A Study on Camphor Derivatives and Its Applications: A Mini-Review

2021 ◽  
Vol 25 ◽  
Author(s):  
Bendi Anjaneyulu ◽  
Sangeeta ◽  
Naina Saini
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Low Cost ◽  
Starting Material ◽  
Biologically Active ◽  
Camphor Sulfonic Acid ◽  
Anti Cancer ◽  
Camphor Derivatives ◽  
Enantiospecific Synthesis ◽  
Active Substances

: Natural compounds are the prominent sources for the synthesis of abundant biologically active substances in medicinal chemistry. Camphor exists in two enantiomeric forms i.e., R and S, or both, which are readily obtainable. Camphor is a small molecule with chirality property that binds to some active site, together with its low cost and convenience to transform into synthetically useful derivatives and one of the most important monoterpenoids widely spread in plants and has been used as starting material for the various camphor based derivatives which exhibit several biological activities include antimicrobial, antiviral, antioxidant, analgesic and anti-cancer. Many of those simple derivatives are commercially available in the form of camphor sulfonic acid or ketopinic acid that can be easily be produced from camphor. This compound is primarily used as a chiral starting material in the enantiospecific synthesis of natural products is because of its available methods for the direct or indirect introduction of functionality at C-3, C-5, C-8, C-9, and C-10 carbon atoms. In this study, heterocyclic compounds derived from camphor are arranged in different groups as Camphor-Derived Simple Heterocycles, Fused Camphor-Derived Heterocycles, Spiro Camphor-Derived Heterocycles, Ring Expanded Camphor-Derived Heterocycles and Camphor derived metal complexes. This study summarizes the transformations of camphor and its derivatives along with their biological activities.

scholarly journals 2-Acetylbenzimidazole: a Valuable Synthon for the Synthesis of Biologically Active Molecules

2020 ◽  
Vol 11 (4) ◽  
pp. 11562-11591
Keyword(s):  
Heterocyclic Compounds ◽  
Heterocyclic System ◽  
Biological Activities ◽  
Biologically Active ◽  
Online Search ◽  
Convenient Synthesis ◽  
Anti Cancer ◽  
Pharmacological Interest ◽  
Main Motive ◽  
Biological Aspects

Benzimidazole is an important moiety from a medicinal chemistry perspective due to its various biological activities such as antimicrobial, anti-cancer, anti-diabetic, anti-Alzheimers, and anti-inflammatory, etc. 2-acetylbenzimidazole is exploited to obtain various heterocyclic compounds of pharmacological interest. This review's main motive is to present the literature on 2-acetylbenzimidazole chemistry and provide valuable and up-to-date information for its applications. The present review is carried out by compiling literature from 1964 to 2020 concerning the synthesis and biological aspects of various heterocyclic compounds derived from 2-acetylbenzimidazole. Literature was collected from various online search engines viz. Google Scholar, PubMed, Science Direct, Core, and Semantic scholar. 2-acetylbenzimidazole has been successfully employed as a synthon to obtain heterocyclic system viz. oxirane, pyrazoline, thiazole, pyrazole, isoxazoline, isoxazole, pyridine, pyrimidine, thiazine, diazepine, and other miscellaneous rings. 2-acetylbenzimidazole has shown promise for the convenient synthesis of various heterocyclic compounds. The reactions can be carried out on various reactive sites of 2-acetylbenzimidazole, which are the carbonyl group and the amino group. This review will help to explore various heterocyclic compounds and particularly in the synthesis of biologically useful compounds.

