Phthalazinone Scaffold: Emerging Tool in the Development of Target Based Novel Anticancer Agents

2020 ◽  
Vol 20 (18) ◽  
pp. 2228-2245
Author(s):  
Jyoti Singh ◽  
Amruta Suryan ◽  
Sandeep Kumar ◽  
Shweta Sharma
Keyword(s):  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Aurora Kinase ◽  
Review Article ◽  
Pharmacological Activities ◽  
Dna Topoisomerase ◽  
Progressive Development ◽  
Anticancer Properties ◽  
Current Review ◽  
P Glycoprotein

Phthalazinones are important nitrogen-rich heterocyclic compounds which have been a topic of considerable medicinal interest because of their diversified pharmacological activities. This versatile scaffold forms a common structural feature for many bioactive compounds, which leads to the design and development of novel anticancer drugs with fruitful results. The current review article discusses the progressive development of novel phthalazinone analogues that are targets for various receptors such as PARP, EGFR, VEGFR-2, Aurora kinase, Proteasome, Hedgehog pathway, DNA topoisomerase and P-glycoprotein. It describes mechanistic insights into the anticancer properties of phthalazinone derivatives and also highlights various simple and economical techniques for the synthesis of phthalazinones.

Recent Progress of Benzimidazole Hybrids for Anticancer Potential

2020 ◽  
Vol 27 (35) ◽  
pp. 5970-6014 ◽  
Author(s):  
Md. Jawaid Akhtar ◽  
Mohammad Shahar Yar ◽  
Vinod Kumar Sharma ◽  
Ahsan Ahmed Khan ◽  
Zulphikar Ali ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Alkylating Agents ◽  
American Chemical Society ◽  
Chemical Society ◽  
Benzimidazole Derivatives ◽  
Progressive Development ◽  
Anticancer Properties ◽  
Naturally Occurring ◽  
Nitrogenous Base

This review presents the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical Society has shown progressive development in fighting cancer. Researchers all over the world in both developed and developing countries are in a continuous effort to tackle this serious concern. Benzimidazole and its derivatives showed a broad range of biological activities due to their resemblance with naturally occurring nitrogenous base i.e. purine. The review discussed benzimidazole derivatives showing anticancer properties through a different mechanism viz. intercalation, alkylating agents, topoisomerases, DHFR enzymes, and tubulin inhibitors. Benzimidazole derivatives act through a different mechanism and the substituents reported from the earlier and recent research articles are prerequisites for the synthesis of targeted based benzimidazole derivatives as anticancer agents. The review focuses on an easy comparison of the substituent essential for potency and selectivity through SAR presented in figures. This will further provide a better outlook or fulfills the challenges faced in the development of novel benzimidazole derivatives as anticancer.

scholarly journals Recent Advances in Chalcones: Synthesis, Transformation and Pharmacological Activities

2019 ◽  
pp. 1-16
Author(s):  
Oluwaseyi Bukky Ovonramwen ◽  
Bodunde Joseph Owolabi ◽  
Amowie Philip Oviawe
Keyword(s):  
Organic Synthesis ◽  
Heterocyclic Compound ◽  
Heterocyclic Compounds ◽  
Condensation Reaction ◽  
Review Article ◽  
Pharmacological Activities ◽  
Usual Approach ◽  
Recent Advances ◽  
Anti Cancer ◽  
Multifunctional Molecules

Chalcones are useful intermediates in the synthesis of heterocyclic compound and the unique reagents in organic synthesis. The usual approach to obtain chalcones is through Claisen-Schmidt condensation. Several novel heterocyclic chalcone analogs have emerged. Chalcones are multifunctional molecules that possess promising pharmacological activities. Chalcones are known for anti-cancer, antioxidant, anti-inflammatory, anti-microbial, anti-tubercular, antileishmanial, antimalarial, anthelmintic, osteogenic activities. This review article focuses on recent applications of Claisen-Schmidt condensation reaction employed in the synthesis of chalcone, its transformation to heterocyclic compounds and pharmacological activities.

scholarly journals A review on Indole and Benzothiazole derivatives its importance

