Naturally Occurring O-heterocycles as Anticancer Agents

Author(s):  
Satya Kumar Avula ◽  
Biswanath Das ◽  
Rene Csuk ◽  
Ahmed Al-Harrasi

: Cancer is a leading cause of death worldwide. Proper efficient drugs are required to treat this deadly disease. Natural products have long been a vital source of anticancer agents and they have generated various “lead compounds” suitable for drug developments. With the recent advancement of chemical synthesis and bioevaluation techniques these lead compounds of natural origins have been utilized for production of useful anticancer drugs. Among the naturally occurring bioactive compounds various O-heterocycles have been evaluated as remarkable cancer therapeutic agents. These compounds generally possess unique structures and novel mechanism of action. In the present review article, some selected O-heterocycles as promoting anticancer agents have been discussed in brief. Various natural sources and chemistry as well as bioactivities of these compounds have been described. The development of improved analogues of these compounds through synthetic modifications and efficient bioevaluation along with proper studies on structure-activity relationship and mechanism of actions has been mentioned. The article has demonstrated the recent relevance of naturally occurring O-heterocyclic compounds in current anticancer drug discovery and development scenario.

Author(s):  
Rakesh Sahu ◽  
Rakhi Mishra ◽  
Rajnish Kumar ◽  
Salahuddin ◽  
Chandana Majee ◽  
...  

: The incidence of cancer is increasing worldwide, affecting a vast majority of the human population. As new different anticancer agents are being developed now, the requirement is to deal somehow with them and evaluate their safety. Among them, pyridine based drugs are contributing a lot, as it is one of the imperative pharmacophores occurring synthetically as well as naturally in heterocyclic compounds, and having a wide range of therapeutic applications in the area of drug discovery, thereby offering many chances for further improvement in antitumor agents via acting onto numerous receptors of extreme prominence. Many pyridine derivatives have been reported to inhibit enzymes, receptors and many other targets for controlling and curing the global health issue of cancer. Nowadays, in combination with other moieties, researchers are focusing on the development of pyridine-based new derivatives for cancer treatment. Therefore, this review sheds light on the recent therapeutic expansions of pyridine together with its molecular docking, structure-activity-relationship, availability in the market, and a summary of recently patented and published research works that shall jointly help the scientists to produce effective drugs with the desired pharmacological activity.


Author(s):  
Ashmit Gill ◽  
Somi Patranabis

The global burden of cancer is projected to have more than doubled over the next two decades, raising the prospect of a significant investment in health systems, thus posing a real medical problem. The increasing number of people with cancer highlights the need for more cancer prevention efforts. An established history exists for plant-derived compounds as effective anticancer agents. More recently, several phytohormones have been assessed for their ability to inhibit the growth and survival of human cancer cell lines. Phytohormones or plant hormones are chemical messengers responsible for harmonizing various cellular activities that revolves around growth, development, and stress-response. The aim of this literature review article is to present the current state of knowledge concerning the several naturally occurring phytohormones which have shown enormous potential in the prevention and treatment of variety of different type of cancers.


Author(s):  
Firdayani Firdayani ◽  
Susi Kusumaningrum ◽  
Doddy Irawan Setyo Utomo ◽  
Agung Eru Wibowo ◽  
Chaidir Chaidir

Rocaglamide derivatives are the compounds which have featuring cyclopenta[b]tetra-hydrobenzofuran skeleton. Until now it includes more than 50 naturally occurring derivatives. They were chosen to be interesting candidates for possible therapeutic agents primarily in the field of cancer chemotherapy due to their cytotoxic activities data against various cancer cells. A quantitative structure activity relationship (QSAR) studies were done to investigate physicochemical properties of molecule which contribute to their activities. Series of rocaglamide derivatives have been used and analyzed using linear free energy regression Hansch model for their cytotoxic activities against MONO-MAC-6 leukemia cells, RAJI lymphoma cells and MEL-JUSO melanoma cells. Results showed that the best QSAR equations were revealed involving C Log P and CMR parameters with nonlinear regression relationships in cytotoxic activities of rocaglamide derivatives against cancer cells above. Keywords: QSAR, Rocaglamide, LFER Hansch


