Synthesis, in vitro anticancer evaluation and in silico studies of novel imidazo[2,1-b]thiazole derivatives bearing pyrazole moieties

Ali, Ahmed R.; El‐Bendary, Eman R.; Ghaly, Mariam A.; Shehata, Ihsan A.

doi:10.1016/j.ejmech.2013.12.010

Cited by 82 publications

(34 citation statements)

References 30 publications

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“…Compound 554j showed significant cytotoxicity in HeLa cells with IC 50 = 6.5 ± 0.56 μM. Ali et al synthesised a series of novel imidazo[2,1‐b]thiazoles bearing pyrazole moieties (Scheme ). Eleven compounds were screened at NCI and their in vitro anticancer evaluation revealed that compounds 558–560(a) were promising towards CNS SB‐75 and renal UO‐31 cancer cell lines when tested against standard drug rapamycin as standard drug.…”

Section: Pharmacological and Synthetic Profiles Of Benzimidazole Derimentioning

confidence: 99%

Benzimidazole Scaffold as Anticancer Agent: Synthetic Approaches and Structure–Activity Relationship

Shrivastava

Naim

Alam

et al. 2017

Archiv der Pharmazie

126

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Cancer, also known as malignant neoplasm, is a dreadful disease which involves abnormal cell growth having the potential to invade or spread to other parts of the body. Benzimidazole is an organic compound that is heterocyclic and aromatic in nature. It is a bicyclic compound formed by the fusion of the benzene and imidazole ring systems. It is an important pharmacophore and a privileged structure in medicinal chemistry. According to the World Health Organisation (2015 survey), one in six deaths is due to cancer around the globe, accounting for 8.8 million deaths of which 70% of the cases were from low- and middle-income countries. In the efforts to develop suitable anticancer drugs, medicinal chemists have focussed on benzimidazole derivatives. This review article covers the current development of benzimidazole-based anticancer agents along with the synthetic approaches and structure-activity relationships (SAR).

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Section: Pharmacological and Synthetic Profiles Of Benzimidazole Derimentioning

confidence: 99%

Benzimidazole Scaffold as Anticancer Agent: Synthetic Approaches and Structure–Activity Relationship

Shrivastava

Naim

Alam

et al. 2017

Archiv der Pharmazie

126

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“…The compounds (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14) were evaluated for activity against diverse RNA-and DNA-viruses, using the following cell-based assays [45] To perform the antiviral assays, the virus was added to subconfluent cell cultures in 96-well plates, and at the same time, the test compounds were added at serial dilutions. Appropriate reference compounds were included, i.e.…”

Section: Antiviral Activitymentioning

confidence: 99%

Synthesis and antiviral activity evaluation of new 4-thiazolidinones bearing an imidazo[2,1-b]thiazole moiety

Güzeldemirci¹,

Pehlivan²,

Naesens³

2018

mpj

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. INTRODUCTIONDespite significant advances in antiviral drug development during the past two decades, viral infections continue to cause serious morbidity and mortality world-wide. Diverse antiviral drugs are now available for the treatment of infections by HIV, herpes-, influenza, hepatitis B or hepatitis C viruses. Except for the broad antiviral agent ribavirin, there is no approved therapy for diverse emerging RNA viruses. In addition, new antiviral molecules are required to tackle the problems of drug toxicity and rapid development of drug resistance, which is particularly problematic for mutation-prone RNA viruses. Since virus replication occurs within host cells, and host cell metabolism and viral replication are tightly integrated, the development of compounds which selectively interfere with virus-specific process is one of the main challenges in antiviral drug design.Imidazo [21][22][23][24][25][26][27][28][29][30][31][32] (including antiviral molecules) (either as a substituent group or as a replacement for another cyclic system). For instance, several 2,3-diaryl-1,3-thiazolidin-4-ones have proved to be potent nonnucleoside HIV reverse transcriptase inhibitors (NNRTIs) [33,34]. The HIV RT is a prime target for designing HIV inhibitors [35,36].We here report the synthesis, structural determination and antiviral evaluation of . 3-alkyl/aryl-2-[((6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-nonsubstituted/methyl-4-thiazolidinones.

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“…[19][20][21] In addition, several 1,3-thiazole scaffolds have been reported as potent anticancer agents. [22][23][24] The synthesis of some new pyrazole-based 1,3-thiazoles as anticancer agents was reported. 25 Most recently, excellent anticancer effectiveness of pyrazolylthiazole derivatives was also reported, via EGFR TK inhibition that plays an important role in cell growth regulation.…”

Section: Introductionmentioning

confidence: 99%

Convenient Synthesis, Characterization, Cytotoxicity and Toxicity of Pyrazole Derivatives

Kamel

2015

ACSi

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The reaction of 1 with phenylisothiocyanate followed by treatment with the α-halocarbonyl compounds 24a-c afforded the thiazole derivatives 25a-c. The synthesized products were evaluated for their cytotoxicity against cancer and normal cell lines. Most compounds showed significant anticancer activity without affecting the normal fibroblast cells. The toxicity of the most pontent cytotoxic compounds was measured using Brine-Shrimp Lethality Assay.

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Synthesis, in vitro anticancer evaluation and in silico studies of novel imidazo[2,1-b]thiazole derivatives bearing pyrazole moieties

Cited by 82 publications

References 30 publications

Benzimidazole Scaffold as Anticancer Agent: Synthetic Approaches and Structure–Activity Relationship

Benzimidazole Scaffold as Anticancer Agent: Synthetic Approaches and Structure–Activity Relationship

Synthesis and antiviral activity evaluation of new 4-thiazolidinones bearing an imidazo[2,1-b]thiazole moiety

Convenient Synthesis, Characterization, Cytotoxicity and Toxicity of Pyrazole Derivatives

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