Utility of Certain 2-Furanone Derivatives for Synthesis of Different Heterocyclic Compounds and Testing their Anti-cancer Activity

2021 ◽  
Vol 17 ◽  
Author(s):  
Rania Helmy Abd El-Hameed ◽  
Hend Medhat El-Shanbaky ◽  
Mosaad Sayed Mohamed
Keyword(s):  
Cell Lines ◽  
Heterocyclic Compounds ◽  
Development Process ◽  
Biological Activities ◽  
Biologically Active ◽  
Cytotoxic Agents ◽  
Inhibition Activity ◽  
Small Cell Lung ◽  
Anti Cancer ◽  
Hct 116

Background: 2-Furanones attracted great attention due to their biological activities. They also have the ability to convert to several biologically active heterocyclic and non-heterocyclic compounds, especially as anti-cancer agents. Objectives: This research aims to assist in the development process of novel cytotoxic agents through synthesizing certain 2-furanone derivatives, using them as starting materials for the preparation of novel heterocyclic and non-heterocyclic compounds, and then testing the synthesized derivatives for their anti-cancer activities. Methods: All the newly synthesized compounds were fully characterized by elemental analysis, IR, Mass, and 1H-NMR spectroscopy. 18 synthesized compounds were selected by National Cancer Institute (NCI) for testing against 60 cell lines, and the active compound was tested as MAPK14 and VEGFR2-inhibitor using Staurosporine as standard. Results: Compound 3a showed higher activity against several cell lines, including leukemia (SR), Non-Small Cell Lung Cancer (NCI-H460), colon cancer (HCT-116), ovarian cancer (OVCAR-4), renal cancer (786-0, ACHN and UO-31), and finally breast cancer (T-47D). It also had better inhibition activity against MAPK14 than the used reference. Conclusion: Compound 3a has promising anti-cancer activities compared to the used standards and may need further modifications and investigations.

scholarly journals Study of antioxidant activity of selected monocarbohydrazone derivatives

2021 ◽  
Vol 62 (1) ◽  
pp. 5-8
Author(s):  
Gorana Mrđan ◽  
Borko Matijević ◽  
Sanja Vlaisavljević ◽  
Đenđi Vaštag ◽  
Suzana Apostolov
Keyword(s):  
Sulfonic Acid ◽  
Biological Activities ◽  
Biologically Active ◽  
Radical Scavengers ◽  
Antioxidant Power ◽  
Antioxidant Agents ◽  
Wide Range ◽  
Anti Cancer ◽  
Ferric Reducing Antioxidant Power ◽  
Active Substances

Many of carbohydrazone derivatives have shown a wide range of biological activities. In previous studies, these compounds have proven to be excellent anti-cancer, antitumor, antibacterial, antimicrobial and antioxidant agents. Monocarbohydrazones, as one of the carbohydrazone derivatives, have been slightly explored. Due to that reason, in this study, eight newly synthesized monocarbohydrazones were subjected to examinations by the use of three antioxidant tests. To determine the effectiveness of monocarbohydrazone as potential radical scavengers, DPPH (2,2-Diphenyl-1-picrylhydrazyl), ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) and FRAP (Ferric Reducing Antioxidant Power) assays were used. The obtained results could open the door for further studies of these compounds as biologically active substances.

Biologically Active 2,5-Disubstituted-1,3,4-Oxadiazoles

2009 ◽  
Vol 2 (1) ◽  
pp. 390-406
Author(s):  
Harish Rajak ◽  
Murli Dhar Kharya ◽  
Pradeep Mishra
Keyword(s):  
Heterocyclic Compounds ◽  
Medical Literature ◽  
Biological Activities ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Clinical Use ◽  
Synthetic Drugs ◽  
Physiologic Activity ◽  
Pharmacologically Active

There are vast numbers of pharmacologically active heterocyclic compounds in regular clinical use. The presence of heterocyclic structures in diverse types of compounds is strongly indicative of the profound effects such structure exerts on physiologic activity, and recognition of this is abundantly reflected in efforts to find useful synthetic drugs. The 1,3,4-oxadiazole nucleus has emerged as one of the potential pharmacophore responsible for diverse pharmacological properties. Medical Literature is flooded with reports of a variety of biological activities of 2,5-Disubstituted-1,3,4-oxadiazoles. The present work is an attempt to summarize and enlist the various reports published on biologically active 2,5-disubstituted-1,3,4-oxadiazoles.

