Development of a novel truncated deguelin derivative possessing nitric oxide donor as a potential anti-lung cancer agent.

Fitoterapia
Haipin ZhouShengtao Xu

Abstract

Lung cancer is the leading cause of cancer death in the world. Natural product deguelin and its truncated analogs have been reported to be potential therapeutic agents for lung cancer. In order to improve the potency, a novel truncated deguelin derivative (4) possessing nitric oxide (NO) donor was designed and synthesized. The biological evaluation showed that hybrid 4 exerted potent activity with an IC50 value of 0.41 μM in H1299 cells. Mechanism studies showed that it arrested the cell cycle at G2/M phase and suppressed Hsp90 function. In addition, hybrid 4 demonstrated potent inhibitory activity on the migration and invasion of lung cancer cells. Together, the promising results warrant further development of hybrid 4 as a potential anticancer agent for the treatment of lung cancer.

References

May 2, 2000·Current Pharmaceutical Design·J K Buolamwini
Jun 15, 2007·Journal of the National Cancer Institute·Seung Hyun OhHo-Young Lee
Jan 24, 2015·Nature Reviews. Drug Discovery·Alan L HarveyRonald J Quinn
Aug 15, 2015·Thoracic Cancer·Wanqing ChenSiwei Zhang
Dec 23, 2016·Expert Opinion on Drug Discovery·Hong YaoJinyi Xu
May 16, 2017·Journal of Medicinal Chemistry·Zhangjian HuangYihua Zhang
Jun 30, 2018·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Huan XiaXiaohong Lv
Dec 12, 2018·Nature Reviews. Cancer·Nasser K AltorkiVivek Mittal
Feb 21, 2019·European Journal of Medicinal Chemistry·Hong YaoShengtao Xu
Dec 31, 2019·Bioorganic & Medicinal Chemistry Letters·Xueyan HuangDahong Li

❮ Previous
Next ❯

Citations


❮ Previous
Next ❯

Related Concepts

Related Feeds

Cell Migration

Cell migration is involved in a variety of physiological and pathological processes such as embryonic development, cancer metastasis, blood vessel formation and remoulding, tissue regeneration, immune surveillance and inflammation. Here is the latest research.