Synthesis, anticancer activity and mechanism of action of new thiazole derivatives

Santana, Temístocles Ítalo de; Barbosa, Míria de Oliveira; Gomes, Paulo André Teixeira de Moraes; Cruz, Anne Cecília Nascimento da; Silva, Teresinha Gonçalves da; Leite, Ana Cristina Lima

doi:10.1016/j.ejmech.2017.12.040

Cited by 160 publications

(78 citation statements)

References 50 publications

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“…Santana et al 10 reported the synthesis of new substances belonging to thiosemicarbazones and thiazoles to develop powerful therapeutic agents for cancer treatment. The intermediate thiosemicarbazones were prepared in reaction between the 4'-trifluoromethylbenzaldehyde with the corresponding thiosemicarbazide under reflux and catalytic amount of HCl.…”

Section: Synthesis Of Thiazole and Thiazolyl Derivativesmentioning

confidence: 99%

Synthesis of new thiazole and thiazolyl derivatives of medicinal significant-a short review

Hussein¹,

Turan-Zitouni²

2018

MOJBOC

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In the field of therapeutic science, thiazoles are of extraordinary importance, because of their potent and significant biological activities. Likewise thiazole and their derivatives are found in various powerful naturally and biologically active compounds which possess a broad spectrum of biological activity therefore, synthesis of this compound is of remarkable concern. This review primarily focuses on the updated research papers reported in literature for the synthesis of thiazole and thiazolyl compounds.Citation: Hussein W, Zitouni TG. Synthesis of new thiazole and thiazolyl derivatives of medicinal significant-a short review. MOJ Biorg Org Chem. 2018;2(2):52-55.

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Section: Synthesis Of Thiazole and Thiazolyl Derivativesmentioning

confidence: 99%

Synthesis of new thiazole and thiazolyl derivatives of medicinal significant-a short review

Hussein¹,

Turan-Zitouni²

2018

MOJBOC

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“…The last years of the research have confirmed that thiazole scaffold has diverse biological properties that can be used to treat many diseases, such as microbial infections (Bikobo et al 2017;Secci et al 2012;Łączkowski et al 2018a, 2018bZaki et al 2018;Ansari et al 2018), Parkinson's disease (Carradori et al 2018), cancer (de Santana et al 2018;Łączkowski et al 2014, 2016a, 2016bPiechowska et al 2019;Gomha et al 2018), epilepsy (Siddiqui and Ahsan 2010;Ahangar et al 2011;Łączkowski et al 2016a, 2016b, toxoplasmosis (Schultz et al 2014;Łączkowski et al 2018a, 2018b, and antioxidants (Geronikaki et al 2013;Djukic et al 2018). Considering the above-mentioned findings, we decided to design and synthesize the structure of hybrids incorporating both the thiazole ring and the cyclohexenyl moiety.…”

Section: Introductionmentioning

confidence: 98%

Synthesis, antimicrobial activity, and determination of the lipophilicity of ((cyclohex-3-enylmethylene)hydrazinyl)thiazole derivatives

et al. 2019

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Synthesis and investigation of antimicrobial activity of fifteen novel thiazoles containing cyclohexene moiety are presented. Among the derivatives, compounds 3a-3d, 3f, 3n, and 3o showed very strong activity against the reference Candida spp. strains with MIC = 0.015-3.91 µg/ml. The activity of these compounds is similar and even higher than the activity of nystatin used as positive control. Compounds 3d, 3f, 3n, 3o showed the highest activity with very strong effect towards most of yeasts isolated from clinical materials with MIC = 0.015-7.81 µg/ml. The cytotoxicity studies for the most active compounds showed that Candida spp. growth was inhibited at noncytotoxic concentrations for the mammalian L929 fibroblast. In addition, a good correlation was obtained between lipophilicity of compounds determined using reversed phase thin-layer chromatography and their antifungal activity.

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“…Thiazole ring is a structural fragment of natural compounds such as thiamine (vitamin B1), thiamine pyrophosphate, epothilones, carboxylase, and the large family of macrocyclic thiopeptide antibiotics, thiostrepton and micrococcin P1 . Thiazole derivatives are associated with a broad spectrum of biological properties, including anticancer, antitumor, anticonvulsant, antimicrobial, antituberculous and bacteriostatic activities ( Figure ) . Therefore, we focused on attention to club theses heterocycles in one molecular framework to synthesize new hybrids thiazolyl acridinedione.…”

Section: Introductionmentioning

confidence: 99%

“…[24,25] Thiazole derivatives are associated with a broad spectrum of biological properties, including anticancer, antitumor, anticonvulsant, antimicrobial, antituberculous and bacteriostatic activities (Figure 1). [26][27][28][29] Therefore, we focused on attention to club theses heterocycles in one molecular framework to synthesize new hybrids thiazolyl acridinedione.…”

Section: Introductionmentioning

confidence: 99%

Organocatalyzed Domino Synthesis of New Thiazole‐Based Decahydroacridine‐1,8‐diones and Dihydropyrido[2,3‐d : 6,5‐d′]‐ dipyrimidines in Water as Antimicrobial Agents

Bhosle

Kharote

Bondle

et al. 2020

Chemistry & Biodiversity

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Organopromoter, 2‐aminoethanesulfonic acid was used to catalyze the synthesis of a series of structurally intriguing new hybrids thiazolyl acridine‐1,8(2H,5H)‐diones and dihydropyrido[2,3‐d : 6,5‐d′]dipyrimidine‐2,4,6,8(1H,3H,5H,7H)‐tetraones for the first time. 2‐Aminoethanesulfonic acid is a biobased organopromoter, used to generate four new bonds for the synthesis of new coupled thiazole‐based decahydroacridine‐1,8‐diones. Superior green credentials, operational simplicity, easy work‐up and recyclability of the catalyst are the key strengths of this method. The broad substrate scope, mild reaction conditions, short reaction time, cost effectiveness, high atom economy and good to excellent yields make the present method a distinct improvement over existing methods. Spectral (IR, 1H‐NMR,13C‐NMR, Mass) data and elemental analyses confirmed the structures of the titled products. A series of thiazolyl acridine‐1,8(2H,5H)‐diones and dihydropyrido[2,3‐d : 6,5‐d′]dipyrimidine‐2,4,6,8(1H,3H,5H,7H)‐tetraones were screened for their antimicrobial activity against four bacterial and three fungal strains.

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Synthesis, anticancer activity and mechanism of action of new thiazole derivatives

Cited by 160 publications

References 50 publications

Synthesis of new thiazole and thiazolyl derivatives of medicinal significant-a short review

Synthesis of new thiazole and thiazolyl derivatives of medicinal significant-a short review

Synthesis, antimicrobial activity, and determination of the lipophilicity of ((cyclohex-3-enylmethylene)hydrazinyl)thiazole derivatives

Organocatalyzed Domino Synthesis of New Thiazole‐Based Decahydroacridine‐1,8‐diones and Dihydropyrido[2,3‐d : 6,5‐d′]‐ dipyrimidines in Water as Antimicrobial Agents

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