipline are prospected.

scholarly journals Ursolic Acid-Based Derivatives as Potential Anti-Cancer Agents: An Update

2020 ◽  
Vol 21 (16) ◽  
pp. 5920 ◽  
Author(s):  
Vuyolwethu Khwaza ◽  
Opeoluwa O. Oyedeji ◽  
Blessing A. Aderibigbe
Keyword(s):  
Ursolic Acid ◽  
Clinical Medicine ◽  
Biological Activities ◽  
Therapeutic Effects ◽  
Pharmacological Activities ◽  
Pentacyclic Triterpenoid ◽  
Anti Cancer ◽  
Pharmacologically Active ◽  
Derivatives Of ◽  
Cell Signaling Pathways

Ursolic acid is a pharmacologically active pentacyclic triterpenoid derived from medicinal plants, fruit, and vegetables. The pharmacological activities of ursolic acid have been extensively studied over the past few years and various reports have revealed that ursolic acid has multiple biological activities, which include anti-inflammatory, antioxidant, anti-cancer, etc. In terms of cancer treatment, ursolic acid interacts with a number of molecular targets that play an essential role in many cell signaling pathways. It suppresses transformation, inhibits proliferation, and induces apoptosis of tumor cells. Although ursolic acid has many benefits, its therapeutic applications in clinical medicine are limited by its poor bioavailability and absorption. To overcome such disadvantages, researchers around the globe have designed and developed synthetic ursolic acid derivatives with enhanced therapeutic effects by structurally modifying the parent skeleton of ursolic acid. These structurally modified compounds display enhanced therapeutic effects when compared to ursolic acid. This present review summarizes various synthesized derivatives of ursolic acid with anti-cancer activity which were reported from 2015 to date.

A Comprehensive Appraisal of Chalcones and Their Heterocyclic Analogs as Antimicrobial Agents

2020 ◽  
Vol 24 (23) ◽  
pp. 2755-2781
Author(s):  
Riddhi Salotra ◽  
Divya Utreja
Keyword(s):  
Antimicrobial Agents ◽  
Biological Activities ◽  
Structural Diversity ◽  
Natural Sources ◽  
Anti Cancer ◽  
Heterocyclic Derivatives ◽  
Synthetic Methodologies ◽  
Microbial Potential ◽  
High Degree ◽  
Therapeutic Profile

Owing to the growing demand for compelling antimicrobial agents, chalcones and their heterocyclic derivatives have engrossed prodigious attention of medicinal chemists as an effective clinical template for the synthesis of such agents on account of their structural diversity and molecular flexibility. Chalcones are considered as a fortunate scaffold in the field of both synthetic as well as natural product chemistry. They are reflected as a remarkable section of logically occurring pharmacophores that possess a comprehensive scale of biological activities, such as anti-cancer, anti-malarial, anti-viral and anti-inflammatory, rendering them with a high degree of assortment and noble therapeutic profile. They act as a crucial intermediate for the synthesis of novel heterocyclic skeletons holding biodynamic behavior. This review emphasizes on different aspects of chalcones including their natural sources, recent synthetic methodologies and evaluation of their anti-microbial potential. It is expected as a persuasive compilation on chalcones that may benefit the experts to design potent and less toxic chalcone referents as medicinal agents.

Learning Analytics

2019 ◽  
pp. 52-72
Author(s):  
Libor Juhaňák ◽  
Jiří Zounek
Keyword(s):  
Learning Analytics ◽  
Wide Spectrum ◽  
Historical Context ◽  
Research Field ◽  
Main Research ◽  
Analytical Instruments ◽  
Research Fields ◽  
Methods And Techniques ◽  
New Research ◽  
Further Development

The goal of this chapter is to present and describe a relatively new research field, known as learning analytics, which focuses on use of a wide spectrum of analytical methods and techniques to analyze data coming from educational contexts. The first part of the chapter focuses on the historical context of analytics in education and introduces several research fields that participated in the creation and formation of learning analytics. At the same time, the development of learning analytics and basic related concepts are described in more detail. In the second part, the authors provide an overview of the main research fields and topics within learning analytics, including an overview of commonly used analytical instruments and systems. The final part of the chapter then focuses on challenges currently faced by the field of learning analytics, as well as on opportunities for further development and research within learning analytics in the upcoming years, which are now under development.

Ursolic Acid in Cancer Treatment and Metastatic Chemoprevention: From Synthesized Derivatives to Nanoformulations in Preclinical Studies

2019 ◽  
Vol 19 (4) ◽  
pp. 245-256 ◽  
Author(s):  
Junjie Zou ◽  
Juanfang Lin ◽  
Chao Li ◽  
Ruirui Zhao ◽  
Lulu Fan ◽  
...  
Keyword(s):  
Ursolic Acid ◽  
Cancer Metastasis ◽  
Biological Activities ◽  
Inhibitory Effect ◽  
Cancer Drug ◽  
Therapeutic Effects ◽  
Candidate Drug ◽  
Wide Range ◽  
Anti Cancer ◽  
Tumor Growth And Metastasis

