Methods for the prepation of azolo-fused systems with thiophene core

Shyyka, Olga Ya.

doi:10.30970/vch.5902.239

Cited by 2 publications

(2 citation statements)

References 16 publications

(27 reference statements)

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“…Thieno-fused five-and six-membered nitrogen containing heterocycles [1] play an important role in medical and pharmaceutical chemistry. One of the reasons is that several of fused cores are bioisosters to the natural purine bases.…”

Section: Introductionmentioning

confidence: 99%

Anticancer activity evaluation of thieno[3,2-e][1,2,3]triazolo[1,5-a]pyrimidines and thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine derivatives

2019

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In vitro evaluation of anticancer activity of synthesized thieno[3,2-e][1,2,3]triazolo[1,5-a] pyrimidines and thieno[2,3-e][1,2,3]triazolo[1,5-a] pyrimidines. Methods. Organic synthesis, in vitro cytotoxicity assay, MTT assay, spectrophotometry, statistical analysis. Results. The isomeric thienotriazolopyrimidines synthesized were tested for their anticancer activity in the NCI-60 cancer cell line panel, a group of 60 human cancer cell lines. The selective influence of 5-oxo-4,5,6,7,8,9-hexahydrobenzo[4,5]thieno[3,2-e][1,2,3]triazolo[1,5-a]pyrimidine-3-carboxamide on melanoma cell line SK-MEL-5 with (GP =-31,50%) was observed. Two compounds possessed a significant activity on CNS and breast cancer cells.Conclusions. Several thienotriazolopyrimidines were found to possess antitumor activity with a selective effect on a single cell line. These results are interesting for further structure optimization to increase selectivity and anticancer activity of fused pyrimidines.

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Section: Introductionmentioning

confidence: 99%

Anticancer activity evaluation of thieno[3,2-e][1,2,3]triazolo[1,5-a]pyrimidines and thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine derivatives

2019

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“…[16] Thiadiazole chemistry has attracted an immense attention in pharmaceutical, medicinal, and agromedical fields in current years. [17] Thiadiazoles containing organic compounds are continuously drawing interest for development of new drug moieties. Of the several isomers of thiadiazole, such as 1,2,3-, 1,2,4-, 1,2,5-, and 1,3,4-thiadiazoles, only 1,3,4-has been studied extensively due to the presence of toxophoric -N=C-S group.…”

Section: Introductionmentioning

confidence: 99%

Phosphosulfonic acid‐catalyzed green synthesis and bioassay of α‐aryl‐α′‐1,3,4‐thiadiazolyl aminophosphonates

Gundluru

Sarva

Kandula

et al. 2016

Heteroatom Chemistry

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A series of new α‐aminophosphonates containing 1,3,4‐thiadiazole moiety (4a–l) were synthesized via a simple, efficient, and one‐pot three‐component Kabachnik–Fields reaction of 2‐amino‐5‐ethyl‐1,3,4‐thiadiazole with various aryl/heteroaryl aldehydes and diethylphosphite under solvent‐free microwave irradiation conditions using phosphosulfonic acid, as a reusable and heterogeneous solid acid catalyst. All the title compounds were screened for radical scavenging activity by DPPH and H2O2 methods, and antimicrobial activity against bacteria (Gram‐positive and Gram‐negative) and fungi using the disc diffusion technique. They exhibited potent in vitro antioxidant and moderate antimicrobial activity.

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Methods for the prepation of azolo-fused systems with thiophene core

Cited by 2 publications

References 16 publications

Anticancer activity evaluation of thieno[3,2-e][1,2,3]triazolo[1,5-a]pyrimidines and thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine derivatives

Anticancer activity evaluation of thieno[3,2-e][1,2,3]triazolo[1,5-a]pyrimidines and thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine derivatives

Phosphosulfonic acid‐catalyzed green synthesis and bioassay of α‐aryl‐α′‐1,3,4‐thiadiazolyl aminophosphonates

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