3-(2-Isocyanoethyl)indole: A Versatile Reagent for Polycyclic Spiroindoline Synthesis

Synlett ◽  
2020 ◽  
Vol 31 (11) ◽  
pp. 1033-1039 ◽  
Author(s):  
Yun-Lin Liu ◽  
Guo-Shu Chen ◽  
Xiao-Tong Lin
Keyword(s):  
Broad Spectrum ◽  
Indole Alkaloids ◽  
Cascade Reactions ◽  
Pharmacological Activities ◽  
The Past ◽  
Large Families ◽  
Biological And Pharmacological Activities ◽  
Versatile Reagent

Polycyclic spiroindolines are the basic skeletons of large families of indole alkaloids that exhibit a broad spectrum of biological and pharmacological activities. The past seven years have seen impressive developments in the construction of polycyclic spiroindolines enabled by 3-(2-isocyanoethyl)indole-based cascade reactions. We herein give a brief summary on this evolution and highlight our contributions in this field.1 Introduction2 Cascade Reactions Involving Nitrilium Ion Intermediates3 Cascade Reactions Involving Ketenimine Intermediates4 Conclusion and Outlook

scholarly journals A Review: Medicinally Important Nitrogen Sulphur Containing Heterocycles

2020 ◽  
Vol 14 (1) ◽  
pp. 49-64
Author(s):  
Praveen K. Sharma ◽  
Andleeb Amin ◽  
M. Kumar
Keyword(s):  
Broad Spectrum ◽  
Mode Of Action ◽  
Mammalian Cells ◽  
Heterocyclic Compounds ◽  
Structural Features ◽  
Present Review ◽  
Pharmacological Activities ◽  
Sulfur Heterocycles ◽  
Biological And Pharmacological Activities

Nitrogen sulphur containing heterocycles have specific properties due to which they can be used as a potential material in a different type of industries such as medicinal/pharmaceutical, paint, packing and textile, required for various chemical, physical operations and their use as products. Especially dyes, paint, agrochemicals, medicine, etc. make them more significant. In present days, Nitrogen-Sulfur heterocycles are repeatedly attracting the interest of chemists due to their exceptional bioactive behavior. The present study is a review of the work carried out by a chemist in the discovery of new, effective, medicinally important heterocyclic compounds. The present review basically focused on nitrogen-sulfur heterocycles of potential therapeutic interest, especially with thiazole, thiazine, pyrimidine, morpholine and piperazine heterosystems, benzothiazines, pyrazole-benzothiazines, morpholine-benzothiazines, piperazine-benzothiazines and pyrimidine-benzothiazoles, mainly due to their unique structural features, which enable them to exhibit a number of biological and pharmacological activities. Due to a novel mode of action, a broad spectrum of activity, lesser toxicity towards mammalian cells, and suitable profiles towards humans have triggered the use of Nitrogen Sulphur containing heterocycles in designing and synthesizing their derivatives with better properties. The overall objective of the review is to discuss the importance of novel biodynamic structurally diverse heterocycles of potential therapeutic interest: pyrimidine, morpholine, piperazine, pyrozole, benothiazoles, pyrimidobenzothiazoles, 4H-1,4-benzothiazines, pyrazolyl-benzothiazines, morpholinyl-benzothiazines and piperazinylbenzothiazines in order to have access to important commercial molecules for the search of better future.

scholarly journals Marine-Derived Indole Alkaloids and Their Biological and Pharmacological Activities

Marine Drugs ◽  
2021 ◽  
Vol 20 (1) ◽  
pp. 3
Author(s):  
Joko Tri Wibowo ◽  
Peni Ahmadi ◽  
Siti Irma Rahmawati ◽  
Asep Bayu ◽  
Masteria Yunovilsa Putra ◽  
...  
Keyword(s):  
Indole Alkaloids ◽  
Structural Features ◽  
New Drugs ◽  
Pharmacological Activities ◽  
Biological Targets ◽  
Scientific Databases ◽  
Lead Compounds ◽  
Wide Range ◽  
Review Reports ◽  
Biological And Pharmacological Activities

