Retracted: Design, Synthesis and Molecular Modeling of Nonsteroidal Anti‐inflammatory Drugs Tagged Substituted 1,2,3‐Triazole Derivatives and Evaluation of Their Biological Activities

Abstract

A novel series of 1,4-disubstituted-1,2,3-triazole derivatives 3a-l and 5a-i were one-pot synthesized via CuAAC-alkyne click chemistry and evaluated for their antibacterial activity against four organisms and screened for their anticancer activity against human colon cancer cell line HT-29 and human lung cancer cell line HTB-29. These hybrid molecules structure elucidation has been performed by IR, 1 H-NMR, 13 C-NMR, and mass spectral analysis. Synthesized nonsteroidal anti-inflammatory drugs-triazoles evaluated for their antibacterial activities against bacterial microorganisms Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, and Klebsiella pneumonia. Final compounds 3i, 3c, and 5b showed magnificent broad spectrum activity against P. aeruginosa, K. pneumonia, E. coli, and S. aureus with zone of inhibition values of 20, 15, 17, and 16 mm, respectively. Among the series of compound, 3j showed the best antibacterial activity against all the strains. Further, the compounds 3i and 5a were more cytotoxic than cisplatin against all tested two human cancer cell lines, with 50.8%, and 52.3% and 73.4% and 75.3% of growth, respectively. The synthesized compounds were tested for kinase inhibitory activity against glycogen synthase kinase-3 protein kinases, in addition, for cytotoxic activity against two different human cancer cell lines.(1-((5-Chloro-2,3-dihydrobenzo[b]oxepin-4-yl)methyl)-1H-1,2,3-triazol-4-yl)methyl-2-(6-methoxynaphthalen-2-yl) propanoate (3j). Off white solid. M.P.: 78-80°C. R f : 0.4 (4:1 petroleum ether: ethyl acetate). IR (KBr) ν max /cm

1,2,3-Triazole-Containing Compounds as Anti–Lung Cancer Agents: Current Developments, Mechanisms of Action, and Structure–Activity Relationship

“…Thus, this compound is worthy of further investigation. Some 1,2,3triazole-containing 2-chloroquinoline derivatives, such as compound 29 (IC 50 : 9.8 μm against A549 cells, MTT assay; 9.7 μm for doxorubicin), also display certain antiproliferative activity against lung cancer cells, but most of them are less potent than the references (Praveena et al, 2016;Dasari et al, 2019). Further modifications implies that incorporation of azole between 1,2,3-triazole and quinoline moieties is also allowed, and 1,2,3-triazole-tethered 1,3,4-oxadiazole-quinoline compound 30 (IC 50 : 5.6 μm, MTT assay) is comparable to doxorubicin (IC 50 : 1.83 μm) against A549 cells (Rachakonda et al, 2017;Shamsi et al, 2019).…”

Exploring bi-carbazole-linked triazoles as inhibitors of prolyl endo peptidase via integrated in vitro and in silico study

“…Some of these activities are mentioned for instance, its therapeutic role in human breast cancer and in HIV produced disorders regarding to immune system as well possess anti-bacterial properties 26 . Also reported for anti-tyrosinase 26 , anti-amoebic 27 , anti-inflammatory 28 , anti-plasmodial 29 and anti-tumor activities 30 and these compounds are also reported for their anti-oxidant activity 31 . Moreover, there are noteworthy uses for the Triazole Forming Click Chemistry in almost all developing domains.…”

Nitric Oxide Induction in Peritoneal Macrophages by a 1,2,3-Triazole Derivative Improves Its Efficacy upon Leishmania amazonensis In Vitro Infection

“…6 1,2,3-Triazoles are an important medicinal scaffold with several biological properties reported, such as antibacterial, 7 anticonvulsant, 8 antiviral, 9 anticancer, 10 and anti-inflammatory activities. 11 In addition, its potential antiprotozoal activity has also been reported against the species of Trypanosoma and Leishmania. 12−14 Leishmaniases are a group of diseases caused by Leishmania spp.…”

“…Besides, the structural characteristics of 1,2,3-triazoles, such as polarity, rigidity, and the ability to act as electron donors and acceptors, allow the mimicking of different functional groups, which enhances the versatility of this class of compounds for the development of new drugs . 1,2,3-Triazoles are an important medicinal scaffold with several biological properties reported, such as antibacterial, anticonvulsant, antiviral, anticancer, and anti-inflammatory activities . In addition, its potential antiprotozoal activity has also been reported against the species of Trypanosoma and Leishmania. − …”