Background:Cancer metastasis has emerged as a major public health threat that causes majority of cancer fatalities. Traditional chemotherapeutics have been effective in the past but suffer from low therapeutic efficiency and harmful side-effects. Recently, it has been reported ursolic acid (UA), one of the naturally abundant pentacyclic triterpenes, possesses a wide range of biological activities including anti-inflammatory, anti-atherosclerotic, and anti-cancer properties. More importantly, UA has the features of low toxicity, liver protection and the potential of anti-cancer metastasis.Objective:This article aimed at reviewing the great potential of UA used as a candidate drug in the field of cancer therapy relating to suppression of tumor initiation, progression and metastasis.Methods:Selective searches were conducted in Pubmed, Google Scholar and Web of Science using the keywords and subheadings from database inception to December 2017. Systemic reviews are summarized here.Results:UA has exhibited chemopreventive and therapeutic effects of cancer mainly through inducing apoptosis, inhibiting cell proliferation, preventing tumor angiogenesis and metastatic. UA nanoformulations could enhance the solubility and bioavailability of UA as well as exhibit better inhibitory effect on tumor growth and metastasis.Conclusion:The information presented in this article can provide useful references for further studies on making UA a promising anti-cancer drug, especially as a prophylactic metastatic agent for clinical applications.

scholarly journals An Overview on Medicinal Perspective and Biological Behavior of Benzotriazole; Synthetic Study on Its Multifaceted Biological Activities

2021 ◽  
Vol 8 (5) ◽  
pp. 365-378
Author(s):  
V. S. Anjana ◽  
P. Manoj Kumar
Keyword(s):  
Biological Activities ◽  
Wide Spectrum ◽  
Research Field ◽  
Synthetic Methods ◽  
Biological Behavior ◽  
Sar Studies ◽  
Structure Activity ◽  
Anti Cancer ◽  
Anti Inflammatory ◽  
Anti Fungal

Benzotriazole (BTA) is a nitrogen containing heterocyclic derivative containing three nitrogen atoms at 1st, 2nd and 3rd positions with chemical formula C6H5N3. Benzotriazole and its derivatives have great significance in medicinal chemistry and these derivatives were used by several chemists for therapeutic conditions because it possessing a wide spectrum of pharmacological activities including anti bacterial, anti fungal, anti viral, anti inflammatory, anti hyperglycemic, anti hypertensive, anti cancer and analgesic activity. In this review, different synthetic methods for the preparation of benzotriazole, importance of benzotriazole derivatives in biomedical research, highlighting its biological behavior, versatile activities and Structure Activity Relationship (SAR) studies are described. This review will help the researchers to understand the structure activity relationships and improvise the concepts in their research field. Keywords: Benzotriazole, Anti microbial, Anthelmintic, Analgesic, Anti mycobacterial, Anti viral, Anti oxidative, Anti tumor, Anti inflammatory, Anti hyperglycemia, Anti fungal, Anticonvulsant activity.

scholarly journals Half-a-century of gamma-ray astrophysics at the Max-Planck Institute for Extraterrestrial Physics

2021 ◽  
Vol 46 (1) ◽  
Author(s):  
Volker Schönfelder ◽  
Jochen Greiner
Keyword(s):  
Gamma Ray ◽  
Scientific Progress ◽  
Research Field ◽  
Substantial Part ◽  
Max Planck ◽  
Main Research ◽  
Gamma Ray Astronomy ◽  
Research Fields ◽  
Technological Developments ◽  
History Of

AbstractGamma-ray astronomy has been one of the prime scientific research fields of the Max-Planck Institute for Extraterrestrial Physics (MPE) from its beginning. Over the years, the entire gamma-ray energy range accessible from space was explored. The purpose of this review article is to summarise the achievements of the gamma-ray group at MPE during the last 50+ years. This covers a substantial part of the general history of space-based gamma-ray astronomy, for which both, general review articles (e.g. Pinkau in Exp Astron 5: 157, 2009; Schönfelder in AN 323: 524, 2002; Trimble in AIP Conf Proc 304: 40, 1994) and a detailed tabular list of events and missions (Leonard and Gehrels in https://heasarc.gsfc.nasa.gov/docs/history, version 1.0.8, 2009), have been compiled. Here, we describe the gamma-ray activities at MPE from the beginning till the present, reviewing the tight interplay between new technological developments towards new instruments and scientific progress in understanding gamma-ray sources in the sky. This covers (i) the early development of instruments and their tests on half a dozen balloon flights, (ii) the involvement in the most important space missions at the time, i.e. ESA’s COS-B satellite, NASA’s Compton Gamma-ray Observatory and Fermi Space Telescope, as well as ESA’s INTEGRAL observatory, (iii) the participation in several other missions such as TD-1, Solar Maximum Mission, or Ulysses, and (iv) the complementary ground-based optical instruments OPTIMA and GROND to enhance selected science topics (pulsars, gamma-ray bursts). With the gradual running-out of institutional support since 2010, gamma-ray astrophysics as a main research field has now come to an end at MPE.

