1-benzoyl-6-hydroxy-2,2,4-trimethyl-1,2-dihydroquinoline exerts a neuroprotective effect and normalises redox homeostasis in a rat model of cerebral ischemia/reperfusion

Крыльский, Е. Д.; Chupandina, E.E.; Popova, T. N.; Шихалиев, Х. С.; Медведева, С. М.; Веревкин, А.Н.; Попов, С. С.; Миттова, В. О.

doi:10.1007/s11011-022-00928-3

Cited by 3 publications

(1 citation statement)

References 53 publications

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“…Therefore, the design of hybrid or chimeric compounds in the structure of which the dithiol ring is combined with another heterocyclic fragment (for example, azaheterocycle) with a certain pharmacological activity is of current interest. Among azaheterocycles, 2,2-disubstituted-1,2-dihydroquinolines functionalized at the benzene ring and/or the nitrogen atom (DHQ), which have a wide spectrum of biological activity-anticoagulant, antimalarial, antiparasitic, antibacterial, antidiabetic, anti-inflammatory, neuroprotective, and hepatoprotective activity-are of particular interest [27][28][29][30][31][32][33].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 4,5-Dihydro-1H-[1,2]dithiolo[3,4-c]quinoline-1-thione Derivatives and Their Application as Protein Kinase Inhibitors

Медведева

Shikhaliev

2022

Molecules

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This study represents the design and synthesis of a new set of hybrid and chimeric derivatives of 4,5-dihydro-4,4-dimethyl-1H-[1,2]dithiolo[3,4-c]quinoline-1-thiones, the structure of which the tricyclic fragment linearly bound or/and condensed with another heterocyclic fragment. Using the PASS Online software, among the previously synthesized and new derivatives of 1,2-dithiolo[3,4-c]quinoline-1-thione we identified 12 substances with pleiotropic activity, including chemoprotective and antitumor activity. All the synthesized derivatives were screened for their inhibitory assessment against a number of kinases. Compounds which exhibited prominent inhibition percentage in cells (>85%) were also examined for their inhibitory efficiency on human kinases via ELISA utilizing sorafenib as a reference standard to estimate their IC50 values. It was revealed that compounds 2a, 2b, 2c, and 2q displayed a significant inhibition JAK3 (IC50 = 0.36 μM, 0.38 μM, 0.41 μM, and 0.46 μM, respectively); moreover, compounds 2a and 2b displayed excellent activities against NPM1-ALK (IC50 = 0.54 μM, 0.25 μM, respectively), against cRAF[Y340D][Y341D], compound 2c showed excellent activity, and compound 2q showed weak activity (IC50 = 0.78 μM, 5.34 μM, respectively) (sorafenib IC50 = 0.78 μM, 0.43 μM, 1.95 μM, respectively). Thus, new promising preferred structures for the creation of drugs for the treatment of cancer and other multifactorial diseases in the future have been found.

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