scholarly journals Chalcone Derivatives: Role in Anticancer Therapy

Biomolecules ◽  
2021 ◽  
Vol 11 (6) ◽  
pp. 894
Author(s):  
Yang Ouyang ◽  
Juanjuan Li ◽  
Xinyue Chen ◽  
Xiaoyu Fu ◽  
Si Sun ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Full Description ◽  
Chalcone Derivatives ◽  
Treatment And Prevention ◽  
Convenient Synthesis ◽  
Prevention Of Cancer ◽  
Cell Cycle Disruption

Chalcones (1,3-diaryl-2-propen-1-ones) are precursors for flavonoids and isoflavonoids, which are common simple chemical scaffolds found in many naturally occurring compounds. Many chalcone derivatives were also prepared due to their convenient synthesis. Chalcones as weandhetic analogues have attracted much interest due to their broad biological activities with clinical potentials against various diseases, particularly for antitumor activity. The chalcone family has demonstrated potential in vitro and in vivo activity against cancers via multiple mechanisms, including cell cycle disruption, autophagy regulation, apoptosis induction, and immunomodulatory and inflammatory mediators. It represents a promising strategy to develop chalcones as novel anticancer agents. In addition, the combination of chalcones and other therapies is expected to be an effective way to improve anticancer therapeutic efficacy. However, despite the encouraging results for their response to cancers observed in clinical studies, a full description of toxicity is required for their clinical use as safe drugs for the treatment of cancer. In this review, we will summarize the recent advances of the chalcone family as potential anticancer agents and the mechanisms of action. Besides, future applications and scope of the chalcone family toward the treatment and prevention of cancer are brought out.

Advances on Quinazoline Based Congeners for Anticancer Potential

2021 ◽  
Vol 25 ◽  
Author(s):  
Parul Grover ◽  
Monika Bhardwaj ◽  
Garima Kapoor ◽  
Lovekesh Mehta ◽  
Roma Ghai ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Anticancer Compounds ◽  
In Vivo Models ◽  
Appropriate Treatment

: The heterocyclic compounds have a great significance in medicinal chemistry because they have extensive biological activities. Cancer is globally the leading cause of death and it is a challenge to develop an appropriate treatment for the management of cancer. Continuous efforts are being made to find a suitable medicinal agent for cancer therapy. Nitrogen-containing heterocycles have received noteworthy attention due to their wide and distinctive pharmacological activities. One of the most important nitrogen-containing heterocycles in medicinal chemistry is ‘quinazoline’ that possesses a wide spectrum of biological properties. This scaffold is an important pharmacophore and is considered a privileged structure. The various substituted quinazolines displayed anticancer activity against different types of cancer. This review highlights the recent advances in quinazoline based molecules as anticancer agents. Several in-vitro and in-vivo models used along with the results are also included. A subpart briefing natural quinazoline containing anticancer compounds is also incorporated in the review.

scholarly journals Thiadiazole derivatives as anticancer agents

2020 ◽  
Vol 72 (5) ◽  
pp. 1079-1100 ◽  
Author(s):  
Monika Szeliga
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Cellular Membrane ◽  
Biological Targets ◽  
Cancer Pathogenesis ◽  
Thiadiazole Ring ◽  
Substantial Progress ◽  
Thiadiazole Derivatives

Abstract In spite of substantial progress made toward understanding cancer pathogenesis, this disease remains one of the leading causes of mortality. Thus, there is an urgent need to develop novel, more effective anticancer therapeutics. Thiadiazole ring is a versatile scaffold widely studied in medicinal chemistry. Mesoionic character of this ring allows thiadiazole-containing compounds to cross cellular membrane and interact strongly with biological targets. Consequently, these compounds exert a broad spectrum of biological activities. This review presents the current state of knowledge on thiadiazole derivatives that demonstrate in vitro and/or in vivo efficacy across the cancer models with an emphasis on targets of action. The influence of the substituent on the compounds’ activity is depicted. Furthermore, the results from clinical trials assessing thiadiazole-containing drugs in cancer patients are summarized.

