Nitrogen Containing Heterocycles as Anticancer Agents: A Medicinal Chemistry Perspective

Pharmaceuticals, Journal Year: 2023, Volume and Issue: 16(2), P. 299 - 299

Published: Feb. 14, 2023

Cancer is one of the major healthcare challenges across globe. Several anticancer drugs are available on market but they either lack specificity or have poor safety, severe side effects, and suffer from resistance. So, there a dire need to develop safer target-specific drugs. More than 85% all physiologically active pharmaceuticals heterocycles contain at least heteroatom. Nitrogen constituting most common heterocyclic framework. In this study, we compiled FDA approved with nitrogen atoms their pharmacological properties. Moreover, reported containing heterocycles, including pyrimidine, quinolone, carbazole, pyridine, imidazole, benzimidazole, triazole, β-lactam, indole, pyrazole, quinazoline, quinoxaline, isatin, pyrrolo-benzodiazepines, pyrido[2,3-d]pyrimidines, which used in treatment different types cancer, concurrently covering biochemical mechanisms action cellular targets.

Language: Английский

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Benzimidazole and its derivatives: Recent Advances (2020–2022)

Results in Chemistry, Journal Year: 2023, Volume and Issue: 5, P. 100925 - 100925

Published: Jan. 1, 2023

Benzimidazoles are fused heterocyclic ring systems containing two nitrogen atoms. They have vital therapeutic significance in drug discovery. Many clinically approved drugs been developed from benzimidazole, and these include liarozole pracinostat (anticancer), omeprazole (proton pump inhibitors), oxfendazole (Anthelmintic), enviroxine (antiviral), ilaprazole (antiulcer), ridinilazole (antibacterial), flubendazole (antiparasitic), bilastine (antihistaminic), many more. The vast applications of benzimidazole its derivatives propelled researchers to develop more biologically active compounds bearing thus broadening the scope finding a remedy for other diseases; as result, new pharmaceutical expected be available within next decade. In this review, we describe bioactive hybrids recent year, 2020 2022, accentuate pros using development.

Language: Английский

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Benzimidazole based derivatives as anticancer agents: Structure activity relationship analysis for various targets

Journal of Heterocyclic Chemistry, Journal Year: 2021, Volume and Issue: 59(1), P. 22 - 66

Published: Aug. 28, 2021

Abstract Benzimidazole, the benzo derivative of imidazole, is a class bicyclic aromatic organic compound consisting six‐membered benzene ring fused to five‐membered imidazole at 4‐ and 5‐positions ring. It vital pharmacophore many biologically active heterocyclic compounds with variety pharmacological activities. Over time, benzimidazole its derivatives have evolved as vibrant systems due their potency in wide range bioactive like analgesics, antifungals, anti‐inflammatory, antihypertensives, proton pump inhibitors, anti‐HIV, antiviral, so on. Multi‐drug resistance cancer that led failure chemotherapeutic drugs major concern. Various approaches are being developed overcome this problem. One them target based drug discovery, which an effective method develop novel anticancer drug. To newer drugs, previously reported work needs be studied. Keeping mind, last 5 years literature on used agents has been reviewed summarized paper herein. This review article along also deal structure activity relationship various having

Language: Английский

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Design and synthesis of novel benzoazoninone derivatives as potential CBSIs and apoptotic inducers: In Vitro, in Vivo, molecular docking, molecular dynamics, and SAR studies

Bioorganic Chemistry, Journal Year: 2022, Volume and Issue: 127, P. 105995 - 105995

Published: June 30, 2022

Language: Английский

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Benzimidazole hybrids as anticancer drugs: An updated review on anticancer properties, structure–activity relationship, and mechanisms of action (2019–2021)

Archiv der Pharmazie, Journal Year: 2022, Volume and Issue: 355(6)

Published: April 6, 2022

Abstract Cancer, characterized by a deregulation of the cell cycle which mainly results in progressive loss cellular differentiation and uncontrolled growth, remains prominent cause death across world. Almost all currently available anticancer agents used clinical practice have developed multidrug resistance, creating an urgent need to develop novel chemotherapeutics. Benzimidazole derivatives could exert properties through diverse mechanisms, inclusive disruption microtubule polymerization, induction apoptosis, (G2/M) arrest, antiangiogenesis, blockage glucose transport. Moreover, several benzimidazole‐based already been approved for treatment cancers. Hence, benzimidazole are useful scaffolds development agents. In particular, hybrids dual or multiple antiproliferative activities had potential overcome drug demonstrating as prototypes deployment control eradication The purpose present review article is provide comprehensive landscape agents, structure–activity relationship well mechanisms action also discussed facilitate further rational design more effective candidates, covering articles published from 2019 2021.

