Diarylamine-Guided Carboxamide Derivatives: Synthesis, Biological Evaluation, and Potential Mechanism of Action DOI Creative Commons
Shaoyong Ke, Wenbo Huang, Zhigang Zhang

et al.

Frontiers in Chemistry, Journal Year: 2022, Volume and Issue: 10

Published: July 12, 2022

Diarylamines are a class of important skeleton widely existing in drugs or natural products. To discover novel diarylamine analogues as potential drugs, two series diamide and carboxamide derivatives containing scaffold were designed, synthesized evaluated for their cytotoxic activities. The bioassay results indicated that some the obtained compounds (C5, C6, C7, C11) exhibited good effect on cancer cell lines (SGC-7901, A875, HepG2), especially, compound C11 present significantly selective proliferation inhibition activity normal (MARC145). In addition, possible apoptosis induction highly molecules was investigated, which could be used lead discovery promising anticancer agents.

Language: Английский

Nitrogen Containing Heterocycles as Anticancer Agents: A Medicinal Chemistry Perspective DOI Creative Commons
Adarsh Kumar, Ankit Kumar Singh, Harshwardhan Singh

et al.

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

Citations

148
Current status of carbazole hybrids as anticancer agents DOI

Gangqiang Wang,

Shaofa Sun,

Hua Guo

et al.

European Journal of Medicinal Chemistry, Journal Year: 2021, Volume and Issue: 229, P. 113999 - 113999

Published: Nov. 20, 2021

Language: Английский

Citations

52
Eco-friendly synthesis, characterization, in-silico ADMET and molecular docking analysis of novel carbazole derivatives as antibacterial and antifungal agents DOI
Oussama Merzouki,

N. Arrousse,

Azeddin El Barnossi

et al.

Journal of Molecular Structure, Journal Year: 2022, Volume and Issue: 1271, P. 133966 - 133966

Published: Aug. 20, 2022

Language: Английский

Citations

32
Update on novel synthetic approaches towards the construction of carbazole nuclei: a review DOI Creative Commons
Saba Munawar, Ameer Fawad Zahoor, Asim Mansha

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(5), P. 2929 - 2946

Published: Jan. 1, 2024

The carbazole scaffold is a significant entity in organic compounds due to its variety of biological and synthetic applications. Traditionally, skeletons have been synthesized either via the Grabe-Ullman method, Clemo-Perkin method or Tauber method. With passage time, these methods modified explored accomplish synthesis target compounds. These include hydroarylations, C-H activations, annulations cyclization reactions mediated by catalysts construct carbazole-based This brief review article intends provide recent updates on important methodological developments reported for nuclei covering 2019-2023.

Language: Английский

Citations

8
Diverse pharmacological actions of potential carbazole derivatives by influencing various pathways of molecular signaling DOI Creative Commons
Archita Tiwari, Bharat Mishra

Future Journal of Pharmaceutical Sciences, Journal Year: 2024, Volume and Issue: 10(1)

Published: June 17, 2024

Abstract Background Carbazoles are an important class of heterocyclic aromatic compounds that contain nitrogen atom in the ring. They have a large-conjugated system, attractive “electrical and charge-transport properties”, ability to efficiently incorporate different functional groups into structurally inflexible carbazolyl Main text Carbazole derivative ECCA acts as anticancer agent by reactivating P53 molecular signaling pathway; similarly, some other derivatives carbazole show antifungal activity acting on RAS-MAPK pathway. also their effect inflammation inhibiting p38 mitogen-activated protein kinase pathway stopping conversion DAXX ASK-1. By modifying AKT through boosting phosphatase brain, they anti-Alzheimer’s translocating GLUT4 these effective against diabetes. Conclusion After exploring literature carbazole, it was found has immeasurably great potential for treatment various diseases nucleus leads synthesized which used pharmacological activities. So there is need explore newer drugs.

Language: Английский

Citations

6
Synthesis and investigation of bis(phenyl)fluorene and carbazole appended dipodal Schiff base for fluorescence sensing towards Sn(II) ion and its regioselective polymerization DOI
Feyza Kolcu,

Süleyman Çulhaoğlu,

İsmet Kaya

et al.

