Design and synthesis of 2,3-dihydro- and 5-chloro-2,3-dihydro-naphtho-[1,2-b]furan-2-carboxylic acid N-(substitutedphenyl)amide analogs and their biological activities as inhibitors of NF-κB activity and anticancer agents

2016 ◽  
Vol 39 (5) ◽  
pp. 618-630 ◽  
Author(s):  
Minho Choi ◽  
Hyeju Jo ◽  
Dayoung Kim ◽  
Jieun Yun ◽  
Jong-Soon Kang ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Design And Synthesis

scholarly journals Exploration of Newer Possibilities to the Synthesis of Diazepine and Quinoline Carboxylic Acid Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-8
Author(s):  
Vatsala Soni ◽  
Meenakshi Sharma ◽  
Anshu Agarwal ◽  
Dharma Kishore
Keyword(s):  
Carboxylic Acid ◽  
Drug Design ◽  
Spectral Data ◽  
Biological Activities ◽  
Design And Synthesis ◽  
Quinoline Carboxylic Acid ◽  
Quinoline Moiety ◽  
Molecular Framework

Heterocyclic systems containing benzothiazoles, carbazole (and azacarbazole) moieties have attracted the attention of chemists owing to these nuclei having been identified in the literature as most promising pharmacophores in drug design and synthesis. Based on these observations, it could be anticipated that incorporation of the bioactive azepine moiety and quinoline moiety into the molecular framework of benzothiazoles fused to carbazole (and azacarbazoles) could produce interesting series of compounds9–12with enhanced biological activities, whose structure was unequivocally established from its microanalyses and spectral data.

scholarly journals Design and Synthesis of Benzimidazole-Chalcone Derivatives as Potential Anticancer Agents

Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3259 ◽  
Author(s):  
Hsieh ◽  
Ko ◽  
Chang ◽  
Kapoor ◽  
Liang ◽  
...  
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Alkyl Chain ◽  
Biological Activities ◽  
Breast Adenocarcinoma ◽  
Benzimidazole Derivatives ◽  
Design And Synthesis ◽  
Anticancer Properties ◽  
Human Ovarian Carcinoma ◽  
Mcf 7

Numerous reports have shown that conjugated benzimidazole derivatives possess various kinds of biological activities, including anticancer properties. In this report, we designed and synthesized 24 new molecules comprising a benzimidazole ring, arene, and alkyl chain-bearing cyclic moieties. The results showed that the N-substituted benzimidazole derivatives bearing an alkyl chain and a nitrogen-containing 5- or 6-membered ring enhanced the cytotoxic effects on human breast adenocarcinoma (MCF-7) and human ovarian carcinoma (OVCAR-3) cell lines. Among the 24 synthesized compounds, (2E)-1-(1-(3-morpholinopropyl)-1H-benzimidazol-2 -yl)-3-phenyl-2-propen-1-one) (23a) reduced the proliferation of MCF-7 and OVCAR-3 cell lines demonstrating superior outcomes to those of cisplatin.

Design and synthesis of 4,5-diaryl/heteroarylthiophene-2-carboxylic acid derivatives and evaluation of their biological activities

2017 ◽  
Vol 23 (1) ◽  
Author(s):  
Ananda Mohan Arasavelli ◽  
Ganapavarapu Sharma Veera Raghava ◽  
Siddaiah Vidavalur
Keyword(s):  
Biological Activity ◽  
Carboxylic Acid ◽  
Biological Activities ◽  
Design And Synthesis

AbstractSynthesis, characterization and biological activity of novel 4,5-diaryl/heteroaryl thiophene-2-carboxylic acid derivatives are described. Aryl/heteroaryl esters were converted to substituted thiophene esters via a Vilsmeier-Haack reaction, which were then hydrolyzed to 4,5-diaryl/heteroaryl thiophene-2-carboxylic acid derivatives

scholarly journals Imidazoles as Potential Anticancer Agents: An Update on Recent Studies

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4213
Author(s):  
Pankaj Sharma ◽  
Chris LaRosa ◽  
Janet Antwi ◽  
Rajgopal Govindarajan ◽  
Karl A. Werbovetz
Keyword(s):  
Anticancer Agents ◽  
Histone Deacetylases ◽  
Biological Activities ◽  
Structural Components ◽  
Mdm2 Protein ◽  
Drug Discovery And Development ◽  
Design And Synthesis ◽  
Wide Range ◽  
Murine Double Minute ◽  
High Polarity

Nitrogen-containing heterocyclic rings are common structural components of marketed drugs. Among these heterocycles, imidazole/fused imidazole rings are present in a wide range of bioactive compounds. The unique properties of such structures, including high polarity and the ability to participate in hydrogen bonding and coordination chemistry, allow them to interact with a wide range of biomolecules, and imidazole-/fused imidazole-containing compounds are reported to have a broad spectrum of biological activities. This review summarizes recent reports of imidazole/fused imidazole derivatives as anticancer agents appearing in the peer-reviewed literature from 2018 through 2020. Such molecules have been shown to modulate various targets, including microtubules, tyrosine and serine-threonine kinases, histone deacetylases, p53-Murine Double Minute 2 (MDM2) protein, poly (ADP-ribose) polymerase (PARP), G-quadraplexes, and other targets. Imidazole-containing compounds that display anticancer activity by unknown/undefined mechanisms are also described, as well as key features of structure-activity relationships. This review is intended to provide an overview of recent advances in imidazole-based anticancer drug discovery and development, as well as inspire the design and synthesis of new anticancer molecules.

