Recent Developments on the Synthesis of Biologically Significant bis/tris(indolyl)methanes under Various Reaction Conditions: A Review

2020 ◽  
Vol 24 (6) ◽  
pp. 583-621
Author(s):  
Arvind Singh ◽  
Gurpreet Kaur ◽  
Bubun Banerjee
Keyword(s):  
Ionic Liquids ◽  
Bioactive Compounds ◽  
Building Block ◽  
Heterogeneous Catalysts ◽  
Metal Catalysts ◽  
Reaction Conditions ◽  
Naturally Occurring ◽  
Wide Range ◽  
Anti Cancer ◽  
Recent Developments

Bis(indolyl)methane skeleton is the main building block of many naturally occurring bioactive compounds. Bis(indolyl)methanes are found to possess a wide range of pharmaceuitical efficacies. These important scaffolds are being used as anti-cancer, antioxidant, anti-bacterial, anti-inflammatory, and anti-proliferative agents. In this review, we summarized the latest developments on the synthesis of various bis/tris(indolyl)methane derivatives from the reactions of two equivalents of indoles and one equivalent of aldehydes or indole-3-carbaldehydes under various reaction conditions. More than hundred different catalysts were employed for these transformations which include various metal catalysts, ionic liquids, organocatalysts, surfactants, homogeneous, heterogeneous catalysts etc.

The chemistry of 4-(dicyanomethylene)-3-methyl-l-phenyl-2-pyrazoline-5- ones as a privileged scaffold in synthesis of heterocycles

2020 ◽  
Vol 17 ◽  
Author(s):  
Mohsen A.-M. Gomaa ◽  
Huda A. Ali
Keyword(s):  
Building Block ◽  
Heterocyclic Compounds ◽  
Recent Progress ◽  
Reaction Conditions ◽  
Azacrown Ethers ◽  
Wide Range ◽  
Privileged Scaffold ◽  
Number Of Publications ◽  
Near Future

Background : The reactivity of 4-(dicyanomethylene)-3-methyl-l-phenyl-2-pyrazoline-5-one DCNP 1 and its derivatives makes it valuable as a building block for the synthesis of heterocyclic compounds like pyrazolo-imidazoles, - thiazoles, spiropyridines, spiropyrroles, spiropyrans and others. As a number of publications have reported on the reactivity of DCNP and its derivatives, we compiled some features of this interesting molecule. Objective: This article aims to review the preparation of DCNP, its reactivity and application in heterocyclic and dyes synthesis. Conclusion: In this review we have provided an overview of recent progress in the chemistry of DCNP and its significance in synthesis of various classes of heterocyclic compounds and dyes. The unique reactivity of DCNP offers unprecedentedly mild reaction conditions for the generation of versatile cynomethylene dyes from a wide range of precursors including amines, α-aminocarboxylic acids, their esters, phenols, malononitriles and azacrown ethers. We anticipate that more innovative transformations involving DCNP will continue to emerge in the near future.

scholarly journals Synthesis, Modification and Biological Activity of Diosgenyl β-d-Glycosaminosides: An Overview

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5433
Author(s):  
Daria Grzywacz ◽  
Beata Liberek ◽  
Henryk Myszka
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Protecting Groups ◽  
Pharmacological Properties ◽  
Amino Group ◽  
Reaction Conditions ◽  
Naturally Occurring ◽  
Anti Cancer ◽  
Wide Group ◽  
Derivatives Of

