Synthesis and bioactivity evaluation of 3-amino-6, 11-dioxo-6, 11-dihydro-5H-benzo[b]carbazole-1-carboxylic acid derivatives

Palanichamy Santhosh Kumar, Asir Obadiah, Arulappan Durairaj, Subramanian Ramanathan, Samuel Vasanthkumar

Research output: Contribution to journalArticlepeer-review

Abstract

A series of 3-amino-5-(1,4-dioxo-1,4-dihydronaphthalen-2-ylamino)benzoic acid derivatives were synthesized by the Michael addition of 1,4-naphthoquinone and 3,5-diaminobenzoic acid followed by the Suzuki coupling reaction. The derivatives of compound 2 were integrated, exposing it to benzolyation by an assortment of acid chlorides. Among the synthesized compounds, compounds 3b, 3c and 3d displayed better IC50 value of cytotoxicity (against HeLa) when compared with other derivatives. All the IC50 esteems were compared with the standard drug doxorubicin. DPPH and ABTS evaluation procedures are employed to assess the antioxidant activity. The compound 3d exhibited the highest inhibition of 75% and 77% in the DPPH and ABTS antioxidant activity evaluation, respectively. Graphic abstract: [Figure not available: see fulltext.]

Original languageEnglish
Pages (from-to)1039-1048
Number of pages10
JournalJournal of the Iranian Chemical Society
Volume19
Issue number4
DOIs
StatePublished - Apr 2022
Externally publishedYes

Bibliographical note

Publisher Copyright:
© 2021, Iranian Chemical Society.

Keywords

  • 1,4-Naphthoquinone
  • Antioxidant activity
  • Cytotoxicity
  • HeLa cell lines
  • Palladium catalyst
  • Suzuki coupling

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