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Journal J Enzyme Inhib Med Chem

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Rational design of biodegradable sulphonamide candidates treating septicaemia by synergistic dual inhibition of COX-2/PGE2 axis and DHPS enzyme.

Nada H El-Dershaby, Soad A El-Hawash, Shaymaa E Kassab, Hoda G Dabees, Ahmed E Abdel Moneim, Ibrahim A Abdel Wahab, Mohammad M Abd-Alhaseeb, Mostafa M M El-Miligy,

A new series of co-drugs was designed based on hybridising the dihydropteroate synthase (DHPS) inhibitor sulphonamide scaffold with the COX-2 inhibitor salicylamide pharmacophore through biodegradable linkage to achieve compounds with synergistic dual inhibition of COX-2/PGE2 axis and DHPS enzyme to enhance antibacterial activity for treatment of septicaemia. Compounds <b>5 b, 5j, ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2022, 37(1):1737-1751]

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Design, synthesis, and biological evaluation of a novel series of 2-(2,6-dioxopiperidin-3-yl)isoquinoline-1,3(2H,4H)-dione derivatives as cereblon modulators.

Yilin Liu, Yuming Song, Yingju Xu, Meixu Jiang, Haibin Lu,

In the current study, we designed and synthesised a novel series of 2-(2,6-dioxopiperidin-3-yl)isoquinoline-1,3(2<i>H</i>,4<i>H</i>)-dione derivatives as cereblon (CRBN) modulators. The results of the CCK8 assay revealed potent antiproliferative activity for the selected compound <b>10a</b> against NCI-H929 (IC<sub>50</sub>=2.25 µM) and U239 (IC<sub>50</sub>=5.86 µM) cell lines. Compound <b>10a</b> also can inhibit the TNF-α level (IC<sub>50</sub>=0.76 µM) ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2022, 37(1):1715-1723]

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