scholarly journals Polyphenols as Key Players for the Antileukaemic Effects of Propolis

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Murtala B. Abubakar ◽  
Wan Zaidah Abdullah ◽  
Siti Amrah Sulaiman ◽  
Boon Suen Ang
Keyword(s):  
Cell Lines ◽  
Biological Activities ◽  
Epidemiological Studies ◽  
Leukaemia Cell ◽  
Phenolic Contents ◽  
Treatment And Prevention ◽  
History Of ◽  
Cell Growth And Proliferation

Propolis (a bee product) which has a long history of medicinal use by humans has attracted a great deal of research interest in the recent time; this is due to its widely reported biological activities such as antiviral, antifungal, antibacterial, anti-inflammatory, antioxidant, and anticarcinogenic properties. Crude form of propolis and its phenolic contents have both been reported to exhibit antileukaemic effects in various leukaemia cell lines. The ability of the polyphenols found in propolis to arrest cell cycle and induce apoptosis and differentiation in addition to inhibition of cell growth and proliferation makes them promising antileukaemic agents, and hence, they are believed to be a key to the antileukaemic effects of propolis in different types of leukaemia. This paper reviews the molecular bases of antileukaemic activity of both crude propolis and individual polyphenols on various leukaemia cell lines, and it indicates that propolis has the potential to be used in both treatment and prevention of leukaemia. This however needs further evaluation byin vitro,in vivo, and epidemiological studies as well as clinical trials.

scholarly journals Design, Synthesis and In-Vitro Biological Evaluation of Antofine and Tylophorine Prodrugs as Hypoxia-Targeted Anticancer Agents

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3327
Author(s):  
Ziad Omran ◽  
Chris P. Guise ◽  
Linwei Chen ◽  
Cyril Rauch ◽  
Ashraf N. Abdalla ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Multidrug Resistant ◽  
Biological Evaluation ◽  
High Chemical ◽  
Design Synthesis ◽  
Hypoxic Conditions ◽  
Cancerous Cell

Phenanthroindolizidines, such as antofine and tylophorine, are a family of natural alkaloids isolated from different species of Asclepiadaceas. They are characterized by interesting biological activities, such as pronounced cytotoxicity against different human cancerous cell lines, including multidrug-resistant examples. Nonetheless, these derivatives are associated with severe neurotoxicity and loss of in vivo activity due to the highly lipophilic nature of the alkaloids. Here, we describe the development of highly polar prodrugs of antofine and tylophorine as hypoxia-targeted prodrugs. The developed quaternary ammonium salts of phenanthroindolizidines showed high chemical and metabolic stability and are predicted to have no penetration through the blood–brain barrier. The designed prodrugs displayed decreased cytotoxicity when tested under normoxic conditions. However, their cytotoxic activity considerably increased when tested under hypoxic conditions.

Current developments in the Pyran-Based Analogues as Anticancer Agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Parul Grover ◽  
Monika Bhardwaj ◽  
Lovekesh Mehta ◽  
Garima Kapoor ◽  
Pooja A. Chawla
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Anticancer Compounds ◽  
Appropriate Treatment ◽  
Anti Cancer ◽  
Privileged Structure ◽  
Different Types

: Heterocyclic compounds offer an enormous area for new lead molecules for drug discovery. Till today, efforts are being continuously made to find appropriate treatment for the management of the deadly disease of cancer. Amongst the large number of heterocycles that are found in nature, heterocycles having oxygen obtained noteworthy attention due to their distinctive and pharmacological activities.‘Pyran’ is one of the most significant non-aromatic, six-membered ring composed of one oxygen atom and five carbon atoms. It is considered a privileged structure since pyran and its related derivatives exhibit a wide spectrum of biological activities. Pyran derivatives are found to have excellent anti-cancer properties against various types of cancer. The present review focussed on the current advances in different types of pyran-based derivatives as anti-cancer agents. Various in-vitro (cell based testing), in-vivo (animal based testing) models as well as molecular docking along with results are also covered. A subsection describing briefly natural pyran containing anticancer compounds is also incorporated in the review.

