Biological evaluation of indolizine-chalcone hybrids as new anticancer agents

  • Eur J Med Chem. 2018 Jan 20:144:435-443. doi: 10.1016/j.ejmech.2017.12.056.
Sujin Park  1 ,  Eun Hye Kim  2 ,  Jinwoo Kim  1 ,  Seong Hwan Kim  3 ,  Ikyon Kim  4
Affiliations
  • 1. College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon, Republic of Korea.
  • 2. Center for Drug Discovery Technology, Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.
  • 3. Center for Drug Discovery Technology, Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea. Electronic address: [email protected].
  • 4. College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon, Republic of Korea. Electronic address: [email protected].
PMID: 29288944 DOI: 10.1016/j.ejmech.2017.12.056
Abstract

A new chemical space was explored based on an indolizine-chalcone hybrid, which was readily accessible by base-mediated aldol condensation of indolizine bearing a 7-acetyl group with various (hetero)aromatic aldehydes. Their Anticancer effect was evaluated, revealing that indolizine-chalcone hybrids with 3,5-dimethoxyphenyl group (4h) or the halogen at the meta position (4j and 4l) could have the potential to induce the caspase-dependent Apoptosis of human lymphoma cells.

Keywords
Aldol condensation; Anticancer activity; Chalcone; Hybrid; Indolizine.