A synthetic 2,3-diarylindole induces cell death via apoptosis and autophagy in A549 lung cancer cells

Thanya Rukkijakan; Lukana Ngiwsara; Kriengsak Lirdprapamongkol; Jisnuson Svasti; Nared Phetrak; Pitak Chuawong

doi:10.1016/j.bmcl.2016.03.079

A synthetic 2,3-diarylindole induces cell death via apoptosis and autophagy in A549 lung cancer cells

Bioorg Med Chem Lett. 2016 May 1;26(9):2119-23. doi: 10.1016/j.bmcl.2016.03.079. Epub 2016 Mar 23.

Authors

Thanya Rukkijakan¹, Lukana Ngiwsara², Kriengsak Lirdprapamongkol³, Jisnuson Svasti³, Nared Phetrak¹, Pitak Chuawong⁴

Affiliations

¹ Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, and Special Research Unit for Advanced Magnetic Resonance (AMR), Kasetsart University, Bangkok 10900, Thailand.
² Laboratory of Biochemistry, Chulabhorn Research Institute, Bangkok 10210, Thailand. Electronic address: [email protected].
³ Laboratory of Biochemistry, Chulabhorn Research Institute, Bangkok 10210, Thailand.
⁴ Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, and Special Research Unit for Advanced Magnetic Resonance (AMR), Kasetsart University, Bangkok 10900, Thailand. Electronic address: [email protected].

PMID: 27032333
DOI: 10.1016/j.bmcl.2016.03.079

Abstract

A series of 2,3-diarylindoles were synthesized via the Larock heteroannulation, and evaluated for their anticancer activity against A549 lung cancer cells. The most potent compound, PCNT13 with IC50=5.17 μM, caused the induction of two modes of programmed cell death, apoptosis and autophagy.

Keywords: 2,3-Diarylindole; Apoptosis; Autophagy; Lung cancer.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

A549 Cells
Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / pharmacology*
Apoptosis / drug effects*
Autophagy / drug effects*
Drug Screening Assays, Antitumor
Humans
Indoles / chemical synthesis
Indoles / pharmacology*
Macrolides / pharmacology
Structure-Activity Relationship

Substances

Antineoplastic Agents
Indoles
Macrolides
PCNT13
bafilomycin A1