scholarly journals Schiff Bases: Interesting Scaffolds with Promising Antitumoral Properties

2021 ◽  
Vol 11 (4) ◽  
pp. 1877
Author(s):  
Domenico Iacopetta ◽  
Jessica Ceramella ◽  
Alessia Catalano ◽  
Carmela Saturnino ◽  
Maria Grazia Bonomo ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Organic Compounds ◽  
Organic Synthesis ◽  
Schiff Bases ◽  
Antitumor Agents ◽  
Biological Activities ◽  
Anti Inflammatory ◽  
Polymer Stabilizers

Schiff bases, named after Hugo Schiff, are highly reactive organic compounds broadly used as pigments and dyes, catalysts, intermediates in organic synthesis, and polymer stabilizers. Lots of Schiff bases are described in the literature for various biological activities, including antimalarial, antibacterial, antifungal, anti-inflammatory, and antiviral. Schiff bases are also known for their ability to form complexes with several metals. Very often, complexes of Schiff bases with metals and Schiff bases alone have demonstrated interesting antitumor activity. Given the innumerable vastness of data regarding antitumor activity of all these compounds, we focused our attention on mono- and bis-Schiff bases alone as antitumor agents. We will highlight the most significant examples of compounds belonging to this class reported in the literature.

4-Formylpyrazoles: Applications in Organic Synthesis

2019 ◽  
Vol 16 (2) ◽  
pp. 193-203 ◽  
Author(s):  
Renu Bala ◽  
Poonam Kumari ◽  
Sumit Sood ◽  
Karan Singh
Keyword(s):  
Organic Compounds ◽  
Organic Synthesis ◽  
Schiff Bases ◽  
Biological Activities ◽  
Building Blocks

4-Formylpyrazoles are useful building blocks in organic synthesis. This review focuses on the applications of 4-formylpyrazoles to generate a large variety of organic compounds and heterocycles such as Schiff bases, pyrazolylpyrazolines, pyrazoloquinolinones, 4H-pyrazolopyran, pyrazolylbenzoxazole, pyrazolothiadiazepines, pyrazolyloxazolone, pyrazolyloxadiazolines, pyrazolylthiadiazolines, imidazolylpyrazoles, pyrazolopyridines, chromenopyrazolones, thiopyranothiazolylpyrazoles and many others. Many of these molecules exhibit excellent biological activities.

Study of the structure–bioactivity relationship of three new pyridine Schiff bases: synthesis, spectral characterization, DFT calculations and biological assays

2018 ◽  
Vol 42 (11) ◽  
pp. 8851-8863 ◽  
Author(s):  
Alexander Carreño ◽  
César Zúñiga ◽  
Dayán Páez-Hernández ◽  
Manuel Gacitúa ◽  
Rubén Polanco ◽  
...  
Keyword(s):  
Dft Calculations ◽  
Organic Synthesis ◽  
Schiff Bases ◽  
Biological Activities ◽  
Spectral Characterization ◽  
Biological Assays ◽  
Antifungal Properties ◽  
Relationship Of

Schiff bases exhibit a broad range of applications, including their use as catalysts, stabilizers, dyes, and intermediates in organic synthesis; and biological activities, such as antifungal properties.

scholarly journals Screening of Antibacterial, Thrombolytic, Membrane Stabilizing, Anti-inflammatory and Antitumor Activity of Citrus assamensis Leaf Extracts

2018 ◽  
Vol 10 (2) ◽  
pp. 195-210
Author(s):  
M. Shahriar ◽  
M. A. Bhuiyan ◽  
M. S. Rana
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Chloroform Extract ◽  
Haemolytic Activity ◽  
Hypotonic Solution ◽  
Leaf Extracts ◽  
Thrombolytic Activity ◽  
Anti Inflammatory

The methanol, ethanol and chlorofom leaf extracts of Satkara, Citrus assamensis (family: Rutaceae), were subjected to in vitro anti-bacterial, thrombolytic, membrane stabilizing and in vivo anti-inflammatory and antitumor activity tests. The chloroform extract of C. assamensis showed the most important spectrum of activity against Bacillus subtilis, Bacillus cereus, Sarcina lutea among 6 gram positive and against 11 gram negative bacteria at the concentration of 1000 μg/disc, while the range of zones of inhibition were within 7-16 mm. Among the tested three extracts CHCl3 extract showed potent thrombolytic activity and hypotonic solution induced haemolytic activity where the percentages of inhibition were found to be 35% and 55% respectively. All the extracts established significant (p<0.05) anti-inflammatory effect by regulating biphasic inflammatory process induced by carrageenan. The leaf extract dose-dependently and significantly decreases the number of EAC cell count and inhibition of cell growth in comparison to the EAC control and standard. The results obtained in the present study indicate that, C. assamensis leaf can be a potential source of anti-bacterial, thrombolytic, membrane stabilizing, anti-inflammatory and antitumor agents.

