2. Academic Validation
  3. Sulfamic and succinic acid derivatives of 25-OH-PPD and their activities to MCF-7, A-549, HCT-116, and BGC-823 cell lines

Sulfamic and succinic acid derivatives of 25-OH-PPD and their activities to MCF-7, A-549, HCT-116, and BGC-823 cell lines

  • Bioorg Med Chem Lett. 2017 Feb 15;27(4):1076-1080. doi: 10.1016/j.bmcl.2016.12.048.
Wu-Xi Zhou 1,  Jia-Qing Cao 1,  Xu-De Wang 1,  Jun-Hui Guo 1,  Yu-Qing Zhao 2
Affiliations

Affiliations

  • 1 Department of Traditional Chinese Medicine Chemical, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • 2 Department of Traditional Chinese Medicine Chemical, Shenyang Pharmaceutical University, Shenyang 110016, PR China; Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: zyq4885@126.com.
PMID: 28073676 DOI: 10.1016/j.bmcl.2016.12.048
Abstract

In the search for new anti-tumor agents with higher potency than our previously identified compound 1 (25-OH-PPD, 25-hydroxyprotopanaxadiol), 12 novel sulfamic and succinic acid derivatives that could improve water solubility and contribute to good drug potency and pharmacokinetic profiles were designed and synthesized. Their in vitro anti-tumor activities in MCF-7, A-549, HCT-116, and BGC-823 cell lines and one normal cell line were tested by standard MTT assay. Results showed that compared with compound 1, compounds 2, 3, and 7 exhibited higher cytotoxic activity on A-549 and BGC-823 cell lines, together with lower toxicity in the normal cell. In particular, compound 2 exhibited the best anti-tumor activity in the in vitro assays, which may provide valuable data for the research and development of new anti-tumor agents.

Keywords

25-OH-PPD; Antitumor activities; MTT; Sulfamic and succinic acid derivatives.

Figures