title: Synthesis and antitumor activity of N-sulfonyl-3,7-dioxo-5β-cholan-24-amides, ursodeoxycholic acid derivatives.
abstract: A series of N-sulfonyl-3,7-dioxo-5β-cholan-24-amides, ursodeoxycholic acid derivatives, have been designed and synthesized in nine steps starting from ursodeoxycholic acid. The in vitro antitumor activity of the target compounds has been evaluated against HCT-116, MCF-7, K562, and SGC-7901 cell lines. The pharmacological results showed that most of the prepared compounds display excellent selective cytotoxicity toward HCT-116, MCF-7, and K562 cell lines. Particularly, compounds 10c, 10f and 10g show high inhibitory activity on these human cancer cell lines (IC50: 2.39-9.34 μM). Conversely, all compounds are generally inactive against SGC-7901, with only 10b having IC₅₀ below 50 μM.
authors.affiliation: School of Pharmaceutical Engineering & Life Science, Changzhou University, 1 Gehu Road, Changzhou, Jiangsu 213164, PR China.
authors.forename: Jie
authors.initials: J
authors.lastname: Ren
authors.forename: Yongchao
authors.initials: Y
authors.lastname: Wang
authors.forename: Junliang
authors.initials: J
authors.lastname: Wang
authors.forename: Jun
authors.initials: J
authors.lastname: Lin
authors.forename: Kun
authors.initials: K
authors.lastname: Wei
authors.forename: Rong
authors.initials: R
authors.lastname: Huang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D010084:Oxidation-Reduction; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology; D014580:Ursodeoxycholic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D013449:Sulfonamides; D014580:Ursodeoxycholic Acid