Kefir: A synbiotic with approved anticarcinogenic properties

2020 ◽  
Vol 16 ◽  
Author(s):  
Wissam Zam ◽  
Sally Shahoud ◽  
Mansour Hayek ◽  
Alaa Saad
Keyword(s):  
Cancer Prevention ◽  
Biological Activities ◽  
Research Literature ◽  
Bibliographic Databases ◽  
Middle Income ◽  
Prevention And Treatment ◽  
Prevention Of Cancer

Background:: As by WHO report, cancer is the second leading cause of death globally, and approximately 70% of deaths from cancer occur in low- and middle-income countries. From this point more attention has been given to the role of nutrition in the prevention of cancer development. Methods:: We undertook a structured search of bibliographic databases for peer-reviewed research literature dealing with the role of kefir in cancer prevention and treatment. Results:: Probiotics are one of the most important food fortifications which are proved to have anti-carcinogenic properties. Probiotics can directly bind to carcinogens and alter the production of enzymes by modifying intestinal environment. Kefir, originating from the Balkan–Caucasian region, is a synbiotic composed of a wide number microflora and exopolysaccharides with approved in vitro and in vivo biological activities. Kefir plays a great potential role in cancer prevention and treatment interfering with apoptosis, proliferation and transformation. Conclusion:: This review highlights the important role of probiotics, exopolysaccharides and common kefir in preventing different types of cancer including colon cancer, sarcoma, breast cancer, lung cancer, leukemia, gastric cancer and melanoma.

scholarly journals Algae as potential repository of anti cancerous natural compounds

2017 ◽  
Vol 9 (2) ◽  
Author(s):  
Ankita Mridha ◽  
Santanu Paul
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Leukemia Cell ◽  
Relevant Information ◽  
Cancer Cell Growth ◽  
History Of ◽  
History Of Use ◽  
Promising Source

<p>Algae constitute a promising source of novel compounds with potential as human therapeutic agents. In particular, algae have been considered as a potential source of new bio-active compound. Algae possess several biological activities, including anticancer activity. This review provides a comprehensive report on the several genera of algae belonging to Chlorophyceae, Pheophyceae and Rhodophyceae having anti-proliferative, apoptotic, anti angiogenic as well as cytotoxic efficacy and their mode of action <em>in vitro</em> as well as <em>in vivo</em> condition. Algae are extensively used as functional foods and medicinal herbs, and have a long history of use in Asian countries. Many algae have been used for the treatment of cancer, many crude or partially purified polysaccharides from various brown, green, and red algae have been tested for their antitumor activities. Relevant information was collected from scientific journals, books, and reports via library and electronic search using Medline, Pubmed, Science Direct, and Scopus. The different extracts with some other solvent shows a huge anti-proliferative action on different cancer as well as on different leukemia cell lines. Here we focus on several bioactive compounds that have been derived as well as characterized from different genera of algae and there mechanism of inhibiting cancer cell growth. Considering the ability of the golden treasure present in algae to act against different cancers, this review highlights the potential use of algae as anticancer agents.</p>

scholarly journals Holoptelea integrifolia(Roxb.) Planch: A Review of Its Ethnobotany, Pharmacology, and Phytochemistry

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Showkat Ahmad Ganie ◽  
Surender Singh Yadav
Keyword(s):  
Chronic Wounds ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Phytochemical Analysis ◽  
Treatment And Prevention ◽  
Cns Depressant ◽  
Crude Extracts ◽  
Prevention And Treatment

