Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.

Clicks: 488
ID: 100193
2018
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Abstract
New series of 5-(morpholinosulfonyl) isatin derivatives were designed and synthesized. The new compounds were characterized on the basis of spectral and elemental analyses. They were examined for their cytotoxic effects using SRB assay on four cancer cell lines HepG2, HCT116, CACO and MCF-7 in addition to the non-cancerous human cell line. They were non cytotoxic towards the normal derived cell line (IC value > 130 μM). Compounds 3, 6, 10 and 11 showed IC values less than 10 μM on three of the tested cell lines HepG2, HCT116 and CACO. Compounds 2h, 5, and 7b showed IC values less than or nearly equal 10 μM on HepG2, CACO and HCT116 respectively. Compounds 3 and 6 revelaed IC values less than 12 μM on MCF7. These obtained IC values are comparable with that of doxrubicin as it has showed IC range from 4.5 to 8.28 μM on the tested cell lines. All these promising derivatives showed inhibitory activity against EGFR with IC values less than 2 μM. The most potent EGFR inhibitors 7b (IC = 46 nM) and 10 (IC = 23 nM) showed to cause cell cycle arrest at G2/M phase and induce apoptosis. Molecular docking studies also were simulated to put insight and make better understanding to their structural features.
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ammar2018designeuropean Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Ammar, Yousry A;Sh El-Sharief, Ahmed M;Belal, Amany;Abbas, Samir Y;Mohamed, Yehia A;Mehany, Ahmed B M;Ragab, Ahmed;
Journal European journal of medicinal chemistry
Year 2018
DOI
S0223-5234(18)30552-X
URL
Keywords
Anti-cancer activity Cytotoxicity isatin sulfonamides egfr tyrosine kinase schiff's bases hydrazones morpholin

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