Novel secondary metabolites from marine macroorganisms and marine-derived microorganisms have been intensively investigated in the last few decades. Several classes of compounds, especially indole alkaloids, have been a target for evaluating biological and pharmacological activities. As one of the most promising classes of compounds, indole alkaloids possess not only intriguing structural features but also a wide range of biological/pharmacological activities including antimicrobial, anti-inflammatory, anticancer, antidiabetic, and antiparasitic activities. This review reports the indole alkaloids isolated during the period of 2016–2021 and their relevant biological/pharmacological activities. The marine-derived indole alkaloids reported from 2016 to 2021 were collected from various scientific databases. A total of 186 indole alkaloids from various marine organisms including fungi, bacteria, sponges, bryozoans, mangroves, and algae, are described. Despite the described bioactivities, further evaluation including their mechanisms of action and biological targets is needed to determine which of these indole alkaloids are worth studying to obtain lead compounds for the development of new drugs.

Anticancer Activity of Natural Flavonoids: Inhibition of HIF-1α Signaling Pathway

2020 ◽  
Vol 23 (26) ◽  
pp. 2945-2959 ◽  
Author(s):  
Xiangping Deng ◽  
Yijiao Peng ◽  
Jingduo Zhao ◽  
Xiaoyong Lei ◽  
Xing Zheng ◽  
...  
Keyword(s):  
Transcription Factor ◽  
Secondary Metabolites ◽  
Anticancer Agents ◽  
Hypoxia Inducible Factor ◽  
Tumor Hypoxia ◽  
Pharmacological Activities ◽  
Hypoxia Inducible Factor 1 ◽  
The Past ◽  
Low Toxicity ◽  
Tumor Blood Vessels

Rapid tumor growth is dependent on the capability of tumor blood vessels and glycolysis to provide oxygen and nutrients. Tumor hypoxia is a common characteristic of many solid tumors, and it essentially happens when the growth of the tumor exceeds the concomitant angiogenesis. Hypoxia-inducible factor 1 (HIF-1) as the critical transcription factor in hypoxia regulation is activated to adapt to this hypoxia situation. Flavonoids, widely distributed in plants, comprise many polyphenolic secondary metabolites, possessing broadspectrum pharmacological activities, including their potentiality as anticancer agents. Due to their low toxicity, intense efforts have been made for investigating natural flavonoids and their derivatives that can be used as HIF-1α inhibitors for cancer therapy during the past few decades. In this review, we sum up the findings concerning the inhibition of HIF-1α by natural flavonoids in the last few years and propose the idea of designing tumor vascular and glycolytic multi-target inhibitors with HIF-1α as one of the targets.

Phytochemical and Pharmacological Review on Two Herbs of Baijiangcao: Patrinia scabiosaefolia Fisch. ex Trev. and Patrinia villosa (Thunb.) Juss

2020 ◽  
Vol 17 (5) ◽  
pp. 496-517
Author(s):  
Yangcheng Liu ◽  
Wei Liu ◽  
Jiaqi Wang ◽  
Yang Liu ◽  
Changlan Chen ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Volatile Components ◽  
Research Papers ◽  
Pharmacological Activities ◽  
Comprehensive Review ◽  
Scientific Databases ◽  
The Past ◽  
Current State ◽  
Patrinia Scabiosaefolia ◽  
Antiviral Activities

