Triazole As Potent Anti-Cancer Agent- A Pharmacophoric Scaffold

2021 ◽  
Vol 17 ◽  
Author(s):  
Nidhi Kala ◽  
Kalpana Praveen Rahate
Keyword(s):  
Characteristic Feature ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring System ◽  
Review Article ◽  
Current Review ◽  
Anti Cancer ◽  
Good Template ◽  
Cancer Agent

: Triazole is the main five-membered Nitrogen-containing basic heterocyclic ring system reported for their biological activities and compounds with multiple pharmacophores, which fetch together acquaintance of a target with sympathetic types of the molecule that might interact with the target. In addition, healthy, adaptable, and scalable chemistry must be employed to achieve the task. This characteristic feature of triazole would make a good template for a lead cohort library. The current review article focuses on recent advancements in triazole moiety as an anti-cancer agent with their mechanism pathways of synthesized analogues.

Resolving the Mystery of Ring Opening in the Synthesis of Benzo[d][1, 3]oxazin-4-one and Quinazolin-4(3H)-one

2019 ◽  
Vol 16 (11) ◽  
pp. 898-905
Author(s):  
Harun Patel ◽  
Rahul Pawara ◽  
Sanjay Surana
Keyword(s):  
Characteristic Feature ◽  
Ring Opening ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring System ◽  
Time Saving ◽  
Fusion Strategy ◽  
Good Template ◽  
Lead Generation

Quinazoline is the six-membered heterocyclic ring system reported for its versatile biological activities. This characteristic feature of quinazoline makes it a good template for a lead generation library. Ring opening is one of the major concerns in the synthesis of quinazolin-4(3H)-one that results in diamide formation. Here, alternative fusion strategy is reported, which is a time-saving and costeffective method to overcome the ring opening problem associated with the synthesis of benzo[ d][1,3]oxazin-4-one and quinazolin-4(3H)-one.

The Chemistry of Triazine Isomers: Structures, Reactions, Synthesis and Applications

2020 ◽  
Vol 20 ◽  
Author(s):  
Neelottama Kushwaha ◽  
C S Sharma
Keyword(s):  
Basic Property ◽  
Electrophilic Substitution ◽  
Antimicrobial Agents ◽  
Resonance Energy ◽  
Heterocyclic Ring ◽  
Ring System ◽  
Agricultural Fields ◽  
Substitution Reactions ◽  
Anti Cancer ◽  
Benzene Structure

: Triazine is the six-membered heterocyclic ring containing three nitrogen which replaces carbon-hydrogen unit in the benzene ring. Based on nitrogen position present in the ring system, it is categorized in three isomeric forms i.e.1, 2, 3-triazine (vicinal triazine), 1, 2, 4-triazine (asymmetrical triazine or isotriazine) and 1, 3, 5-triazine (symmetrical or s-triazine or cyanidine). Triazines have weakly basic property. Its isomers have much weaker resonance energy than benzene structure, so nucleophilic substitution reactions are more preferred than electrophilic substitution reactions. Triazine isomers and their derivatives are known to play important roles possessing various activities in medicinal and agricultural fields such as anti-cancer, antiviral, fungicidal, insecticidal, bactericidal, herbicidal, antimalarial and antimicrobial agents.

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.

scholarly journals Synthesis and Biological Activities of Some Pyrimidine Derivatives: A Review

2020 ◽  
Vol 36 (6) ◽  
pp. 1001-1015
Author(s):  
Nadia Ali Ahmed Elkanzi
Keyword(s):  
Nitrogen Atom ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring System ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Cardiovascular Agents ◽  
Anti Hiv ◽  
Biological And Pharmacological Activities