2019 ◽  
Vol 9 (1-s) ◽  
pp. 505-509 ◽  
Author(s):  
Shaheen Sulthana ◽  
P. Pandian
Keyword(s):  
Heterocyclic Compounds ◽  
Structural Modification ◽  
Biological Activities ◽  
New Product ◽  
Review Article ◽  
Literature Survey ◽  
Pharmacological Activities ◽  
Benzothiazole Derivatives ◽  
Wide Range ◽  
Anti Inflammatory

In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Indole, Benzothiazole and its analogs are versatile substrates, which can be used for the synthesis of numerous heterocyclic compounds. Indole, Benzothiazole and its derivatives are used in organic synthesis and they are used in evaluating new product that possesses different biological activities. Hence, their extensive structural modification has result in different analogues of Indole and Benzothiazole derivatives depicting wide range of biological and pharmacological activities such as antiviral, anticonvulsant, anti-inflammatory, analgesic, antimicrobial and anticancer. This review article literature survey summarizes the synthesis and pharmacological activities of Indole, Benzothiazole and its derivatives. Keywords: Indole, Benzothiazole, antiviral, anticonvulsant, anti-inflammatory, analgesic, antimicrobial and anticancer

Naturally Occurring O-heterocycles as Anticancer Agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Satya Kumar Avula ◽  
Biswanath Das ◽  
Rene Csuk ◽  
Ahmed Al-Harrasi
Keyword(s):  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Therapeutic Agents ◽  
Review Article ◽  
Drug Discovery And Development ◽  
Lead Compounds ◽  
Naturally Occurring ◽  
Structure Activity ◽  
Recent Advancement ◽  
Deadly Disease

: 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.

Bioinorganic Chemistry of Platinum(IV) Complexes as Platforms for Anticancer Agents

2020 ◽  
Vol 16 (6) ◽  
pp. 726-737
Author(s):  
Little Nagyal ◽  
Amit Kumar ◽  
Rishipal Sharma ◽  
Rohit Yadav ◽  
Pratibha Chaudhary ◽  
...  
Keyword(s):  
Coordination Chemistry ◽  
Anticancer Agents ◽  
Binding Sites ◽  
Metal Particle ◽  
Bioinorganic Chemistry ◽  
Oxidation States ◽  
Current Status ◽  
Anticancer Properties ◽  
Current Review ◽  
Detoxification Mechanism

The current review focuses on the comprehensive studies of platinum-based complexes that are known to exhibit anticancer properties. The research on metal-particle work has helped in treating sicknesses which plays an imperative part in therapeutic bioinorganic science. Understanding the biochemistry of the detoxification mechanism of metals can help in advancing as well as enhancing the anticancer property of metal complexes for several types of a tumour. The classifications of complexes discussed have been done on the basis of Platinum oxidation states and binding sites of the ligands. Further background and current status of Pt(IV) complexes are briefly explained along with a special reference to Structural Activity Relationships and Mode of Action. The coordination chemistry of Pt(IV) has been summarised and Pt(IV) complexes are reviewed on the basis of binding of Pt(IV) with Human Serum Albumin and DNA. Finally, the results were summarized and concluded emphasizing on the most important features.

N-heterocycles: Recent advances in biological applications

2021 ◽  
Vol 19 ◽  
Author(s):  
Monica Dinodia
Keyword(s):  
Structural Design ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Review Article ◽  
Biological Applications ◽  
Pharmacological Activities ◽  
Physiological Properties ◽  
Anti Cancer ◽  
Anti Hiv ◽  
Depth View

Abstract: Nitrogen based heterocycles display an impressive repertoire of biological activities, including antioxidant, antimicrobial, anti-tuberculosis, analgesic, anti-inflammatory, anti-viral, anti-HIV, anti-cancer, anti-helminthic, and other pharmacological activities. Numerous novel nitrogen-based heterocycles have been synthesized, which showed various physiological properties, and their application in medicinal chemistry is ever-growing. The present review will provide an in-depth view of N-heterocyclic compounds that showed biological activities in the last 5 years (2017-2021). This review article will be helpful for the structural design of effective and sustainable N-heterocyclic drugs against diseases with minimal side effects.

