Discovery of pyrazolone spirocyclohexadienone derivatives with potent antitumor activity

  • Bioorg Med Chem Lett. 2020 Jan 1;30(1):126662. doi: 10.1016/j.bmcl.2019.126662.
Lei Wang  1 ,  Zixuan Yang  2 ,  Tianyu Ni  2 ,  Wencai Shi  3 ,  Yunbo Guo  2 ,  Keliang Li  2 ,  Anzhe Shi  2 ,  Shanchao Wu  4 ,  Chunquan Sheng  5
Affiliations
  • 1. School of Pharmacy, Fujian University of Traditional Chinese Medicine, 1 Qiuyang Road, Fuzhou, Fujian 350122, People's Republic of China.
  • 2. Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China.
  • 3. Department of Clinical Nutrition, Changhai Hospital, Second Military Medical University, 168 Changhai Road, Shanghai 200433, People's Republic of China.
  • 4. Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China. Electronic address: [email protected].
  • 5. School of Pharmacy, Fujian University of Traditional Chinese Medicine, 1 Qiuyang Road, Fuzhou, Fujian 350122, People's Republic of China; Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China. Electronic address: [email protected].
PMID: 31784322 DOI: 10.1016/j.bmcl.2019.126662
Abstract

Starting from easy accessible pyrazoletetrahydropyran acetals, a series of new pyrazolone spirocyclohexadienone derivatives were synthesized and assayed for antitumor activity. Compound 10s was identified to possess good antitumor activity. It could induce MDA-MB-231 Cancer cell Apoptosis in a concentration dependent manner and arrest the cell cycle progression mainly at the G1 phase.

Keywords
Antitumor; Pyrazolone spirocyclohexadienone; Structure-activity relationship.