title: Sulfamic and succinic acid derivatives of 25-OH-PPD and their activities to MCF-7, A-549, HCT-116, and BGC-823 cell lines.
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.
authors.affiliation: Department of Traditional Chinese Medicine Chemical, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Wu-Xi
authors.initials: WX
authors.lastname: Zhou
authors.affiliation: Department of Traditional Chinese Medicine Chemical, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Jia-Qing
authors.initials: JQ
authors.lastname: Cao
authors.affiliation: Department of Traditional Chinese Medicine Chemical, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Xu-De
authors.initials: XD
authors.lastname: Wang
authors.affiliation: Department of Traditional Chinese Medicine Chemical, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Jun-Hui
authors.initials: JH
authors.lastname: Guo
authors.affiliation: 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.
authors.forename: Yu-Qing
authors.initials: YQ
authors.lastname: Zhao
mesh_terms: D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D036145:Ginsenosides / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D013329:Structure-Activity Relationship; D019802:Succinic Acid / Q000737:chemistry*; D013451:Sulfonic Acids / Q000737:chemistry*
chemical_list: C529607:25-hydroxyprotopanaxadiol; D036145:Ginsenosides; D013451:Sulfonic Acids; C005741:sulfamic acid; D019802:Succinic Acid
keywords: 25-OH-PPD; Antitumor activities; MTT; Sulfamic and succinic acid derivatives