Synthesis of heteroannulated cyclopent[b]indoles: Exploration of in vitro cytotoxicity and molecular docking studies

Rajendran Satheeshkumar, Aathi Muthusankar, Lincy Edatt, V. B. Sameer Kumar, Hazel A. Sparkes, Karnam Jayarampillai Rajendra Prasad*

*Corresponding author for this work

Research output: Contribution to journalArticle (Academic Journal)peer-review

3 Citations (Scopus)
232 Downloads (Pure)

Abstract

A series of novel cyclopent[b]indole analogues that hold isoxazolo-, pyrido-templates were designed and synthesized in good yields. The in vitro cytotoxicity was concerned for all the newly synthesized compounds by MTT assay against HeLa (cervix adeno carcinoma) and MCF-7 (breast cancer). These synthesized compounds were further compared with the standard drug ellipticine, 5-fluorouracil, cisplatin, and methotrexate. The synthesized heteroannulated cyclopent[b]indole compounds were found to show better cytotoxic activity against HeLa and MCF-7 with primary structure activity relationship studies. To identify with the nature of interactions of these molecules, we performed molecular docking studies using the protein kinase CK2 inhibitors. The docking results afforded some valuable information for the future design of more potent inhibitors.

Original languageEnglish
Pages (from-to)447-461
Number of pages15
JournalSynthetic Communications
Volume48
Issue number4
Early online date24 Jan 2018
DOIs
Publication statusPublished - 16 Feb 2018

Keywords

  • CK2 inhibitors
  • HeLa and MCF-7
  • isoxazolo-cyclopent[b]indole
  • pyrido-cyclopent[b]indole

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