D-ring modified novel isosteviol derivatives: design, synthesis and cytotoxic activity evaluation.
A series of polyhydric, amino alcohol and tricyclic derivatives were facilely synthesized by D-ring modification of isosteviol. These compounds were screened for their cytotoxic activities against four human tumor cell lines in vitro. Among them, the 15-α-aminomethyl-16-β-hydroxyl isosteviol 23 exhibits significant cytotoxicity superior to the positive control (cisplatin) against EC9706, PC-3 and HCT-116 cell lines.
College of Chemistry and Molecular Engineering, New Drug Research & Development Center, Zhengzhou University, 75 Daxue Road, Zhengzhou 450052, PR China.
Tao
T
Zhang
Li-Hui
LH
Lu
Hao
H
Liu
Jun-Wei
JW
Wang
Rui-Xue
RX
Wang
Yun-Xiao
YX
Zhang
Jing-Chao
JC
Tao
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D045786:Diterpenes, Kaurane / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D006801:Humans; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D045786:Diterpenes, Kaurane; C515747:isosteviol