Saponins are a structurally diverse class of natural glycosides that possess a broad spectrum of biological activities. They are composed of hydrophilic carbohydrate moiety and hydrophobic triterpenoid or steroid aglycon. Naturally occurring diosgenyl glycosides are the most abundant steroid saponins, and many of them exhibit various pharmacological properties. Herein, we present an overview of semisynthetic saponins syntheses–diosgenyl β-d-glycosaminosides (d-gluco and d-galacto). These glycosides possess a 2-amino group, which creates great possibilities for further modifications. A wide group of glycosyl donors, different N-protecting groups and various reaction conditions used for their synthesis are presented. In addition, this paper demonstrates the possibilities of chemical modifications of diosgenyl β-d-glycosaminosides, associated with functionalisation of the amino group. These provide N-acyl, N-alkyl, N,N-dialkyl, N-cinnamoyl, 2-ureido and 2-thiosemicarbazonyl derivatives of diosgenyl β-d-glycosaminosides, for which the results of biological activity tests (antifungal, antibacterial, anti-cancer and hemolytic) are presented.

scholarly journals 3,3-Difluoroallyl ammonium salts: highly versatile, stable and selective gem-difluoroallylation reagents

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Fei Ye ◽  
Yao Ge ◽  
Anke Spannenberg ◽  
Helfried Neumann ◽  
Li-Wen Xu ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Organic Molecules ◽  
Metal Catalysts ◽  
Ammonium Salts ◽  
Direct Reaction ◽  
Selective Synthesis ◽  
Mild Conditions ◽  
Wide Range

AbstractThe selective synthesis of fluorinated organic molecules continues to be of major importance for the development of bioactive compounds (agrochemicals and pharmaceuticals) as well as unique materials. Among the established synthetic toolbox for incorporation of fluorine-containing units, efficient and general reagents for introducing -CF2- groups have been largely neglected. Here, we present the synthesis of 3,3-difluoropropen-1-yl ammonium salts (DFPAs) as stable, and scalable gem-difluoromethylation reagents, which allow for the direct reaction with a wide range of fascinating nucleophiles. DFPAs smoothly react with N-, O-, S-, Se-, and C-nucleophiles under mild conditions without necessity of metal catalysts with exclusive regioselectivity. In this way, the presented reagents also permit the straightforward preparation of many analogues of existing pharmaceuticals.

Recent Developments on Ultrasound-Assisted Synthesis of Bioactive N-Heterocycles at Ambient Temperature

2017 ◽  
Vol 70 (8) ◽  
pp. 872 ◽  
Author(s):  
Bubun Banerjee
Keyword(s):  
Ambient Temperature ◽  
Organic Synthesis ◽  
Ultrasonic Irradiation ◽  
Room Temperature ◽  
Biological Activities ◽  
Reaction Conditions ◽  
Biologically Relevant ◽  
Naturally Occurring ◽  
Recent Developments ◽  
Ultrasound Assisted

N-Heterocycles represent privileged structural subunits well distributed in naturally occurring compounds with immense biological activities. The last decade has seen a tremendous practice to carry out reactions at ambient temperature avoiding harsh reaction conditions. By applying ultrasonic radiation in organic synthesis we can make synthetic protocols more sustainable and can carry out reactions at room temperature avoiding the traditional thermal harsh reaction conditions. Therefore the synthesis of biologically relevant N-heterocycles at room temperature under the influence of ultrasonic irradiation is one of the advancing areas in the 21st century among organic chemists. The present review summarises the latest developments on ultrasound-assisted synthesis of biologically relevant N-heterocycles at ambient temperature.

scholarly journals A Comprehensive Review on Anti-Inflammatory Activity of The Traditional Plants Plumbago zeylanica(Chitra)

2021 ◽  
Vol 22 (1) ◽  
Keyword(s):  
Bioactive Compounds ◽  
Pharmacological Action ◽  
Comprehensive Understanding ◽  
High Demand ◽  
Plumbago Zeylanica ◽  
Wide Range ◽  
Anti Cancer ◽  
Long Time ◽  
Medicinal Properties ◽  
Anti Inflammatory

Medicinal plants have long been utilised as a source of medicine and are in high demand throughout the world. They've been around for a long time, and they've been utilised to cure and prevent ailments. Plumbago zeylanica is a medicinal plant that is frequently utilised for its medicinal properties. It contains several bioactive compounds like napthoquinones, flavonoids, alkaloids, glycosides, steroids, tri-terpenoids, tannins, fixed oils, fats, proteins, etc. among all plumbagin is most important bioactive compounds. It possesses wide range of pharmaceutical activities such as anti-inflammatory, antimicrobial, anti-cancer, anti-ulcer, antidiabetic etc. Several investigations on its pharmacological activity have been conducted. The goal of this review is to provide a comprehensive understanding of P. zeylanica's chemical composition and pharmacological action.