Language: Английский

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A Review of the Recent Developments of Molecular Hybrids Targeting Tubulin Polymerization

International Journal of Molecular Sciences, Journal Year: 2022, Volume and Issue: 23(7), P. 4001 - 4001

Published: April 4, 2022

Microtubules are cylindrical protein polymers formed from αβ-tubulin heterodimers in the cytoplasm of eukaryotic cells. Microtubule disturbance may cause cell cycle arrest G2/M phase, and anomalous mitotic spindles will form. an important target for cancer drug action because their critical role mitosis. Several microtubule-targeting agents with vast therapeutic advantages have been developed, but they often lead to multidrug resistance adverse side effects. Thus, single-target therapy has drawbacks effective control tubulin polymerization. Molecular hybridization, based on amalgamation two or more pharmacophores bioactive conjugates engender a single molecular structure enhanced pharmacokinetics biological activity, compared parent molecules, recently become promising approach development. The practical application combined active scaffolds targeting polymerization inhibitors corroborated past few years. Meanwhile, different designs syntheses novel anti-tubulin hybrids broadly studied, illustrated, detailed literature. This review describes various reported structural–activity relationships (SARs) where it is possible effort generate efficacious inhibitors. aim create platform which new can be modeled improved inhibitory potency hence, development against cancer.

Language: Английский

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Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships

ChemistrySelect, Journal Year: 2023, Volume and Issue: 8(26)

Published: July 10, 2023

Abstract Cancer is a wide collection of diseases and among the numerous pathways involved in cancer pathogenesis, pathway involving epidermal growth factor receptor (EGFR) one most prominent. EGFR frequently articulated variety such as breast cancer, pancreatic non‐small cell lung (NSCLC), head neck cancer. There are different tyrosine kinase inhibitors (TKIs) approved by FDA for treatment However, none them evidenced boon to oncological medical department. Frequently occurrence inherent acquired resistance TKIs result mutations principal cause current situation. Therefore, researchers desire evolving novel TKIs. Further, N ‐heterocyclic ring system always proved be magical weapon designed discovery synthetic molecules they comprehensive range pharmacological properties. In recent year (2018–2022) derivatives were uncovered potential The present review summarised research progress dazed limitations currently accessible drugs consecrating, anatomy, mutation EGFR, its role types highlights medicinal chemistry prospective emphasising about designing strategies, docking studies, biological evaluation, selectivity structural activity relationship compounds. Our will support chemists direction development based

Language: Английский

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In vitro and in vivo anti-pigmentation effects of 2-mercaptobenzimidazoles as nanomolar tyrosinase inhibitors on mammalian cells and zebrafish embryos: Preparation of pigment-free zebrafish embryos

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 266, P. 116136 - 116136

Published: Jan. 9, 2024

Language: Английский

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Synthesis and biological evaluation of 1-phenyl-4,6-dihydrobenzo[b]pyrazolo[3,4-d]azepin-5(1H)-one/thiones as anticancer agents

Bioorganic Chemistry, Journal Year: 2023, Volume and Issue: 135, P. 106478 - 106478

Published: March 17, 2023

Language: Английский

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Discovery of Pyrazole-5-yl-amide Derivatives Containing Cinnamamide Structural Fragments as Potential Succinate Dehydrogenase Inhibitors

Journal of Agricultural and Food Chemistry, Journal Year: 2023, Volume and Issue: unknown

Published: Nov. 3, 2023

To promote the development of novel agricultural succinate dehydrogenase inhibitor (SDHI) fungicides, we introduced cinnamamide and nicotinamide structural fragments into structure pyrazol-5-yl-amide by carbon chain extension scaffold hopping, respectively, synthesized a series derivatives. The results biological activity assays indicated that most target compounds exhibited varying degrees inhibitory against tested fungi. Notably, G22, G28, G34, G38, G39 excellent in vitro antifungal activities Valsa mali with EC50 values 0.48, 0.86, 0.57, 0.73, 0.87 mg/L, this result was significantly more potent than boscalid (EC50 = 2.80 mg/L) closer to specialty control drug tebuconazole 0.30 mg/L). Compounds G22 G34 also vivo protective curative effects V. at 40 mg/L. SEM TEM observations may affect normal mycelial morphology as well cellular ultrastructure. Molecular docking analysis possessed similar binding mode SDH, detailed SDH inhibition validated feasibility designed potential inhibitors. G3 were selected for theoretical calculations, terminal carboxylic acid group be key region influencing activity. Furthermore, toxicity tests on Apis mellifera l. revealed low A. populations. above demonstrated these pyrazole-5-yl-amide derivatives are promising low-risk drug-resistance SDHI fungicides.

Language: Английский

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