4.5 Article

Rationally designed TNF-α inhibitors: Identification of promising cytotoxic agents

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 41, Issue -, Pages -

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2021.127982

Keywords

Indole; Morpholinone hybrids; Molecular modeling; Cytotoxicity; Tumor necrosis factor-?

Funding

  1. CSIR, New Delhi
  2. NCI Bethesda USA

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The study focused on designing and synthesizing new indole derivatives as potential agents for inhibiting tumor growth by targeting TNF-α. Results indicated that compounds 2d and 2g exhibited significant cytotoxicity against a panel of human cancer cell lines.
Design and synthesis of new indole derivatives as tumor growth inhibiting agents via inhibiting the TNF-? is described. The preliminary results showed the inhibition of LPS induced production of NO, TNF-? and IL-6 by these compounds out of which compounds 2d and 2g exhibited appreciable cytotoxicity against the 60 cell lines panel of human cancer. The rationale behind the design of the molecules and the results of their biological studies are presented. 2009 Elsevier Ltd. All rights reserved.

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