Synthesis and biological evaluation of new bisindole-imidazopyridine hybrids as apoptosis inducers

Satish Sunkari, Srinivasa Reddy Bonam, A. V.Subba Rao, Sd Riyaz, V. Lakshma Nayak, Halmuthur Mahabalarao Sampath Kumar, Ahmed Kamal, Bathini Nagendra Babu

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

Abstract

A series of diindolylmethanes (5a-t) were designed, synthesized, and examined for their cytotoxicity against four human cancer cell lines like prostate (DU-145), lung (A549), breast (MCF-7) and cervical cancer (HeLa). These results revealed that among all the hybrids, two (5k and 5r) were identified and exhibited significant cytotoxic effect against A549 cancer cells with IC 50 values of 1.65 ± 0.3 and 1.80 ± 0.8 µM respectively. To investigate the reasons for the cytotoxic activity, the conventional biological assays were carried out with 5k and 5r on the A549 cancer cells. Both hybrids led to the arrest of A549 cell lines at the G2/M phase of the cell cycle and strongly induced apoptosis. Further the apoptotic effects of 5k and 5r were confirmed by ROS, annexin-V FITC, and mitochondrial membrane potential. Moreover, structure–activity relationships were elucidated with various substitutions on these hybrids.

Original languageEnglish (US)
Pages (from-to)484-494
Number of pages11
JournalBioorganic Chemistry
Volume87
DOIs
StatePublished - Jun 2019
Externally publishedYes

Keywords

  • Apoptosis
  • Bisindole-imidazopyridine
  • Cytotoxicity
  • Heterocyclic
  • ROS

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Drug Discovery
  • Organic Chemistry

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