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: hwan@krict.re.kr.
4 College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon, Republic of Korea. Electronic address: ikyonkim@yonsei.ac.kr.

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.

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