2018 ◽  
Vol 15 (8) ◽  
pp. 1043-1072 ◽  
Author(s):  
Hamzeh Kiyani

Background: The majority of naturally occurring compounds, pharmaceuticals, and drug-candidate molecules possess heterocyclic scaffolds. In this context, tetrahydobenzo[b]pyrans are of considerable importance. In the line with the synthesis of these valuable heterocyclic compounds, the researchers tried to synthesize these molecules using different organocatalysts. The development of new strategies for three-component condensation of dimedone, various aldehydes and malononitrile for construction of tetrahydrobenzo[b]pyrans is of particular interest to organic chemists and pharmacologists. Objective: In this review, three-component catalyzed synthesis of tetrahydrobenzo[b]pyran compounds is introduced, focusing on the developments in the use of organocatalysts. Organocatalytic approaches were investigated for the synthesis of tetrahydrobenzo[b]pyrans. This contribution covers the literature concerning the synthesis of heterocycles referred to, in recent times. Conclusion: This review article is associated with the study of the three-component synthesis of tetrahydrobenzo[b]pyrans using organocatalysts. This review also provides an insight into the importance of these heterocycles. In the vast majority of these reactions, water and water-ethanol system have been used as green solvent media for implementation of them. The use of green solvents, the development of less toxic and promising reagents/catalysts as well as the design of inexpensive and reliable approaches are some of the principles of green chemistry, and most of the methods are benefited from them. Tetrahydrobenzo[b]pyrans and organocatalysts open avenue ofnew horizons. The recyclability of the many of these organocatalysts offers an additional merit for the use of these catalysts in 3-CR of aldehydes, dimedone, and malononitrile reactions.


2020 ◽  
Vol 26 (1) ◽  
pp. 46-59 ◽  
Author(s):  
Ali Irfan ◽  
Laila Rubab ◽  
Mishbah Ur Rehman ◽  
Rukhsana Anjum ◽  
Sami Ullah ◽  
...  

AbstractCoumarin sulfonamide is a heterocyclic pharmacophore and an important structural motif which is a core and integral part of different therapeutic scaffolds and analogues. Coumarin sulfonamides are privileged and pivotal templates which have a broad spectrum of applications in the fields of medicine, pharmacology and pharmaceutics. Coumarin sulfonamide exhibited versatile and myriad biomedical activities such as anti-bacterial, antiviral, antifungal, anti-inflammatory and anti-cancer. This review article focuses on the structural features of coumarin sulfonamide derivatives in the treatment of different lethal diseases on the basis of structure-activity relationships (SAR). The plethora of research cited in this review article summarizes and discusses the various substitutions around the coumarin sulfonamide nucleus which have provided a wide spectrum of biological activities and therapeutic potential that has proved attractive to many researchers looking to exploit the coumarin sulfonamide skeleton for drug discovery and the development of novel therapeutic agents.


Author(s):  
Gangqiang Wang ◽  
Shaofa Sun ◽  
Bin Wu ◽  
Jikai Liu

: Cancer is the main cause of death, and the emergence of resistance by cancer cells towards existing anticancer agents is one of the major problems for effective chemotherapy, creating a great demand for the development of novel anticancer drugs. Coumarins, abundantly found in nature, constitute an important class of pharmacological agents pos-sessing physiological activities. The mechanism investigations elucidated that coumarins could lead to self-programmed cancer cell death (apoptosis) via different mechanisms, thereby coumarin-based derivatives possess potential activity against various forms of cancers including drug-resistant even multidrug-resistant cancers. This review article describes the recent progress in the discovery, structural modification, structure-activity relationship, and mechanism of action studies of cou-marin-based derivatives with potential activity against drug-resistant cancers, covering articles published between 2010 and 2020.


