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

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.

• Authors: Haipin Zhou, Yonggan Dong, Xiaoqian Ma, Jinyi Xu, Shengtao Xu
• Journal: Fitoterapia (Fitoterapia) Vol. 146 Pg. 104670 (Oct 2020) ISSN: 1873-6971 [Electronic] Netherlands
• PMID: 32540381 (Publication Type: Journal Article)
• Copyright: Copyright © 2020 Elsevier B.V. All rights reserved.

Chemical References

• Antineoplastic Agents
• Nitric Oxide Donors
• Rotenone
• deguelin

Topics

• Antineoplastic Agents (chemistry, pharmacology)
• Cell Cycle Checkpoints (drug effects)
• Cell Line, Tumor
• Drug Screening Assays, Antitumor
• Humans
• Lung Neoplasms (drug therapy)
• Molecular Structure
• Nitric Oxide Donors (chemistry, pharmacology)
• Rotenone (analogs & derivatives, chemistry, pharmacology)