8-Azapurines as new inhibitors of cyclin-dependent kinases

Havlı́cěk, Libor; Fuksová, Květoslava; Kryštof, Vladimír; Orság, M; Vojtěšek, Bořivoj; Strnad, Miroslav

doi:10.1016/j.bmc.2005.06.007

Cited by 49 publications

(39 citation statements)

References 29 publications

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“…After cooling, methanol (~10 mL) was added. The reaction mixture was allowed to stand overnight and then filtered to give the solid (Scheme 1) affords the N-cyclohexyl-4,7-dihydro-5-isopropyl-7-phenyl- [1,2,4]triazolo[1,5-a]pyrimidine-6-carboxamide derivatives (5a-o) was obtained in excellent yield. …”

Section: Resultsmentioning

confidence: 99%

“…Recently, 1,2,4-triazolo [1,5-a]pyrimidines have aroused increasing attention from the chemical and biological view points, due to their diverse pharmacological activities, such as antitumor potency [1,2] inhibition of KDR kinase [3], antifungal effect [4] and macrophage activation [5]. They have proved to be promising anticancer agents with dual mechanisms of tubulin polymerization promotion [1,2] as well as cyclin dependent kinases [2] inhibition [6].…”

Section: Introductionmentioning

confidence: 99%

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One Pot Multi Component Synthetic Approach towards the Formation of 1,2,4-Triazolo[1,5 a]Pyrimidine Analogues and their Biological Evaluation

Khunt

Pipaliya

Ghelani

et al. 2014

ILCPA

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

One Pot Multi Component Synthetic Approach towards the Formation of 1,2,4-Triazolo[1,5 a]Pyrimidine Analogues and their Biological Evaluation

Khunt

Pipaliya

Ghelani

et al. 2014

ILCPA

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“…Among these isomeric families of compounds, 1, 2, 4-triazolo [1, 5-a]pyrimidine derivatives are thermodynamically more stable and thus, the most studied ones 1 , a few of them being commercially available. Revisions surveying the synthesis, reactivity, spectroscopic characterization and crystallographic studies of 1,2,4-triazolo [1,5- 5,6 , inhibition of KDR kinase 7 , antifungal effect 8 and macrophage activation 9 . They have proved to be promising anticancer agents with dual mechanisms of tubulin polymerization promotion as well as cycling dependent kinases 2 inhibition 10 .…”

Section: Introductionmentioning

confidence: 99%

Microwave Assisted Synthesis and Biological Evaluation of 1, 2, 4-Triazolo[1, 5-a]pyrimidines

2017

Chem Sci Trans

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Abstract:A microwave assisted synthesis of three new series of of 1, 2, 4-triazolo[1, 5-a]pyrimidines (PK-101 to PK-110) has been synthesized by the mixture of 5-(methylthio)-2H-1,2,4-triazol-3-amine (0.01 mol), 4,4,4-trifluoro-1-(4-methoxyphenyl)butane-1,3-dione (0.01 mol) and an appropriate aromatic aldehyde (0.01 mol) in ethanol (5 mL) was irradiated under microwave conditions at 120 °C for 10-15 min. The structures of all the newly synthesized compounds are elucidated by FT-IR, mass spectra, 1 H NMR and elemental analysis. The newly synthesized compounds are subjected to various biological activities viz., antimicrobial, antimycobacterial, anticancer and antiviral.

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“…Recently, 1,2,4-triazolo [1,5-a]pyrimidines have aroused increasing attention from the chemical and biological view points, due to their diverse pharmacological activities, such as antitumor potency [19,20], inhibition of KDR kinase [21], antifungal effect [22] and macrophage activation [23]. They have proved to be promising anticancer agents with dual mechanisms of tubulin polymerization promotion [19,20] as well as anti-mycobacterial agents [24].…”

Section: Introductionmentioning

confidence: 99%