Synthesis and Cytotoxicity Activity of Novel Benzotrizolyl Methyl[1,2,4-triazolo][3,4-b]thiadiazinyl Substituted Chromene 2-ones

Yakaiah, S.; Durgaprasad, K.; Rao, A.K.S. Bhujanga; Rani, Preeti; Awantika, S.; Buchappa, G.; Aparna, P.

doi:10.14233/ajchem.2016.19714

Cited by 2 publications

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“…Yakaiah et al [ 72 ] carried out synthesis of 1,2,4-triazolo[3,4- b ][1,3,4]thiadiazines ( 101 ) containing coumarin and benzotriazole moieties and evaluated their anticancer against a human lung cancer (HCC 827) cell line. Bioassay results indicated that compound 101k exhibited promising activity, with an IC 50 value of 0.821 µM.…”

Section: Pharmacological Properties Of 124-triazolo[34- B ][134]thiadiazinesmentioning

confidence: 99%

Vision on Synthetic and Medicinal Facets of 1,2,4-Triazolo[3,4-b][1,3,4]thiadiazine Scaffold

et al. 2022

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The present review article strives to compile the latest synthetic approaches for the synthesis of triazolothiadiazine and its derivatives, along with their diverse pharmacological activities, viz. anticancer, antimicrobial, analgesic and anti-inflammatory, antioxidant, antiviral, enzyme inhibitors (carbonic anhydrase inhibitors, cholinesterase inhibitors, alkaline phosphatase inhibitors, anti-lipase activity, and aromatase inhibitors) and antitubercular agents. The review focuses particularly on the structure–activity relationship of biologically important 1,2,4-triazolo[3,4- b ][1,3,4]thiadiazines, which have profound importance in drug design, discovery and development. In silico pharmacokinetic and molecular modeling studies have also been summarized. It is hoped that this review article will be of help to researchers engaged in the development of new biologically active entities for the rational design and development of new target-oriented 1,2,4-triazolo[3,4- b ][1,3,4]thiadiazine-based drugs for the treatment of multifunctional diseases. Graphical Abstract

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Section: Pharmacological Properties Of 124-triazolo[34- B ][134]thiadiazinesmentioning

confidence: 99%

Vision on Synthetic and Medicinal Facets of 1,2,4-Triazolo[3,4-b][1,3,4]thiadiazine Scaffold

et al. 2022

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“…Various hydrazone 34 , [1,2,4‐triazolo][3,4‐ b ]thiadiazinyl 35 , pyrazole 36 , alkyl and aryl 37 , pyridine 38 , chalcone 39 , 3‐oxo‐2,3‐dihydrofuran 40 , pyrrole , dithiocarbamate , benzimidazole , dialkynylcarbinol , steroidal , costunolide , colchicines , (−)‐Dibromophakellstatin fused coumarin–triazole hybrids and cyclized coumarin–triazole hybrids , the 1,2,4‐triazole‐5‐one hybrids 41 , as well as triazole tethered bis‐coumarin 42 (Fig. ) were screened for their anticancer activities, in spite of the majority of them showed weak to moderate activity against the tested cancer cell lines, the enriched SAR paved the way to the further rational design.…”

Section: Antitumor Activitymentioning

confidence: 99%

Coumarin–triazole Hybrids and Their Biological Activities

Fan

Xing

Liu

2018

Journal of Heterocyclic Chem

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Hybridization is emerged as a promising strategy in the discovery of new drugs, especially these with complimentary activities and multiple pharmacological targets that are the potential weapons to prevent the drug resistance. Currently, several hybrids are under different stages of clinical trial, and may be introduced into clinical practice to treat various diseases in the near future. Triazoles including 1,2,3‐triazole and 1,2,4‐triazole as well as coumarins occupy an important position in medicinal chemistry attribute to their various biological activities, and some of them have been used in clinical practice. Obviously, hybridization of these two pharmacophores may lead to novel candidates with broader spectrum, more effective, lower toxicity, and multiple mechanisms of action. This review aims to outline the biological activities of coumarin–triazole hybrids, and discuss their structure–activity relationship to pave the way for the further rational development of this kind of hybrids.

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Synthesis and Cytotoxicity Activity of Novel Benzotrizolyl Methyl[1,2,4-triazolo][3,4-b]thiadiazinyl Substituted Chromene 2-ones

Cited by 2 publications

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Vision on Synthetic and Medicinal Facets of 1,2,4-Triazolo[3,4-b][1,3,4]thiadiazine Scaffold

Vision on Synthetic and Medicinal Facets of 1,2,4-Triazolo[3,4-b][1,3,4]thiadiazine Scaffold

Coumarin–triazole Hybrids and Their Biological Activities

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