An Overview on Pyranocoumarins: Synthesis and Biological Activities

2020 ◽  
Vol 23 (24) ◽  
pp. 2679-2721 ◽  
Author(s):  
Evangelia-Eirini N. Vlachou ◽  
Konstantinos E. Litinas
Keyword(s):  
Organic Compounds ◽  
Antifungal Agents ◽  
Biological Activities ◽  
Biological Properties ◽  
Pyran Ring ◽  
Naturally Occurring ◽  
Anti Cancer ◽  
Anti Inflammatory ◽  
Antibacterial And Antifungal ◽  
Anti Hiv

Pyrano- and dipyranocoumarins are classes of naturally occurring organic compounds with very interesting biological activities. This review focuses on the synthetic strategies for the synthesis of pyranocoumarins and dipyranocoumarins and the biological properties of those compounds. The synthesis involves the formation of the pyran ring, at first, from a coumarin or the formation of pyranone moiety from an existing pyran. Pyranocoumarins and dipyranocoumarins present anti-HIV, anti-cancer, neuroprotective, antidiabetic, antibacterial, antifungal, anti-inflammatory activities. Especially khellactones and calanolides are usually potent and selective in anti-HIV activity. Decursin and decursinol derivatives are effective as anticancer, neuroprotective, antidiabetic, antibacterial, and antifungal agents.

Overview of Coumarins and its Derivatives: Synthesis and Biological Activity

2020 ◽  
Vol 17 ◽  
Author(s):  
Tanvi Sahni ◽  
Sunita Sharma ◽  
Diksha Verma ◽  
Pardeep Kaur
Keyword(s):  
Biological Activity ◽  
Pharmaceutical Industry ◽  
Schiff Bases ◽  
Enzyme Inhibitors ◽  
Biological Activities ◽  
Anti Inflammatory

Abstract: Coumarin is a heterocyclic scaffold and its derivatives namely Schiff bases, esters, and hydrazides, etc, play an important role in the field of agrochemical and pharmaceutical industry due to its structure. Over the years, various biological activities like antifungal, antimicrobial, anti-viral, anti-cancerous, anti-tumor, anti-inflammatory, anti-filarial, enzyme inhibitors, anti-aflatoxigenic, analgesics, antioxidant and Oestrogenic, etc had been analyzed. This review covers the latest literature and knowledge on the synthetic procedures for various coumarin and its derivatives, biological and pharmacological applications.

Tetralone scaffolds and their potential therapeutic applications

2020 ◽  
Vol 17 ◽  
Author(s):  
Bhagwati Gauni ◽  
Krunal Mehariya ◽  
Anamik Shah ◽  
Srinivas Murty Duggirala
Keyword(s):  
Antitumor Activity ◽  
Organic Synthesis ◽  
Small Molecule ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Acetylcholinesterase Inhibitors ◽  
Building Blocks ◽  
Structural Features ◽  
Therapeutic Applications ◽  
Small Molecule Library

: Substituted tetralones have played a substantial role in organic synthesis due to their strong reactivity and suitability as a starting material for a range of synthetic heterocyclic compounds, pharmaceuticals along with biological activities as well as precursors of many natural products and their derivatives. Many α-tetralone derivatives are building blocks, that have been used in the synthesis of therapeutically functional compounds like some antibiotics, antidepressants, acetylcholinesterase inhibitors effective for treating Alzheimer’s disease and alkaloids possessing antitumor activity. In this review, there has been an attempt to explore the small molecule library having α-tetralone scaffold along with their diverse biological activities. Structural features of α-tetralone derivatives responsible for potential therapeutic applications are also described.

scholarly journals A REVIEW: THIAZINES DERIVATIVES TREATED AS POTENTIAL ANTIMICROBIAL AGENTS

2016 ◽  
Vol 10 (1) ◽  
pp. 43 ◽  
Author(s):  
Praveen Kumar Sharma ◽  
Reena Makkar
Keyword(s):  
Natural Products ◽  
Organic Compounds ◽  
Heterocyclic Compounds ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Natural World ◽  
Antimicrobial Activities ◽  
Pharmacological Activities ◽  
Strong Reflection ◽  
Anti Inflammatory

ABSTRACTIn recent days, heterocycles and their derivatives have become strong reflection in medicinal research and pharmaceutical fields because of theirpractical pharmacological and biological activities. Organic compounds; mainly heterocyclic compounds are wealthy in natural world and containextra value because their structural subunits are established in many natural products such as enzymes, vitamins, antibiotics, acids, and hormones.Thiazine nucleuses found in compounds have variety of pharmacological activities such as antitumor, antimicrobial, antibacterial, antifungal, antiviral,and anti-inflammatory. This review spotlight on the substituted thiazines with possible antimicrobial activities that are at the present in development.Keywords: Antibacterial, Substituted thiazines, Antimicrobial agents.