Nitrogen containing synthetically and biologically important heterocyclic ring system namely pyrimidine possess both biological and pharmacological activities, and defend as aromatic six heterocyclic with 1and 3 nitrogen atom in ring. Preparation of pyrimidine via different methods offer its importance in fields of medicinal chemistry and Chemistry. Pyrimidines and their derivatives act as anti-inflammatory, anti-malaria, anti-tumor, cardiovascular agents, anti-neoplastic, anti-tubercular, anti- HIV, diuretic ,anti-viral, anti-microbial, ,analgesic .This review give light up on biological and pharmacological activities of pyrimidine nucleus.

scholarly journals Coumarin sulfonamide derivatives: An emerging class of therapeutic agents

2020 ◽  
Vol 26 (1) ◽  
pp. 46-59 ◽  
Author(s):  
Ali Irfan ◽  
Laila Rubab ◽  
Mishbah Ur Rehman ◽  
Rukhsana Anjum ◽  
Sami Ullah ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Structural Features ◽  
Therapeutic Agents ◽  
Review Article ◽  
Structural Motif ◽  
Structure Activity ◽  
Anti Cancer ◽  
Novel Therapeutic

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.

scholarly journals Purification, Structural Characteristics, and Biological Activities of Exopolysaccharide Isolated From Leuconostoc mesenteroides SN-8

2021 ◽  
Vol 12 ◽  
Author(s):  
Junrui Wu ◽  
Danli Yan ◽  
Yumeng Liu ◽  
Xue Luo ◽  
Yang Li ◽  
...  
Keyword(s):  
Leuconostoc Mesenteroides ◽  
Biological Activities ◽  
Structural Characteristics ◽  
Molecular Weights ◽  
Cycle Arrest ◽  
Glycosidic Bonds ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Inhibitory Potential ◽  
Cancer Agent

In this study, a novel exopolysaccharide (EPS) was extracted from Leuconostoc mesenteroides Shen Nong’s (SN)-8 which can be obtained from Dajiang. After the purification step, EPS-8-2 was obtained with molecular weights of 1.46 × 105 Da. The structural characterization of EPS indicated that the EPS belonged to the class polysaccharide, mainly composed of glucan and also contained certain mannose residues that were found to be connected by α-1,6 glycosidic bonds. Moreover, the results demonstrated that EPS displayed a significant capacity to scavenge free radical to some extent, and this anti-oxidant potential was found to be concentration dependent. The results further revealed that EPS displayed a significant inhibitory potential on the growth of HepG2 cells by promoting apoptosis and induced cell cycle arrest in G1 and G2 phases. Overall, these results suggested that EPS can be explored as a possible anti-cancer agent.

An Overview on Chemistry and Biological Importance of Pyrrolidinone

2018 ◽  
Vol 15 (2) ◽  
pp. 166-178 ◽  
Author(s):  
Zahra Hosseinzadeh ◽  
Ali Ramazani ◽  
Kamaleddin Hosseinzadeh ◽  
Nima Razzaghi-Asl ◽  
Farideh Gouranlou
Keyword(s):  
Biological Activities ◽  
Wide Spectrum ◽  
Heterocyclic Ring ◽  
Review Article ◽  
Pharmacological Activities ◽  
Future Studies ◽  
Comprehensive Information ◽  
Novel Drugs ◽  
Bioactive Agents ◽  
Great Scope

Background: Pyrrolidinone is a five membered heterocyclic ring that is a versatile lead compound for designing powerful bioactive agents. Pyrrolidinone nucleus is one of the most important heterocyclic compound indicating notable pharmaceutical effects. Many procedures for the preparation of pyrrolidinone and also their various reactions offer great scope in the field of medicinal chemistry. This fascinating group of compounds has diverse pharmacological activities such as antibacterial, antifungal, anticancer and anticonvulsant. Objective: The review article proposes to classify comprehensive information on chemistry and pharmaceutical effects of pyrrolidinone in order to open new viewpoint for future studies. Conclusion: It is clear from the review of the topic that a wide spectrum of pyrrolidinone analogues have been synthesized and the majority of these derivatives have indicated different significant biological activities. Thus, these analogues can be used for future progression of novel drugs against many more poor agents.