Oxazole-Based Compounds As Anticancer Agents

2020 ◽  
Vol 26 (41) ◽  
pp. 7337-7371 ◽  
Author(s):  
Maria A. Chiacchio ◽  
Giuseppe Lanza ◽  
Ugo Chiacchio ◽  
Salvatore V. Giofrè ◽  
Roberto Romeo ◽  
...  
Keyword(s):  
Cancer Research ◽  
Drug Discovery ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Chemical Diversity ◽  
Biologically Active ◽  
New Drugs ◽  
The Core ◽  
Anti Cancer ◽  
Biologically Active Derivatives

: Heterocyclic compounds represent a significant target for anti-cancer research and drug discovery, due to their structural and chemical diversity. Oxazoles, with oxygen and nitrogen atoms present in the core structure, enable various types of interactions with different enzymes and receptors, favoring the discovery of new drugs. Aim of this review is to describe the most recent reports on the use of oxazole-based compounds in anticancer research, with reference to the newly discovered iso/oxazole-based drugs, to their synthesis and to the evaluation of the most biologically active derivatives. The corresponding dehydrogenated derivatives, i.e. iso/oxazolines and iso/oxazolidines, are also reported.

scholarly journals Mangiferin as New Potential Anti-Cancer Agent and Mangiferin-Integrated Polymer Systems—A Novel Research Direction

Biomolecules ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 79
Author(s):  
Svetlana N. Morozkina ◽  
Thi Hong Nhung Vu ◽  
Yuliya E. Generalova ◽  
Petr P. Snetkov ◽  
Mayya V. Uspenskaya
Keyword(s):  
Molecular Mechanisms ◽  
Biological Activities ◽  
Research Direction ◽  
Biological Action ◽  
The Body ◽  
Biologically Active ◽  
Polymer Systems ◽  
Anti Cancer ◽  
Long Time ◽  
Cancer Agent

For a long time, the pharmaceutical industry focused on natural biologically active molecules due to their unique properties, availability and significantly less side-effects. Mangiferin is a naturally occurring C-glucosylxantone that has substantial potential for the treatment of various diseases thanks to its numerous biological activities. Many research studies have proven that mangiferin possesses antioxidant, anti-infection, anti-cancer, anti-diabetic, cardiovascular, neuroprotective properties and it also increases immunity. It is especially important that it has no toxicity. However, mangiferin is not being currently applied to clinical use because its oral bioavailability as well as its absorption in the body are too low. To improve the solubility, enhance the biological action and bioavailability, mangiferin integrated polymer systems have been developed. In this paper, we review molecular mechanisms of anti-cancer action as well as a number of designed polymer-mangiferin systems. Taking together, mangiferin is a very promising anti-cancer molecule with excellent properties and the absence of toxicity.

Synthesis of biologically active heterocyclic compounds from allenic and acetylenic nitriles and related compounds

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Marthe Carine Djuidje Fotsing ◽  
Dieudonné Njamen ◽  
Zacharias Tanee Fomum ◽  
Derek Tantoh Ndinteh
Keyword(s):  
Michael Addition ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Biologically Active ◽  
Polycyclic Compounds ◽  
One Step ◽  
Pharmaceutical Properties ◽  
Related Compounds ◽  
Acetylenic Acids ◽  
The Michael Addition

Abstract Cyclic and polycyclic compounds containing moieties such as imidazole, pyrazole, isoxazole, thiazoline, oxazine, indole, benzothiazole and benzoxazole benzimidazole are prized molecules because of the various pharmaceutical properties that they display. This led Prof. Landor and co-workers to engage in the synthesis of several of them such as alkylimidazolenes, oxazolines, thiazolines, pyrimidopyrimidines, pyridylpyrazoles, benzoxazines, quinolines, pyrimidobenzimidazoles and pyrimidobenzothiazolones. This review covers the synthesis of biologically active heterocyclic compounds by the Michael addition and the double Michael addition of various amines and diamines on allenic nitriles, acetylenic nitriles, hydroxyacetylenic nitriles, acetylenic acids and acetylenic aldehydes. The heterocycles were obtained in one step reaction and in most cases, did not give side products. A brief discussion on the biological activities of some heterocycles is also provided.