Patrinia scabiosaefolia Fisch. Trev. and Patrinia villosa (Thunb.) Juss, are two species of Patrinia recorded in the Chinese Pharmacopoeia with the same Chinese name “Baijiangcao” and similar therapeutic effect in traditional Chinese medicine. The present article is the first comprehensive review on the chemical composition and pharmacological activities of these herbs. In this review, data on chemical constituents and pharmacological profile of the two herbs are provided. This review discusses all the classes of the 223 compounds (phenylpropanoids, flavonoids, terpenes, saponins and volatile components, etc.) detected in the two herbs providing information on the current state of knowledge of the phytochemicals present in them. In the past three years, our research group has isolated and identified about more than 100 ingredients from the two herbs. Therefore, we published a systematic review of our research papers and studies on the two herbs were carried out using resources such as classic books about Chinese herbal medicine and scientific databases including Pubmed, Web of Science, SciFinder, CNKI. etc. The present review discusses the most thoroughly studied pharmacological activities (antioxidant, anti-inflammatory, immunomodulatory, antimicrobial, antitumor and antiviral activities) of the two herbs. This comprehensive review will be informative for scientists searching for new properties of these herbs and will be important and significant for the discovery of bioactive compounds from the two herbs and in complete utilization of Patrinia scabiosaefolia Fisch. ex Trev. and Patrinia villosa (Thunb.) Juss.

Recent Advances in Therapeutic Applications of Bisbenzimidazoles

2020 ◽  
Vol 16 (4) ◽  
pp. 454-486 ◽  
Author(s):  
Smita Verma ◽  
Vishnuvardh Ravichandiran ◽  
Nihar Ranjan ◽  
Swaran J.S. Flora
Keyword(s):  
Heterocyclic Compounds ◽  
Wide Spectrum ◽  
Dna Recognition ◽  
Present Review ◽  
Pharmacological Activities ◽  
Structural Motifs ◽  
Therapeutic Applications ◽  
The Past ◽  
Recent Advances

Nitrogen-containing heterocycles are one of the most common structural motifs in approximately 80% of the marketed drugs. Of these, benzimidazoles analogues are known to elicit a wide spectrum of pharmaceutical activities such as anticancer, antibacterial, antiparasitic, antiviral, antifungal as well as chemosensor effect. Based on the benzimidazole core fused heterocyclic compounds, crescent-shaped bisbenzimidazoles were developed which provided an early breakthrough in the sequence-specific DNA recognition. Over the years, a number of functional variations in the bisbenzimidazole core have led to the emergence of their unique properties and established them as versatile ligands against several classes of pathogens. The present review provides an overview of diverse pharmacological activities of the bisbenzimidazole analogues in the past decade with a brief account of its development through the years.

An Overview on Phytochemical and Pharmacological Profile of Morus alba Linn.

2020 ◽  
Vol 16 ◽  
Author(s):  
Arpita Paul ◽  
Monami Rajiung ◽  
Kamaruz Zaman ◽  
Sushil Kumar Chaudhary ◽  
Hans Raj Bhat ◽  
...  
Keyword(s):  
Traditional Medicine ◽  
Morus Alba ◽  
Biologically Active ◽  
Pharmacological Profile ◽  
Pharmacological Activities ◽  
Significant Information ◽  
The Past ◽  
Comprehensive Information ◽  
The Family ◽  
White Mulberry

Background: Morus alba Linn. commonly known as white mulberry, belongs to the family Moraceae, is a promising traditional medicine. In Asia, besides its use in the preparation of delicacies, every part of this plant is utilized in traditional medicine. Over the past decade, studies related to identification and isolation of biologically active compounds, with flavonoids as the major class of phytoconstituents, from this plant has been reported. These phytoconstituents are not only found to be beneficial for the maintenance of general health but also are associated with a range of potential pharmacological activities such as antioxidant, anti-inflammatory, anti-diabetic, anticancer, hepatoprotective, cardioprotective, neuroprotective to name a few. Objective: This review aims to provide upgraded and comprehensive information regarding the phytochemical, ethnomedicinal use and pharmacological profile of the plant Morus alba Linn. Method: The significant information has been collected through various database viz. PubMed, Scopus, Web of Science, Science Direct based on the recent findings, using different terms of Morus alba. Results: The outcome of the study suggests that Morus alba is a multifunctional plant numerous phytochemicals, and possess a range of pharmacological activities. Conclusion: The data assembled on Morus alba will be beneficial to trigger research in various fields of pharmaceutical and allied science to explore the medicinal importance of this unique plant.

