الفهرس 
Synthesis and biological evaluation of substituted indole derivatives
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Abstract
The present investigation deals with the synthesis of 3-(1H-indol-2-yl)aniline I, N-[3-(3-formyl-1H-indol-2-yl) phenyl] acetamide VII and 1H-indole-3-carbaldehyde XIII as key intermediates for the preparation of novel indole based nucleus I-XVIII. A preliminary testing of all of the synthesized compounds for their in-vitro antitumor activity against MCF-7 cell line and twelve of them against A549 cell line in NCI, Egypt. A further investigation of the cytotoxic activity of 23 of the prepared compounds, selected according to the rules of NCI in Bethesda, USA, was performed on a panel of 60 tumor cell lines. Compound XVIIIb was the most active showing high growth inhibition percentages (31-82.5%) against 47 cell lines. Study of the binding pattern and binding affinities of all of the synthesized in the VEGFR-2 active site using sorafenib as a reference VEGFR-2 inhibitor. In addition, evaluation of the VEGFR-2 level inhibition percent in human breast cancer MCF-7 cell line was carried out on ten of the synthesized compounds being chosen according to docking study results. Compound XVIIIc showed a high percent reduction value of 85% as compared to sorafenib 84% and further evaluation of the VEGFR-2 inhibitory activity was performed on seven compounds using the VEGFR-2 kinase inhibitory kit assay. Compound XVIIIb showed an IC50 0.07æM which is better than that of sorafenib (IC50 = 0.09 æ)