Sixty Years Young: The Diverse Biological Activities of Metal Polypyridyl Complexes Pioneered by Francis P. Dwyer

2012 ◽  
Vol 65 (9) ◽  
pp. 1325 ◽  
Author(s):  
Nathan L. Kilah ◽  
Eric Meggers
Keyword(s):  
Inorganic Chemistry ◽  
Biological Activities ◽  
Biologically Active ◽  
Ruthenium Polypyridyl ◽  
Polypyridyl Complexes ◽  
Anti Cancer ◽  
Ruthenium Polypyridyl Complexes ◽  
Medicinal Inorganic Chemistry ◽  
Sixtieth Anniversary

Sixty years ago, the Australian chemist Francis P. Dwyer pioneered the use of ruthenium polypyridyl complexes as biologically active compounds. These chemically inert and configurationally stable complexes revealed an astonishing range of interesting biological activities, such as the inhibition of the enzyme acetylcholinesterase, anti-cancer activity in vivo, and bacteriostatic/bacteriocidal action. This review commemorates the sixtieth anniversary of Dwyer and co-workers’ landmark 1952 publication, summarises their broader achievements in biological inorganic chemistry, and discusses the contribution of this work to the development of modern biological and medicinal inorganic chemistry.

scholarly journals Bee Venom: From Venom to Drug

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4941
Author(s):  
Abdelwahab Khalil ◽  
Basem H. Elesawy ◽  
Tarek M. Ali ◽  
Osama M. Ahmed
Keyword(s):  
Molecular Mechanisms ◽  
Biological Activities ◽  
Biologically Active ◽  
Bee Venom ◽  
Bee Sting ◽  
Anti Cancer ◽  
Defensive Substance ◽  
Injectable Form

Insects of the order Hymenoptera have a defensive substance that contains many biologically active compounds. Specifically, venom from honeybees (Apis mellifera) contains many enzymes and peptides that are effective against various diseases. Different research papers stated the possibility of using bee venom (a direct bee sting or in an injectable form) in treating several complications; either in vivo or in vitro. Other reports used the active fractions of bee venom clinically or at labratory scale. Many reports and publications have stated that bee venom and its constituents have multiple biological activities including anti-microbial, anti-protozoan, anti-cancer, anti-inflammatory, and anti-arthritic properties. The present review aims to refer to the use of bee venom itself or its fractions in treating several diseases and counteracting drug toxicities as an alternative protocol of therapy. The updated molecular mechanisms of actions of bee venom and its components are discussed in light of the previous updated publications. The review also summarizes the potential of venom loaded on nanoparticles as a drug delivery vehicle and its molecular mechanisms. Finally, the products of bee venom available in markets are also demonstrated.

scholarly journals Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs

Molecules ◽  
2020 ◽  
Vol 25 (13) ◽  
pp. 3036
Author(s):  
Ashraf A. Aly ◽  
Alaa A. Hassan ◽  
Maysa M. Makhlouf ◽  
Stefan Bräse
Keyword(s):  
Natural Products ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Biologically Active ◽  
Biological Applications ◽  
Active Moiety ◽  
Interesting Class

Mercapto-substituted 1,2,4-triazoles are very interesting compounds as they play an important role in chemopreventive and chemotherapeutic effects on cancer. In recent decades, literature has been enriched with sulfur- and nitrogen-containing heterocycles which are used as a basic nucleus of different heterocyclic compounds with various biological applications in medicine and also occupy a huge part of natural products. Therefore, we shed, herein, more light on the synthesis of this interesting class and its application as a biologically active moiety. They might also be suitable as antiviral and anti-infective drugs.

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