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

Bioorg Med Chem Lett. 2021 Jun 1:41:127982. doi: 10.1016/j.bmcl.2021.127982.

Baljit Kaur ¹, Sahil Mishra ¹, Ramandeep Kaur ², Shikha Kalotra ², Palwinder Singh ³

Affiliations

1 Department of Chemistry, Centre for Advanced Studies, Guru Nanak Dev University, Amritsar 143005, India.
2 Department of Biotechnology, Guru Nanak Dev University, Amritsar 143005, India.
3 Department of Chemistry, Centre for Advanced Studies, Guru Nanak Dev University, Amritsar 143005, India. Electronic address: palwinder.chem@gndu.ac.in.

PMID: 33766762 DOI: 10.1016/j.bmcl.2021.127982

Abstract

Design and synthesis of new indole derivatives as tumor growth inhibiting agents via inhibiting the TNF-α is described. The preliminary results showed the inhibition of LPS induced production of NO, TNF-α 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.

Keywords

Cytotoxicity; Indole; Molecular modeling; Morpholinone hybrids; Tumor necrosis factor-α.

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