Holoptelea integrifolia(Ulmaceae) is a versatile medicinal plant used in various indigenous systems of medicine for curing routine healthcare maladies. It is traditionally used in the treatment and prevention of several ailments like leprosy, inflammation, rickets, leucoderma, scabies, rheumatism, ringworm, eczema, malaria, intestinal cancer, and chronic wounds.In vitroandin vivopharmacological investigations on crude extracts and isolated compounds showed antibacterial, antifungal, analgesic, antioxidant, anti-inflammatory, anthelmintic, antidiabetic, antidiarrhoeal, adaptogenic, anticancer, wound healing, hepatoprotective, larvicidal, antiemetic, CNS depressant, and hypolipidemic activities. Phytochemical analysis showed the presence of terpenoids, sterols, saponins, tannins, proteins, carbohydrates, alkaloids, phenols, flavonoids, glycosides, and quinines. Numerous compounds including Holoptelin-A, Holoptelin-B, friedlin, epifriedlin,β-amyrin, stigmasterol,β-sitosterol, 1, 4-napthalenedione, betulin, betulinic acid, hexacosanol, and octacosanol have been identified and isolated from the plant species. The results of several studies indicated thatH. integrifoliamay be used as an effective therapeutic remedy in the prevention and treatment of various ailments. However, further studies on chemical constituents and their mechanisms in exhibiting certain biological activities are needed. In addition, study on the toxicity of the crude extracts and the compounds isolated from this plant should be assessed to ensure their eligibility to be used as source of modern medicines.

scholarly journals Nutritive Importance and Therapeutics Uses of Three Different Varieties (Murraya koenigii, Micromelum minutum, and Clausena indica) of Curry Leaves: An Updated Review

2021 ◽  
Vol 2021 ◽  
pp. 1-23
Author(s):  
D. T. Abeysinghe ◽  
D. D. D. H. Alwis ◽  
K. A. H. Kumara ◽  
U. G. Chandrika
Keyword(s):  
Current Knowledge ◽  
Biological Activities ◽  
Biological Effects ◽  
Herbal Remedies ◽  
Murraya Koenigii ◽  
In Vivo Models ◽  
Treatment And Prevention ◽  
Curry Leaves

Murraya koenigii (M. koenigii), Micromelum minutum (M. minutum), and Clausena indica (C. indica) are three varieties of curry leaves in the family Rutaceae. They have been widely used in Ayurvedic medicine worldwide in the treatment and prevention of various diseases. Earlier findings provide strong evidence to support the three curry leaf species’ potent pharmaceutical and biological effects, including antioxidant, antidiabetic, anti-inflammatory, and antitumor activities. Various parts of these plants, such as leaves, seeds, flowers, and fruit, contain constituents responsible for the modulation of numerous biological processes. Leading constituents of curry leaves play a crucial role in diabetic and anticancer management by regulating various molecular pathways, including Bcl-2, Bax, NF-κB, and TNFα, according to in vitro and in vivo models established. Therefore, this review summarizes the current knowledge on research achievements made in terms of phytoconstituents, their structures, biological activities, and pharmacological actions with clinical studies of curry leaves up to date. The review also emphasizes the necessity for comprehensive research studies on the pharmacological actions and the mechanisms of selected phytochemicals of M. koenigii, M. minutum, and C. indica to validate their efficacy as potent herbal remedies for many ailments.

Recent Progress on Anticancer Agents Incorporating Pyrazole Scaffold

2021 ◽  
Vol 21 ◽  
Author(s):  
Satbir Mor ◽  
Mohini Khatri ◽  
Ravinder punia ◽  
Suchita Sindhu
Keyword(s):  
20Th Century ◽  
Anticancer Agents ◽  
Recent Progress ◽  
Biological Activities ◽  
Biologically Active ◽  
Anticancer Activities ◽  
Number Of Publications ◽  
Heterocyclic Moiety

: The search of new anticancer agents is considered as a dynamic field of medicinal chemistry. In recent years, the synthesis of compounds with anticancer potential has increased and a large number of structurally varied compounds displaying potent anticancer activities have been published. Pyrazole is an important biologically active scaffold that possessed nearly all types of biological activities. The aim of this review is to collate literature work reported by researchers to provide an overview on in vivo and in vitro anticancer activities of pyrazole based derivatives among the diverse biological activities displayed by them and also presents recent efforts made on this heterocyclic moiety regarding anticancer activities. This review has been driven from the increasing number of publications, on this issue, which have been reported in the literature since the ending of the 20th century (from 1995-to date).

Sign in / Sign up

Export Citation Format

Share Document