Flavonoids from marine-derived actinobacteria as anticancer drugs

2020 ◽  
Vol 26 ◽  
Author(s):  
Wael N. Hozzein ◽  
Mohamed Mohany ◽  
Sana M.M. Alhawsawi ◽  
Mohamed Y. Zaky ◽  
Salim S. Al-Rejaie ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Anticancer Agents ◽  
De Novo ◽  
Biological Activities ◽  
Anticancer Activities ◽  
Marine Actinobacteria ◽  
Screening Programs ◽  
Structures And Properties ◽  
Wide Range ◽  
Anti Cancer

: Flavonoids represent a large diverse group of natural products that are used as a traditional medicine against various infectious diseases. They possess many biological activities including antimicrobial, antioxidant, antiinflammatory, anti-cancer and anti-diabetic. Commercially Flavonoids are mainly obtained from plants, however, several challenges faced that production. Microorganisms have been known as natural sources of a wide range of bioactive compounds including flavonoids. Actinobacteria are the most prolific group of microorganisms for the production of bioactive secondary metabolites hold many advantages for the production of flavonoids. The screening programs for bioactive compounds revealed the potential application of actinobacteria to produce flavonoids with interesting biological activities, especially anticancer activities. Since marine actinobacteria are recognized as a potential source of novel anticancer agents, they are highly expected to be potential producers of anticancer flavonoids with unusual structures and properties. In this review, we highlight the production of flavonoids by actinobacteria through classical fermentation, engineering of plant biosynthetic genes in a recombinant actinobacterium and the de novo biosynthesis approach. Through these approaches we can control and improve the production of interesting flavonoids or their derivatives for cancer treatment.

Ionic Liquid Assisted C-C Bond Formation

2020 ◽  
Vol 24 (16) ◽  
pp. 1853-1875
Author(s):  
Mandeep Kaur ◽  
Opinder Kaur ◽  
Rahul Badru ◽  
Sandeep Kaushal ◽  
Pritpal Singh
Keyword(s):  
Ionic Liquids ◽  
Heterogeneous Catalysts ◽  
Bond Formation ◽  
Solvent System ◽  
Solid Support ◽  
Organic Transformations ◽  
Diverse Range ◽  
Bond Forming ◽  
The Past ◽  
Wide Range

With their ability to dissolve inorganic as well as organic materials, ionic liquids have emerged as a versatile solvent system for a diverse range of organic transformations. In the past few decades, the literature has witnessed remarkable advances in a wide range of organic conversions carried out in the presence of various imidazolium, pyridinium, pyrrolidinium, quinolinium and diazobicyclo-octane based ionic liquids. In the reaction, ionic liquids serve as a solvent, catalyst or sometimes both. In certain cases, they are also modified with metal nanoparticles or complexes to form heterogeneous catalysts or are immobilized onto solid support like agar-agar to act as solid-support catalysts. Reactions catalysed by ionic liquids incorporating chiral catalysts possess the advantageous features of being highly enantioselective and reproducible, besides being economical and easy to handle. In this review, an updated insight regarding the role played by ionic liquids in various C-C bond-forming organic reactions, has been summarized.

scholarly journals Chemocatalytic Conversion of Cellulose into Key Platform Chemicals

2018 ◽  
Vol 2018 ◽  
pp. 1-21 ◽  
Author(s):  
Guangbi Li ◽  
Wei Liu ◽  
Chenliang Ye ◽  
Xiaoyun Li ◽  
Chuan-Ling Si
Keyword(s):  
Heterogeneous Catalysis ◽  
Lignocellulosic Biomass ◽  
Heterogeneous Catalysts ◽  
Value Added ◽  
Direct Conversion ◽  
Reaction Conditions ◽  
Platform Chemicals ◽  
Stable Chemical ◽  
Wide Range ◽  
Sustainable Societies