Recent Synthetic Strategies for Monocyclic Azole Nucleus and Its Role in Drug Discovery and Development

2018 ◽  
Vol 15 (3) ◽  
pp. 321-340 ◽  
Author(s):  
Neha ◽  
Ashish Ranjan Dwivedi ◽  
Rakesh Kumar ◽  
Vinod Kumar
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Review Article ◽  
Drug Discovery And Development ◽  
Drug Candidates ◽  
Drug Molecules ◽  
Current Review ◽  
Biological Potential ◽  
Recent Developments ◽  
Potent Drug

Background: In recent years, the development and diversification of heterocyclic compounds has become central to the discovery of bioactive compounds with novel or improved pharmacological properties. In particular, N-containing heterocycles are proved to be promising leads and drug candidates, and received huge attention of the medicinal chemists. Objective: Many drugs especially antibiotics are becoming obsolete due to the development of multidrug resistance. Moreover, toxicity and other side effects of some drugs necessitated the quest for safer and more potent drug candidates. The current review article described biological potential of various monocyclic azoles. Recent developments in the synthesis of azole derivatives have been also reviewed. Conclusion: The presence of N-heterocyclic rings can influence the pharmacokinetics, pharmacodynamics, pKa and bioavailability profile of the drug molecules. Compounds containing monocyclic azole rings showed various biological activities and number of molecules are in clinical practice. A number of important leads and potential drug candidates containing azole nucleus are in advance stages of drug developments. Thus, simple, atom economic and more efficient synthetic strategies are desired for the synthesis of new libraries of the compounds.

A REVIEW ON RECENT ADVANCES IN CHEMISTRY, SYNTHESIS AND BIOLOGICAL APPLICATIONS OF ISATIN DERIVATIVES

2018 ◽  
pp. 16-22
Author(s):  
Shukla PK ◽  
Singh MP ◽  
Patel R
Keyword(s):  
Heterocyclic Compounds ◽  
Biologically Active ◽  
Biological Applications ◽  
Plant Origin ◽  
Recent Past ◽  
Pharmacological Activities ◽  
Naturally Occurring ◽  
Recent Advances ◽  
Biological Aspects ◽  
Isatin Derivatives

Indole and its derivatives have engaged a unique place in the chemistry of nitrogen heterocyclic compounds. The recognition of the plant growthhormone, heteroauxin, the significant amino acids, tryptamine & tryptophan and anti-inflammatory drug, indomethacine are the imperativederivatives of indole which have added stimulus to this review work. Isatin (1H-indole-2,3-dione), an indole derivative of plant origin. Althoughit is a naturally occurring compound, but was synthesized by Erdmann and Laurent in 1840 before it was found in nature. Isatin is a versatileprecursor for many biologically active molecules and its diversified nature makes it a versatile substrate for further modifications. It is concernedin many pharmacological activities like anti-malarial, antiviral, anti-allergic, antimicrobial etc; isatin and its derivatives have been also found todemonstrate promising outcomes against various cancer cell lines. This review provides a brief overview on the recent advances and futureperspectives on chemistry and biological aspects of isatin and its derivatives reported in the recent past.

Novel Chemotherapeutic Agents - The Contribution of Scorpionates

2020 ◽  
Vol 26 (41) ◽  
pp. 7452-7475 ◽  
Author(s):  
Marta A. Andrade ◽  
Luísa M.D.R.S. Martins
Keyword(s):  
Transition Metal ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Bioinorganic Chemistry ◽  
Chemotherapeutic Agents ◽  
Great Role ◽  
Anticancer Properties ◽  
Scorpionate Ligands

: The development of safe and effective chemotherapeutic agents is one of the uppermost priorities and challenges of medicinal chemistry and new transition metal complexes are being continuously designed and tested as anticancer agents. Scorpionate ligands have played a great role in coordination chemistry, since their discovery by Trofimenko in the late 1960s, with significant contributions in the fields of catalysis and bioinorganic chemistry. Scorpionate metal complexes have also shown interesting anticancer properties, and herein, the most recent (last decade) and relevant scorpionate complexes reported for application in medicinal chemistry as chemotherapeutic agents are reviewed. The current progress on the anticancer properties of transition metal complexes bearing homo- or hetero- scorpionate ligands, derived from bis- or tris-(pyrazol-1-yl)-borate or -methane moieties is highlighted.

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.

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