scholarly journals Reimagining unfinished architectures: ruin perspectives between art and heritage

2018 ◽  
Vol 26 (2) ◽  
pp. 227-244
Author(s):  
Pablo Arboleda
Keyword(s):  
Financial Crisis ◽  
Broad Spectrum ◽  
Organised Crime ◽  
Public Works ◽  
Architectural Style ◽  
2008 Financial Crisis ◽  
Complex Issue ◽  
The Past ◽  
Single Solution ◽  
The 2008 Financial Crisis

For the past five decades, hundreds of unfinished public works have been erected in Italy as the result of inconsistent planning and the presence of corruption and organised crime. A third of these constructions are located in Sicily alone, and so, in 2007, a group of artists labelled this phenomenon an architectural style: ‘ Incompiuto Siciliano’. Through this creative approach, the artists’ objective is to put incompletion back on the agenda by viewing it from a heritage perspective. This article reviews the different approaches that the artists have envisaged to handle unfinished public works; whether to finish them, demolish them, leave them as they are or opt for an ‘active’ arrested decay. The critical implications of these strategies are analysed in order to, ultimately, conclude that incompletion is such a vast and complex issue that it will surely have more than one single solution; but rather a combination of these four. This is important because it opens up a debate on the broad spectrum of possibilities to tackle incompletion – establishing this as one of the key contemporary urban themes not only in Italy but also in those countries affected by unfinished geographies after the 2008 financial crisis.

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
Keyword(s):  
Kinase Inhibitors ◽  
Therapeutic Agents ◽  
Current Status ◽  
Pyrazole Derivatives ◽  
Chronological Order ◽  
Pharmacological Activities ◽  
The Past ◽  
Cancer Types ◽  
Privileged Scaffold ◽  
Almost All

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).

scholarly journals Review Based Upon Ayurvedic and Traditional Uses of Cinnamomum tamala (Tejpatta)

2021 ◽  
Vol 68 (2) ◽  
Author(s):  
Shifali Thakur ◽  
Gitika Chaudhary
Keyword(s):  
Chemical Constituents ◽  
Bioactive Constituents ◽  
Pharmacological Activities ◽  
The Past ◽  
Cinnamomum Tamala ◽  
Medicinal Use ◽  
Phytochemical Compounds ◽  
Phytochemical Constituents ◽  
Herbal Plant ◽  
Flavoring Agent

Cinnamomum tamala is an evergreen plant native to Sri Lanka and India. This herbal plant is commonly called Indian cassia, Tejpatta and Indian bay leaf. There are many bioactive constituents isolated from plant Cinnamomum tamala. Leaves of the plant possess aromatic fragrance and are also utilized as a flavoring agent. It is used in food curry, pickles and other spices. Besides food application, the leaves have also been used for curing a number of ailments. All parts of the plant possess many major bioactive chemical constituents like cinnamaldehyde, trans-cinnamaldehyde, 3,4,5,7- tetrahydroxyflavone, 3,3,4,5,6- pentahydroflavone (non-glycoside compounds), kaempferol, eugenol, etc. These phytochemical compounds have many pharmacological activities such as anticancer, antidiabetic, antimicrobial, hepatoprotective, antidiarrheal and immunomodulatory. In the past time, it is also considered for medicinal use. Their medicinal use was also mentioned in the literature of ayurveda, yunani and other traditional systems of medicine. Due to aromatic fragrance, it is also utilized in the perfume industry. The major aim of this review is to give a brief knowledge about the plant Cinnamomum tamala based on their phytochemical constituents, ayurvedic view, folk view and pharmacological application.

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