Planta Medica ◽  
2019 ◽  
Vol 85 (11/12) ◽  
pp. 802-814 ◽  
Author(s):  
Yulin Ren ◽  
A. Douglas Kinghorn

Triterpenoids are distributed widely in higher plants and are of interest because of their structural diversity and broad range of bioactivities. In particular, there is a very large literature on the propensity of a variety of triterpenoids to act as potential anticancer agents. In the present review, the anticancer potential is summarized for naturally occurring triterpenoids and their semi-synthetic derivatives, including examples of lupane-, oleanane-, ursane-, and cucurbitane-type pentacyclic triterpenoids, along with dammarane-type tetracyclic triterpenes including ginsenosides and their sapogenins and dichapetalins, which have been characterized as antitumor leads from higher plants. Preliminary structure-activity relationships and reported mechanisms of the antineoplastic-related activity are included. Prior studies for triterpenoids of plant origin are supportive of additional work being conducted on the more detailed biological and mechanistic evaluation for the progression of this type of natural products as possible cancer chemotherapeutic agents.


2009 ◽  
Vol 62 (7) ◽  
pp. 624 ◽  
Author(s):  
Ian Paterson ◽  
Alison D. Findlay

A growing number of complex polyketides, isolated from a variety of marine and terrestrial sources, present novel scaffolds for the development of cancer therapeutic agents. However, the low natural abundance of such lead compounds often precludes full biological evaluation, which demands the development of efficient synthetic routes to afford a sustainable supply. In this account, we provide an overview of the total synthesis of several representative anticancer polyketides – dolastatin 19, spirangien A, reidispongiolide A, and spongistatin 1/altohyrtin A – based on versatile aldol methodology developed in our group.


2021 ◽  
Vol 28 ◽  
Author(s):  
Alessia Catalano ◽  
Domenico Iacopetta ◽  
Jessica Ceramella ◽  
Carmela Saturnino ◽  
Maria Stefania Sinicropi

: A huge number of nitrogen-containing heterocyclic compounds are ubiquitous in natural products, pharmaceuticals, and bioactive molecules. Among these, the pyranoindole represents an important structural motif, as it constitutes the central subunit in both the biologically active natural products and therapeutic agents. Talathermophilins, notoamides, norgeamides, carneamides, and versicamides are examples of naturally occurring pyranoindoles, while the well-known etodolac and pemedolac are a tetrahydropyrano[3,4-b]indole deriving from synthetic procedures. Besides the well-known antiinflammatory and fibrinolytic activity, molecules comprising the pyranoindole framework have been demonstrated to exhibit various biological activities, such as antiulcer, antidepressant, analgesic, and antiproliferative. Herein, we report the most common natural and synthetic products bearing a pyranoindole nucleus, their syntheses, and biological activities.


Author(s):  
D. Gowtham Kumar ◽  
Naresh R ◽  
K. Rakesh Varma ◽  
Nagasen D ◽  
Sudheer B ◽  
...  

Nanoparticles with naturally occurring biodegradable polymers have emerged as potential carriers of various therapeutic agents. Chitosan, a cationic polysaccharide, is one of such biodegradable polymers, which has been extensively exploited for the preparation of nanoparticles with several therapeutic agents. In recent years, the area of focus has shifted from chitosan to chitosan derivatized polymers due to its vastly improved properties such as better drug retention capability, improved permeation, enhanced mucoadhesion, and sustained release of therapeutic agents. Chitosan derivatized polymers are primarily the quaternized chitosan derivatives, chitosan cyclodextrin complexes, thiolated chitosan, pegylated chitosan, chitosan combined with sugar ligands, chitosan with cholanic acid, chitosan-linolenic acid and chitosan-DTPA. This review article covers the various modifications of chitosan, their preparation procedures and various works done with them.   


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