Synthesis and antitumor activity of novel N-(5-benzyl-4-(tert-butyl)thiazol-2-yl)-2-(piperazin-1-yl)acetamides

Wu, Zhilin; Ding, Na; Tang, YH; Ye, Jiao; Peng, Junmei; Hu, Aiguo

doi:10.1007/s11164-017-2915-6

Cited by 7 publications

(3 citation statements)

References 30 publications

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“…Replacement of X with Cl in the para-position of phenyl created most activity against three A549 cells, HeLa cells, and MCF-7cell lines (Fig. 6) [52].…”

Section: Structural Modification Of 2-amine Group Of 2-aminothiazole Frameworkmentioning

confidence: 96%

Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

Alizadeh

Hashemi

2021

Med Chem Res

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Currently, the development of anticancer drug resistance is significantly restricted the clinical efficacy of the most commonly prescribed anticancer drug. Malignant disease is widely prevalent and considered to be the major challenges of this century, which concerns the medical community all over the world. Consequently, investigating small molecule antitumor agents, which could decrease drug resistance and reduce unpleasant side effect is more desirable. 2-aminothiazole scaffold has emerged as a promising scaffold in medicinal chemistry and drug discovery research. This nucleus is a fundamental part of some clinically applied anticancer drugs such as dasatinib and alpelisib. Literature survey documented that different 2aminothiazole analogs exhibited their potent and selective nanomolar inhibitory activity against a wide range of human cancerous cell lines such as breast, leukemia, lung, colon, CNS, melanoma, ovarian, renal, and prostate. In this paper, we have reviewed the progresses and structural modification of 2-aminothiazole to pursuit potent anticancers and also highlighted in vitro activities and in silico studies. The information will useful for future innovation.

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“…Replacement of X with Cl in the para-position of phenyl created most activity against three A549 cells, HeLa cells, and MCF-7cell lines (Fig. 6) [52].…”

Section: Structural Modification Of 2-amine Group Of 2-aminothiazole Frameworkmentioning

confidence: 96%

Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

Alizadeh

Hashemi

2021

Med Chem Res

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“…and co-workers also stated that this compound stopped G1 phase cell cycle, which causes cell apoptosis. 50 Ciprofloxacin is an antibiotic having apoptotic and antiproliferative activity.…”

Section: Piperazinementioning

confidence: 99%

Heterocyclic Compounds and their Derivatives with Potential Anticancer Activity

Kaur,

Shakya,

Singh

et al. 2024

Ind. J. Pharm. Edu. Res

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Cancer is the second leading cause of the death worldwide. As per the reports published by WHO, the cases of cancer in the world will increase to 22 million by 2030. Many resources are investigated all around the world for developing preventive, diagnostic and therapeutic strategies for cancer. Malignant cells display metabolic changes because of genetic and epigenetic alterations as compared to normal cell. Heterocycles are the key structural feature of many anti-cancer drugs present in the market. Between 2010 to 2015, FDA approved anticancer drugs also contain heterocyclic rings in their structures. Their presence in anti-cancer drugs can be credited to their being extremely common in nature, with enormous cellular processes and mechanisms. This review throws light on several heterocyclic compounds containing nitrogen, sulphur and oxygen in their rings, possessing anticancer activity on different cell lines. A compiled data of heterocyclic rings will help in providing a new way towards future development of new compound for treatment of cancer.

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“…Cell viability is commonly evaluated through staining with acridine orange (AO) or ethidium bromide (EB) [26,27]. AO is a fluorescent dye that can cross intact cell membranes and emit green fluorescence when combined with DNA.…”

Section: Cell Viabilitymentioning

confidence: 99%

Microwave-induced release and degradation of airborne endotoxins from Escherichia coli bioaerosol

WANG

Zhang

Liu

2019

Journal of Hazardous Materials

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Endotoxins are widely distributed toxins in the outer cell-wall membranes of Gram-negative bacteria and other microorganisms. Chronic exposure to endotoxins can induce and exacerbate airway symptoms and diseases. However, the release and degradation of airborne endotoxins from bioaerosol by microwave (MW) irradiation have not yet been reported. This study investigated the distribution and fate of airborne endotoxins during MW irradiation process, as well as the kinetics and thermodynamics of the degradation of airborne endotoxins. Results showed that MW irradiation induced cell lysis, thus considerably increasing the proportion of cells with ruptured membranes. Furthermore, MW irradiation changed the distribution of airborne endotoxins, sharply decreased the concentration of bound endotoxins from 230 EU/m 3 to 68 EU/m 3 , and increased the concentration of free endotoxins from 21 EU/m 3 to 122 EU/m 3 . These results indicated that MW irradiation released endotoxins from cells into the atmosphere. MW irradiation likely degraded endotoxins by exerting thermal effects, which achieved a total endotoxin removal efficiency of as high as 35%. Endotoxin degradation was a first-order reaction and required the activation energy of 26.3 kJ/mol. Fig. 7. Thermodynamic of airborne endotoxin degradation. (A) Endotoxin removal efficiency under various temperatures. (B) Relationship between the reaction rate constant of endotoxin lnk and temperature 1/T. (Error bar presents standard deviation, n presents numbers of samples, n = 3). C. Wang et al.

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Synthesis and antitumor activity of novel N-(5-benzyl-4-(tert-butyl)thiazol-2-yl)-2-(piperazin-1-yl)acetamides

Cited by 7 publications

References 30 publications

Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

Heterocyclic Compounds and their Derivatives with Potential Anticancer Activity

Microwave-induced release and degradation of airborne endotoxins from Escherichia coli bioaerosol

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