2. Academic Validation
  3. A novel, broad-spectrum antitumor compound containing the 1-hydroxycyclohexa-2,5-dien-4-one group: the disclosure of a new antitumor pharmacophore in protoapigenone 1

A novel, broad-spectrum antitumor compound containing the 1-hydroxycyclohexa-2,5-dien-4-one group: the disclosure of a new antitumor pharmacophore in protoapigenone 1

  • Bioorg Med Chem Lett. 2011 Jun 1;21(11):3427-30. doi: 10.1016/j.bmcl.2011.03.108.
Qianying Yuan 1,  Ziwei Liu,  Chaomei Xiong,  Liqian Wu,  Jianping Wang,  Jinlan Ruan
Affiliations

Affiliation

  • 1 Key Laboratory of Natural Medicinal Chemistry and Resources Evaluation of Hubei Province, College of Pharmacy, Tongji Medical Center of Huazhong University of Science and Technology, Wuhan 430030, China.
PMID: 21515048 DOI: 10.1016/j.bmcl.2011.03.108
Abstract

The synthesis of a new compound 9 containing the 4-hydroxy-2,5-cyclohexadien-1-one system, a key elements toward elucidation of the protoapigenone 1 antitumor pharmacophore, was described. The compound showed potent in vitro antitumor potency with low micromolar IC(50)'s against breast, ovarian, prostate, liver, pancreas, and blood Cancer cell lines tested and could inhibit tumor growth in vivo but no significant impairment of hematopoiesis or immune function was observed. The minimum structural pharmacophore of 1 has now been refined.

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