Synthesis and anticancer evaluation of 3-aryl-6-phenylimidazo[2,1-b]thiazoles

Koppireddi, Satish; Chilaka, Deepika Raj Kumari; Avula, Sreenivas; Komsani, Jayaram Reddy; Kotamraju, Srigiridhar; Yadla, R.

doi:10.1016/j.bmcl.2014.10.030

Cited by 46 publications

(16 citation statements)

References 20 publications

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“…Compound 550b showed potent in vitro anti‐tumour activity against Huh‐7 hepatocarcinoma cell line with IC 50 = 16.22 μg/mL. Koppireddi et al synthesised a series of new 3,6‐diphenylimidazo[2,1‐b]thiazole derivatives (Scheme ) and evaluated for anticancer activity against HeLa, MDA‐MB‐231, A549 and THP1 human cancer cell lines. Compound 554j showed significant cytotoxicity in HeLa cells with IC 50 = 6.5 ± 0.56 μM.…”

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

127

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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

127

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“…1,3-Thiazoles undergo different types of reactions to yield various biologically active fused heterocyclic moieties as thiazolopyrimidine, imidazothiazoles, thiazolopyridine, etc. [19][20][21].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of Thiazole Derivatives

Ibrahim¹,

Rizk²

2021

Azoles - Synthesis, Properties, Applications and Perspectives

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Thiazoles belong to the group of azole heterocycles. They are aromatic five-membered heterocycles containing one sulfur and one nitrogen atom. In recent years thiazoles, their derivatives, and isomers have gained considerable attention because of their broad applications in different fields, such as agrochemicals, industrial, and photographic sensitizers. Also, they have pharmaceutical and biological activities that include antimicrobial (sulfazole), antiretroviral (ritonavir), antifungal (abafungin), anticancer (tiazofurin), antidiabetic, anti-inflammatory, anti-Alzheimer, antihypertensive, antioxidant, and hepatoprotective activities. The compounds containing thiazole moieties are a prominent structural feature in a variety of natural products, such as vitamin B and penicillin. Thus, in this chapter several types of thiazole-based heterocyclic scaffolds such as monocyclic or bicyclic systems synthesis and their biological activities studies are presented. Furthermore modification of thiazole-based compounds at different positions to generate new molecules with potent antitumor, antioxidant, and antimicrobial activities is described.

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“…In addition, thiazoles are valuable basic units in the field of medicinal science and are found in a wide assortment of bioactive scaffolds [10,11]. It has been well established that they possess antibacterial [12,13], anti-inflammatory [14,15], antitubercular [16,17], anticonvulsant [18,19], and anticancer [20][21][22][23] activities. Aminothiazole-containing medicines have been applied in clinical use for over thirty years, e.g., Famotidine is used to treat and prevent gastroesophageal reflux disease [24,25], Abafungin as an antifungal agent is used in the treatment of dermatomycoses [26] and Cefdinir is a well-known FDA-approved antibiotic and a third generation broad-spectrum cephalosporin [27].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Modeling Study and Antioxidants Activity of New Heterocycles Derived from 4-Antipyrinyl-2-Chloroacetamidothiazoles

Abu‐Melha

2018

Applied Sciences

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The present work reports the preparation of twelve new heterocyclic scaffolds containing an antipyrinyl-thiazole hybrid through the reaction of 4-antipyrinyl-2-chloroacetamido-thiazoles 1 and 6 with various types of nucleophiles, namely; ethyl thioglycolate, 2-mercaptobenzothiazole, 2-mercaptobenzoxazole, ammonium thiocyanate, malononitrile, and salicylaldehyde. The constructed compounds were characterized by conventional spectroscopic techniques (IR, 1H NMR, 13C NMR, and mass analysis). A DFT method (material studio package) was used to predict the geometry, bond lengths, bond angles, and dipole moments as well as other global chemical reactivities of the constructed antipyrinyl-thiazole compounds. Also, their semi-core pseudopods calculations (dspp) were carried out with DNP (double numerical basis sets plus polarization functional) to predict the properties of materials. In addition, the antioxidant activity of these antipyrinyl-thiazole scaffolds has been screened by the ABTS method. The results indicated that 2-(4-antipyrinylthiazolylamino)-5-substituitedbenzylidene-thiazol-4(5H)-ones 10b and 10c exhibited the best antioxidant activity with a percentage inhibition of 85.74% and 83.51%, respectively.

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Synthesis and anticancer evaluation of 3-aryl-6-phenylimidazo[2,1-b]thiazoles

Cited by 46 publications

References 20 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 Biological Evaluation of Thiazole Derivatives

Synthesis, Modeling Study and Antioxidants Activity of New Heterocycles Derived from 4-Antipyrinyl-2-Chloroacetamidothiazoles

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