2. Academic Validation
  3. Regioselective synthesis and evaluation of 2-amino 3-cyano chromene-chrysin hybrids as potential anticancer agents

Regioselective synthesis and evaluation of 2-amino 3-cyano chromene-chrysin hybrids as potential anticancer agents

  • Bioorg Med Chem Lett. 2020 May 1;30(9):127087. doi: 10.1016/j.bmcl.2020.127087.
Hui-Juan Wang 1,  Yan-You Zhou 1,  Xiong-Li Liu 2,  Wen-Hui Zhang 3,  Shuang Chen 1,  Xiong-Wei Liu 3,  Ying Zhou 4
Affiliations

Affiliations

  • 1 Guizhou Medicine Edible Plant Resources Research and Development Center, Guizhou University, Guiyang 550025, China.
  • 2 Guizhou Medicine Edible Plant Resources Research and Development Center, Guizhou University, Guiyang 550025, China. Electronic address: xlliu1@gzu.edu.cn.
  • 3 College of Pharmaceutical Sciences, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, China.
  • 4 College of Pharmaceutical Sciences, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, China. Electronic address: zhouying067@gzy.edu.cn.
PMID: 32160978 DOI: 10.1016/j.bmcl.2020.127087
Abstract

The first example of CA(OH)2-activated p-regioselective synthesis of chrysin-fused chromene was reported through a cascade Michael/cyclization of chrysin and arylidenemalononitrile. The newly synthesized structurally diverse 2-amino 3-cyano chromene-chrysin hybrids 3 were evaluated for their in vitro Anticancer activity, and some of the compounds showed stronger anti-proliferative activity against K562, PC-3, A549 and NCI-H1299 than parent compound chrysin, and demonstrated equipotent potency compared with the reference drug of cisplatin. In particular, compound 3h had the highest cytotoxicity towards K562 cells (IC50 = 6.41 µM). Furthermore, compound 3h induced Apoptosis of K562 cells in a concentration-dependent manner, as well as induced the Apoptosis possibly through promoting the formation of apoptotic DNA of Cancer cell via the intrinsic apoptotic pathway. Thus, our results provide in vitro evidence that compound 3h may be a potential candidate for the development of new anti-tumour drugs.

Keywords

2-Amino 3-cyano chromene; Anticancer agents; Chrysin; Hybrids; Regioselective.

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