Chemocatalytic transformation of lignocellulosic biomass to value-added chemicals has attracted global interest in order to build up sustainable societies. Cellulose, the first most abundant constituent of lignocellulosic biomass, has received extensive attention for its comprehensive utilization of resource, such as its catalytic conversion into high value-added chemicals and fuels (e.g., HMF, DMF, and isosorbide). However, the low reactivity of cellulose has prevented its use in chemical industry due to stable chemical structure and poor solubility in common solvents over the cellulose. Recently, homogeneous or heterogeneous catalysis for the conversion of cellulose has been expected to overcome this issue, because various types of pretreatment and homogeneous or heterogeneous catalysts can be designed and applied in a wide range of reaction conditions. In this review, we show the present situation and perspective of homogeneous or heterogeneous catalysis for the direct conversion of cellulose into useful platform chemicals.

The Use of Bio-Active Compounds of Citrus Fruits as Chemopreventive Agents and Inhibitor of Cancer Cells Viability

2020 ◽  
Vol 20 ◽  
Author(s):  
Mahboubeh Tajaldini ◽  
Jahanbakhsh Asadi
Keyword(s):  
Side Effects ◽  
Cancer Treatment ◽  
Bioactive Compounds ◽  
Herbal Medicines ◽  
Citrus Fruits ◽  
Active Compounds ◽  
Chemotherapy Drugs ◽  
New Therapeutic Approaches ◽  
Wide Range ◽  
Anti Cancer

: Common therapy of cancer such as chemotherapy have various side effects for the patients. In recent studies, new therapeutic approaches in cancer treatment are adjuvant therapy, along with a reduction in side effects of chemotherapy drugs. Treatment by herbal medicines may have some advantages over treatment with single purified chemicals, also in the terms of side effects the use of plants in cancer treatment is a more secure method. Citrus fruits are one of the most consumed natural products in the world due to the presence of various metabolites and bioactive compounds, such as phenols, flavonoids and, carotenoids. Bioactive compounds of citrus modulates signaling pathways and interacts with signaling molecules such as apoptotic and cell cycle (P53, P21, etc) and thus have a wide range of pharmacological activities, including anti-inflammatory, anti-cancer and oxidative stress. The findings discussed in this review strongly support their potential as anti-cancer agents. Therefore, the purpose of this review was to review the effects of active compounds in citrus as a therapy agent in cancer treatment.

scholarly journals Recent Developments on the Synthetic and Biological Applications of Chalcones-A Review

2021 ◽  
Vol 12 (1) ◽  
pp. 180-195
Keyword(s):  
Physical Properties ◽  
Scientific Community ◽  
Biological Activities ◽  
Critical Discussion ◽  
Biological Applications ◽  
Wide Range ◽  
Anti Cancer ◽  
The World ◽  
Recent Developments ◽  
Optical Fluorescence

Chalcones are precursors of the biosynthesis of flavonoids present in plants. These motifs serve a wide range of applications, from synthetic to pharmacological to physical spheres. Chalcone derivatives attracted the scientific community all over the world in recent times due to their diversified applications. The presence of reactive α,β-unsaturated carbonyl moiety in chalcones makes them a versatile intermediate in synthesizing various classes of compounds of biological and physical interest. More importantly, the chalcones themselves have been known to possess enormous biological activities and physical properties like semiconductor, non-linear optical, fluorescence, and electronic properties. In this context, the present review summarises the overall developments in the synthetic, pharmacological, and physical applications of chalcones in recent fast. The critical discussion was attempted on the synthetic applications and biological potencies as anti-cancer, antidiabetic, antimicrobial, antioxidant, and anti-inflammatory.

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