2. Academic Validation
  3. Discovery of pyrazolone spirocyclohexadienone derivatives with potent antitumor activity

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

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: wushanchao07_2@126.com.
  • 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: shengcq@smmu.edu.cn.
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.

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