Journal of Photochemistry and Photobiology A Chemistry, Journal Year: 2023, Volume and Issue: 441, P. 114665 - 114665

Published: March 9, 2023

Language: Английский

Citations

12
Design, Synthesis and Various Bioactivity of Acylhydrazone-Containing Matrine Analogues DOI Creative Commons

Wanjun Ni,

Hongjian Song, Lizhong Wang

et al.

Molecules, Journal Year: 2023, Volume and Issue: 28(10), P. 4163 - 4163

Published: May 18, 2023

Compounds with acylhydrazone fragments contain amide and imine groups that can act as electron donors acceptors, so they are easier to bind biological targets thus generally exhibit significant activity. In this work, were introduced the C-14 or C-11 position of matrine, a natural alkaloid, aiming enhance their activities. The result bioassay showed many synthesized compounds exhibited excellent anti-virus activity against tobacco mosaic virus (TMV). Seventeen out 25 14-acylhydrazone matrine derivatives 17 20 11-butanehydrazone had higher inhibitory TMV than commercial antiviral agent Ribavirin (the in vitro activity, vivo inactivation, curative protection activities at 500 µg/mL 40.9, 36.5 ± 0.9, 38.0 1.6 35.1 2.2%, respectively), four even similar most efficient Ningnanmycin (55.4, 57.8 1.4, 55.3 0.5 60.3 1.2% for above test modes). Among them, N-benzyl-11-butanehydrazone formed 4-bromoindole-3-carboxaldehyde best anti-TMV (65.8, 71.8 2.8, 66.8 1.3 69.5 3.1% µg/mL; 29, 33.5 0.7, 24.1 0.2 30.3 0.6% 100 modes), deserving further investigation an agent. Other these, two series acylhydrazone-containing evaluated insecticidal fungicidal Several found have good diamondback moth (Plutella xylostella) mosquito larvae (Culex pipiens pallens), showing broad

Language: Английский

Citations

12
Anticancer agents incorporating the N‐acylhydrazone scaffold: Progress from 2017 to present DOI
Asmaa E. Kassab

Archiv der Pharmazie, Journal Year: 2023, Volume and Issue: 356(5)

Published: Jan. 13, 2023

Abstract The N ‐acylhydrazone motif has been shown to be particularly adaptable and promising in the area of medicinal chemistry drug development, due its significant biological pharmacological characteristics. Moreover, ‐acylhydrazones are appealing synthetic tools because their simple straightforward synthesis. This scaffold emerged as a fundamental building block for synthesis bioactive compounds. Particularly, served base number potent anticancer agents acting via different mechanisms. An updated summary activity derivatives described literature (from 2017 2022) is provided current review. It discusses structure–activity relationship (SAR) exhibiting potential, which could helpful designing developing new effective antiproliferative candidates future.

Language: Английский

Citations

11
Synthesis, Biological Evaluation and Molecular Modeling Studies of Quinazolin-4(3h)-One and Benzenesulfonamide Hybrids as Potential Anticancer Agents DOI
Emre Kadir Ayan, Ali Ergüç, Ege Arzuk

et al.

Published: Jan. 1, 2025

Language: Английский

Citations

0
2-Alkynyl Indole-3-carbonitriles: Synthon for the Regioselective Synthesis of Functionalized 4-Aminocarbazoles DOI
D. K. Panda,

Shivam A. Meena,

Manvi Sharma

et al.

The Journal of Organic Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: March 26, 2025

An operationally easy and atom-economical approach for the regioselective tandem synthesis of functionalized 4-aminocarbazoles from easily accessible 2-alkynyl indole-3-carbonitriles under mild reaction conditions has been developed. The developed chemistry involves aza-Henry successive annulation to afford carbazoles. Replacement nitromethane with acetophenone led formation corresponding amino(phenyl)methanone-substituted carbazoles, further extending diversity chemistry. methodology accommodates wide functional group variation on alkyne is successfully applied late-stage modification bioactive molecules.

Language: Английский

Citations

0