DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL INDOLE-THALIDOMIDE HYBRIDS ANALOGS

Document Type : Original Article

Authors

1 Faculty of Science, Department of Chemistry, Menoufia University, Shebin El-Koom, Egypt

2 Faculty of Science, Department of Zoology, Al-Azhar University, Cairo, Egypt

Abstract

Abstract
A series of novel Indole-Thalidomide hybrids were designed and synthesized in a good yield to improve and develop higher potency and selective anti-tumor agents. By two steps alkylation of Indole with Thalidomide then react the product with different active methylene groups.Their antiprolifer-ative evaluation activities against HCT 116 (colon cancer cell line), HepG2 (liver cancer cell line) and MCF-7 (breast cancer cell line). In vitro were tested by using Sulforhodamine-B stain (SRB) assay. The chemical structures of all synthesized analogs were elucidated on the basis of their spectral IR, 1H NMR, 13C NMR, Mass spectroscopy and element analysis. The result of the present work indicated all new analogs showed good activity toward all the tested cell lines, analog 8 has broad-spectrum anticancer activity toward all the tested cancer cell lines, followed by analog 2. The apop-tosis evaluation for new analogs on Caspase-3, Bcl2 and Bax shown the best activity for analogs 2 and 8, so that the two analogs were histopathologi-cally investigated.

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History

  • Receive Date: 08 February 2020
  • Revise Date: 10 March 2020
  • Accept Date: 11 March 2020

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