scholarly journals An Insight into 4-Thiazolidinones

2021 ◽  
pp. 162-174
Author(s):  
Smriti Sahu ◽  
Prabhat Kumar Upadhyay ◽  
Pradeep Mishra
Keyword(s):  
Biological Activities ◽  
Ring System ◽  
Future Research ◽  
Aryl Group ◽  
Synthetic Compounds ◽  
Structural Modifications ◽  
The Core ◽  
Anti Cancer ◽  
Anti Fungal ◽  
Insight Into

Aims: This assessment is all about to get imminent into 4-thiazolidinones and comprehensively reviewing this molecule. 4-Thiazolidinones are known for their wide-ranging biological activities. 4 - Thiazolidinones contains thiazolidine ring having carbonyl group in the 4-position. The chemistry of thiazolidinones has drawn scientific interest through the years because this particular ring system is the core structure in a variety of synthetic compounds with a broad spectrum of biological activities such as anti-bacterial, anti-fungal, insecticidal, anti-epileptic, anti-mycobacterial, anti- inflammatory, anti-parasitic, hypnotic and anti-cancer. Structural modifications on the 4-thiazolidinone moiety, either by replacing the aryl group with the heteroaryl scaffold or by incorporating different groups and moieties (A&B) on –CH– group of nucleus paving a new pathway for the future research. It necessitates to widely reviewing the structure, chemistry and pharmacological aspects of 4-thiazolidinones.

Amygdalin from Apricot Kernels Induces Apoptosis and Causes Cell Cycle Arrest in Cancer Cells: An Updated Review

2019 ◽  
Vol 18 (12) ◽  
pp. 1650-1655 ◽  
Author(s):  
Mohammad Saleem ◽  
Jawaria Asif ◽  
Muhammad Asif ◽  
Uzma Saleem
Keyword(s):  
Cell Cycle ◽  
Cancer Cells ◽  
Time Frame ◽  
Central Process ◽  
Naturally Occurring ◽  
Current Review ◽  
Anti Cancer ◽  
Apoptotic Proteins ◽  
Cancer Agent

Background: Amygdalin is a cyanogenic glycoside which is described as a naturally occurring anticancer agent. Current review highlights apoptosis-inducing attributes of amygdalin towards different cancers and its potential application as an anti-cancer agent in cancer therapy. Method: Data about amygdalin was retrieved from all major scientific databases i.e., PubMed, ScienceDirect, Google Scholar, Scopus and Medline by using combination of keywords like amygdalin, apoptosis, laetrile, vitamin B- 17, pro-apoptotic proteins, anti-apoptotic proteins, hydrogen cyanide, mechanism of action of amygdalin and amygdalin therapy on humans. However, no specific time frame was followed for collection of data. Results: Data collected from already published articles revealed that apoptosis is a central process activated by amygdalin in cancer cells. It is suggested to stimulate apoptotic process by upregulating expression of Bax (proapoptotic protein) and caspase-3 and downregulating expression of Bcl-2 (anti-apoptotic protein). It also promotes arrest of cell cycle in G0/G1 phase and decrease number of cells entering S and G2/M phases. Thus, it is proposed to enhance deceleration of cell cycle by blocking cell proliferation and growth. Conclusion: The current review epitomizes published information and provides complete interpretations about all known anti-cancer mechanisms of amygdalin, possible role of naturally occurring amygdalin in fight against cancer and mistaken belief about cyanide toxicity causing potential of amygdalin. However, well-planned clinical trials are still needed to be conducted to prove effectiveness of this substance in vivo and to get approval for human use.

scholarly journals Biological activities of fusarochromanone: a potent anti-cancer agent

2014 ◽  
Vol 7 (1) ◽  
Author(s):  
Elahe Mahdavian ◽  
Phillip Palyok ◽  
Steven Adelmund ◽  
Tara Williams-Hart ◽  
Brian D Furmanski ◽  
...  
Keyword(s):  
Biological Activities ◽  
Anti Cancer ◽  
Cancer Agent
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