Novel anthraquinone compounds as anticancer agents and their potential mechanism

2020 ◽  
Author(s):  
Wei Tian ◽  
Chunmiao Wang ◽  
Danrong Li ◽  
Huaxin Hou
Keyword(s):  
Dna Damage ◽  
Anticancer Activity ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Review Article ◽  
Potential Mechanism ◽  
Structural Modifications ◽  
Design And Synthesis ◽  
Cycle Arrest ◽  
Anticancer Mechanism

Anthraquinones exhibit a unique anticancer activity. Since their discovery, medicinal chemists have made several structural modifications, resulting in the design and synthesis of a large number of novel anthraquinone compounds with different biological activities. In general, anthraquinone compounds have been considered to have anticancer activity mainly through DNA damage, cycle arrest and apoptosis. However, recent studies have shown that novel anthraquinone compounds may also inhibit cancer through paraptosis, autophagy, radiosensitising, overcoming chemoresistance and other methods. This Review article provides an overview of novel anthraquinone compounds that have been developed as anticancer agents in recent years and focuses on their anticancer mechanism.

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.

A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

Tetrazoloquinolines: Synthesis, Reactions, and Applications

2020 ◽  
Vol 24 (4) ◽  
pp. 439-464 ◽  
Author(s):  
Rizk E. Khidre ◽  
Tahah A. Ameen ◽  
Mounir A. I. Salem
Keyword(s):  
Carboxylic Acid ◽  
Chemical Reactions ◽  
Sodium Azide ◽  
Biological Activities ◽  
Quinoline Derivatives ◽  
Pharmacological Activities ◽  
Synthesis Reactions ◽  
Intramolecular Cyclocondensation

This review summarizes the synthesis, reactions, and biological activities of tetrazolo[1,5-a]quinoline derivatives. These derivatives were synthesized by several methods such as i) from the reaction of 2-chloroquinoline with sodium azide ii) from diazotization 2-hydrazinylquinoline derivatives, and iii) from intramolecular cyclocondensation of 2-azidoarylidenes. Also, the chemical reactions and pharmacological activities of some tetrazoloquinolines such as tetrazolo[1,5-a]quinoline-4-carbaldehyde, 5-chlorotetrazolo[ 1,5-a]quinoline, 4-(chloromethyl)tetrazolo[1,5-a]quinoline, tetrazolo[1,5- a]quinoline-4-carboxylic acid, and 5-azidotetrazolo[1,5-a]quinoline were discussed.

Design, Synthesis, Anti-Proliferative Evaluation and Cell Cycle Analysis of Hybrid 2-Quinolones

2019 ◽  
Vol 19 (9) ◽  
pp. 1132-1140
Author(s):  
Heba A.E. Mohamed ◽  
Hossa F. Al-Shareef
Keyword(s):  
Cell Cycle ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Flow Cytometric Analysis ◽  
Annexin V ◽  
Cytotoxic Activities ◽  
Significant Group ◽  
Design Synthesis ◽  
Standard Drug ◽  
Wide Range

Background: Quinolones are a significant group of nitrogen heterocyclic compounds that exist in therapeutic agents, alkaloids, and synthetic small molecules that have important biological activities. A wide range of quinolones have been used as antituberculosis, antibacterial, anti-malarial, antifungal, anticonvulsant, anticancer agents and urease inhibitors. Methods: Ethyl 3,3-disubstituted-2-cyano propionates containing hybride quinolones derivatives were synthesized by the reaction of 1-amino-7-hydroxy-4-methylquinolin-2(1H)-one and its dibromo derivative with α, β-unsaturated carbonyl in ethanol. Results: A novel series of hybrid 2-quinolone derivatives was designed and synthesized. The compounds structures were confirmed using different spectroscopic methods and elemental analysis. The cytotoxic activities of all the compounds were assessed against HepG2 cell line in comparison with doxorubicin as a standard drug. Conclusion: Most compounds revealed superior anti-proliferative activity than the standard. Compound 4b, is the most active compound (IC50 = 0.39mM) compared with doxorubicin (IC50 = 9.23mM). DNA flow cytometric analysis of compound 4b showed cell cycle arrest at G2/M phase with a concomitant increase of cells in apoptotic phase. Dual annexin-V/ propidium iodide staining assay of compound 4b revealed that the selected candidate increased the apoptosis of HepG-2 cells more than control.

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