scholarly journals Chiral Flavonoids as Antitumor Agents

2021 ◽  
Vol 14 (12) ◽  
pp. 1267
Author(s):  
Cláudia Pinto ◽  
Honorina Cidade ◽  
Madalena Pinto ◽  
Maria Elizabeth Tiritan
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Biological Activities ◽  
Structural Diversity ◽  
Building Blocks ◽  
Inhibitory Effect ◽  
Chiral Molecules ◽  
Growth Inhibitory ◽  
Synthetic Approaches

Flavonoids are a group of natural products with a great structural diversity, widely distributed in plant kingdom. They play an important role in plant growth, development and defense against aggressors. Flavonoids show a huge variety of biological activities such as antioxidant, anti-inflammatory, anti-mutagenic, antimicrobial and antitumor, being able to modulate a large diversity of cellular enzymatic activities. Among natural flavonoids, some classes comprise chiral molecules including flavanones, flavan-3-ols, isoflavanones, and rotenoids, which have one or more stereogenic centers. Interestingly, in some cases, individual compounds of enantiomeric pairs have shown different antitumor activity. In nature, these compounds are mainly biosynthesized as pure enantiomers. Nevertheless, they are often isolated as racemates, being necessary to carry out their chiral separation to perform enantioselectivity studies. Synthetic chiral flavonoids with promising antitumor activity have also been obtained using diverse synthetic approaches. In fact, several new chiral bioactive flavonoids have been synthesized by enantioselective synthesis. Particularly, flavopiridol was the first cyclin-dependent kinase (CDK) inhibitor which entered clinical trials. The chiral pool approaches using amino acid as chiral building blocks have also been reported to achieve small libraries of chrysin derivatives with more potent in vitro growth inhibitory effect than chrysin, reinforcing the importance of the introduction of chiral moieties to improve antitumor activity. In this work, a literature review of natural and synthetic chiral flavonoids with antitumor activity is reported for the first time.

Versatile Synthesis of Organic Compounds Derived from Ascorbic Acid.

2021 ◽  
Vol 08 ◽  
Author(s):  
Aparna Das ◽  
Bimal Krishna Banik
Keyword(s):  
Ascorbic Acid ◽  
Vitamin C ◽  
Organic Compounds ◽  
Organic Synthesis ◽  
Biological Activities ◽  
Wide Range ◽  
Derivatives Of

: Ascorbic acid, also known as Vitamin C, is the essential vitamin observed in diverse food. Ascorbic acid has various applications in several fields. Studies have depicted that in organic synthesis, it can be used as a mediator or substrate. The derivatives of ascorbic acid have been found to possess numerous biological activities. In this review, we report the crucial derivatives of ascorbic acid, which have significant biological activities. Various studies are considered in this review to prove its wide range of availability.

Synthesis of thiazolyl-N-phenylmorpholine derivatives and their biological activities

2020 ◽  
Vol 16 ◽  
Author(s):  
Amerah M. Al-Soliemy ◽  
Thoraya A. Farghaly ◽  
Eman M. H. Abbas ◽  
Mohamed R. Shaaban ◽  
Mohie E. M. Zayed ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Tumor Cells ◽  
Antitumor Agents ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Thiazole Derivatives ◽  
Design And Synthesis ◽  
Good Potential ◽  
Potent Growth ◽  
Mcf 7

Background: Morpholine and thiazole rings are two heterocycles which well-known with wide spectrum of different biological activities especially antitumor activity. Objective: The aim of the work is to design and synthesis hybrid heterocyclic compounds of morpholine and thiazole moieties via the reaction of morpholino-thiosemicarbazone derivatives with various αhalocarbonyl compounds and screening their antitumor activity against three tumor cell lines namely, TK-10, MCF-7 and UACC-62. Method: An efficient synthesis of a series of Nphenylmorpholine derivatives linked with thiazole moiety were accomplished. The reaction of Nsubistituted-2-(N-phenylmorpholine)ethylidene)hydrazine-1-carbothioamide (thiosemicarbazone derivative) with acetyl and ester-hydrazonoyl chlorides, α-chloroketones, or α-bromoesters afforded the corresponding thiazole derivatives pendent to N-phenylmorpholine moiety in good to excellent yields. Result: Mass, 1 H NMR, 13C NMR, and elemental analysis were used to confirm the structure of all the new derivatives. The antitumor activities of synthesized Nphenylmorpholine-thiazole derivatives were investigated against three tumor cells namely, TK-10, MCF-7 and UACC-62. The results of such investigation indicated that some derivatives showed good potential to inhibit the growth of the two cells of the tested tumor cells. Surprise, one of the tested compounds, N-methyl thiosemicarbazone derivative 7 revealed potent growth inhibition of all the three tumor cells. Conclusion: We have succeeded to synthesize a series of Nphenylmorpholine derivatives pendant to thiazole moiety as antitumor agents.

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