Sulphonamido-quinoxalines: Search for anticancer agent

• Sulphonamido-quinoxalines 3(a–p) prepared and evaluated for anticancer activity.
• Compounds were designed based upon (HTS) hit identified by Porter and collaborator.
• Compound 3l showed highest activity (Leukemia RPMI-8226 cell lines GI50: 1.11 μM).
• Docking studies proved c-Met kinase inhibition.
• Lipinski's rule and in silico ADME parameters are within the acceptable range.

A series of new sulphonamido-quinoxaline derivatives 3(a–p) have been prepared which are structurally similar to the High Throughput Screening (HTS) hit identified by Porter and collaborator. The newly synthesized compounds 3b, 3c, 3f, 3i, 3j, 3l, 3n and 3o were further evaluated in the National Cancer Institute for in vitro cytotoxicity assay among them compound 3l showed highest activity against Leukemia RPMI-8226 cell lines (GI50: 1.11 μM) as compared to other tested compounds. It is to be noted that compound 3l shows significant activity (GI50: 1.11 μM) compared to the High Throughput Screening (HTS) hit identified by Porter and collaborator (IC50 = 1.3 μM). Further docking study confirms the c-Met kinase inhibitory mechanism of the synthesized compounds.

A novel series of sulphonamido-quinoxalines were synthesized and evaluated in vitro for anticancer activity at NCI.Figure optionsDownload as PowerPoint slide