Search by property

Property "Has-20abstract" (as page type) with input value "New-20molecular-20hybrids-20were-20synthesized-20by-20combining-20tetrahydroquinoline-20(THQ)-20and-20isoxazole-20(ISX)-20scaffolds,-20in-20search-20for-20chemical-20structures-20with-20improved-20pharmacological-20properties.-20Our-20tetrahydroquinoline-20(THQ)-20and-20isoxazole-20(ISX)-20hybrids-20differ-20in-20the-20X-20and-20Y-20substituents:-20FM53-20(X = H-3B-20Y=-20H),-20FM49-20(X = CH-3Csub-3E3-3C-2Fsub-3E-3B-20Y=-20OCH-3Csub-3E3-3C-2Fsub-3E),-20FM50-20(X = Cl-3B-20Y=-20H)-20and-20FM48-20(X = Cl-3B-20Y=-20OCH-3Csub-3E3-3C-2Fsub-3E).-20Aiming-20at-20exploring-20their-20bioactivity-20in-20liver-20cancer-20cells,-20in-20this-20paper-20we-20report-20the-20effect-20of-20four-20THQ-2DISX-20hybrids-20on-20viability,-20respiration-20and-20oxidative-20stress-20in-20Hep-2DG2-20human-20hepatoma-20cells.-20In-20addition,-20we-20measured-20the-20alterations-20induced-20by-20these-20compounds-20on-20oxygen-20uptake-20and-20respiratory-20chain-20enzymes-20in-20isolated-20mitochondria.-20Cell-20viability-20assay-20indicated-20that-20these-20THQ-2DISX-20hybrids-20displayed-20antiproliferative-20activity-20on-20Hep-2DG2-20cells.-20Among-20these,-20FM50-20(IC-3Csub-3E50-3C-2Fsub-3E = 5.2 ± 1.9 μM)-20and-20FM53-20(IC-3Csub-3E50-3C-2Fsub-3E = 6.8 ± 0.7 μM)-20had-20the-20highest-20cytotoxicity.-20These-20four-20hybrids-20also-20inhibited-20the-20Hep-2DG2-20cells-20respiration-20in-20the-20uncoupled-20state,-20with-20FM50-20decreasing-20all-20respiratory-20states-20(basal,-20leak,-20uncoupled).-20While-20only-20FM49-20and-20FM53-20altered-20the-20Hep-2DG2-20cells-20redox-20function.-20In-20terms-20of-20mitochondrial-20bioenergetics,-20THQ-2DISX-20hybrids-20decreased-20the-20oxygen-20consumption-20in-20state-203-20(via-20complex-20I-20and-20II),-20and-20also-20inhibited-20NADH-20oxidase-20and-20NADH-20cytochrome-20c-20reductase-20enzyme-20activities.-20In-20these-20experiments,-20the-20structural-20homologues-20FM50-20and-20FM53-20had-20a-20remarkable-20inhibitory-20effect-20(∼50-25)-20with-20respect-20to-20FM49-20and-20FM48.-20These-20results-20show-20that-20THQ-2DISX-20hybrids-20are-20promising-20compounds-20for-20hepatoma-20cancer-20treatment-20and-20that-20the-20phenyl-20substituent-20(Y=-20H)-20in-20the-20ISX-20scaffold-20intensifies-20both,-20the-20cytotoxicity-20in-20Hep-2DG2-20cells-20and,-20inhibition-20of-20electron-20transport-20through-20complex-20I-20of-20the-20mitochondrial-20respiratory-20chain.-0A-0A-3Csmall-3ECopyright-20©-202019.-20Published-20by-20Elsevier-20B.V.-3C-2Fsmall-3E" contains invalid characters or is incomplete and therefore can cause unexpected results during a query or annotation process.

Showing below up to 0 results starting with #1.

View (previous 50 | next 50) (20 | 50 | 100 | 250 | 500)