scholarly journals Black Garlic and Its Bioactive Compounds on Human Health Diseases: A Review

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 5028
Author(s):  
Tanvir Ahmed ◽  
Chin-Kun Wang
Keyword(s):  
Human Health ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Water Soluble ◽  
Therapeutic Effects ◽  
Organosulfur Compounds ◽  
Wide Range ◽  
Anti Cancer ◽  
Future Challenges ◽  
Anti Inflammation

Black garlic (BG) is a form of aged garlic obtained from raw garlic (Allium sativum) via Millard reaction under high temperature (60–90 °C) and humidity (70–90%) for a period of time. Several studies reported higher contents of water-soluble antioxidants compounds (S-allyl cysteine, S-allyl-mercapto cysteine), 5-hydroxymethylfurfural, organosulfur compounds, polyphenol, volatile compounds, and products of other Millard reactions compared to fresh garlic after the thermal processing. Recent studies have demonstrated that BG and its bioactive compounds possess a wide range of biological activities and pharmacological properties that preserve and show better efficacy in preventing different types of diseases. Most of these benefits can be attributed to its anti-oxidation, anti-inflammation, anti-obesity, hepatoprotection, hypolipidemia, anti-cancer, anti-allergy, immunomodulation, nephroprotection, cardiovascular protection, and neuroprotection. Substantial studies have been conducted on BG and its components against different common human diseases in the last few decades. Still, a lot of research is ongoing to find out the therapeutic effects of BG. Thus, in this review, we summarized the pre-clinical and clinical studies of BG and its bioactive compounds on human health along with diverse bioactivity, a related mode of action, and also future challenges.

Anodyne activities of New Tetrazole derivatives from Triazine

2020 ◽  
Vol 11 (3) ◽  
pp. 3377-3383
Author(s):  
Arulmozhi R ◽  
Abirami N ◽  
Helen P Kavitha ◽  
Arulmurugan S ◽  
Vinoth Kumar J
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Pharmaceutical Chemistry ◽  
Tail Flick ◽  
Structural Fragment ◽  
Hot Plate ◽  
Standard Drug ◽  
New Class ◽  
Novel Drugs ◽  
Tetrazole Derivatives

The creation of novel drugs containing a tetrazole ring as a structural fragment has contributed considerably to the outstanding achievements of the pharmaceutical chemistry in the last decade. Tetrazoles are the heterocyclic compounds having diverse biological activities such as analgesic, antiinflammation, antimicrobial, anticancer, antidiabetic, etc., and an impending source in biosciences. In this paper, the authors describe the synthesis of novel tetrazoles from N, N-( 6-Phenyl-1,3,5-triazine-2,4-diyl) dibenzamide (PTDDB) and 2-phenyl-4, 6-di(2H-tetrazole-2-yl)-1,3,5-triazine(5a-i) were prepared per the proposed scheme. A new class of tetrazole heterocycles were synthesised and characterised. I n vivo analysis was carried out on the analgesic property of synthesised tetrazole derivatives (5a, 5b, 5c). Characterisation studies such as IR, 1H NMR, 13C NMR, Mass and elemental analysis were performed for the synthesised tetrazole derivatives. Some of the tetrazole derivatives 5a, 5b, and 5c were tested for anodyne activity using morphine as the standard drug. The data reveals that all the three compounds 5a, 5b and 5c taken for the study show analgesic activity by hot plate method and tail flick methods. Among tested compounds, compound 5c is found to have potent analgesic (anodyne) activity. The results of the study indicate that the sample taken for the study show fairly good business using morphine as the standard drug.

ANTICANCER EFFECT OF UVARIA GENUS

2014 ◽  
pp. 98-101
Author(s):  
Thi Bich Hien Le ◽  
Viet Duc Ho ◽  
Thi Hoai Nguyen
Keyword(s):  
Biological Activities ◽  
Current Trend ◽  
Healthcare Systems ◽  
Chemical Compositions ◽  
Cancer Therapies ◽  
Pharmacological Effects ◽  
Anticancer Effect ◽  
Anti Cancer ◽  
Tropical Areas ◽  
Cancer Activity

Nowadays, cancer treatment has been a big challenge to healthcare systems. Most of clinical anti-cancer therapies are toxic and cause adverse effects to human body. Therefore, current trend in science is seeking and screening of natural compounds which possess antineoplastic activities to utilize in treatment. Uvaria L. - Annonaceae includes approximately 175 species spreading over tropical areas of Asia, Australia, Africa and America. Studies on chemical compositions and pharmacological effects of Uvaria showed that several compound classes in this genus such as alkaloid, flavonoid, cyclohexen derivaties, acetogenin, steroid, terpenoid, etc. indicate considerable biological activities, for example anti-tumor, anti-cancer, antibacterial, antifungal, antioxidant, etc. Specifically, anti-cancer activity of fractions of extract and pure isolated compounds stands out for cytotoxicity against many cancer cell lines. This study provides an overview of anti-cancer activity of Uvaria and suggests a potential for further studies on seeking and developing novel anti-cancer compounds. Key words: Anti-cancer, Uvaria.

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