Synthesis and evaluation of cytotoxic effects of novel α-methylenelactone tetracyclic diterpenoids.
A series of tetracyclic diterpenoids bearing the α-methylenelactone group have been synthesized and screened for their in vitro anti-tumor activities against six human cancer cell lines. The results showed that compounds 1c, 2a and 2b exhibited significant cytotoxicity superior to the positive control doxorubicin hydrochloride against MDA-MB-231, K562 and HepG2 cell lines. In particular, compound 2b was identified as the most promising anticancer agent against HepG2 cells with IC(50) value of 0.09μM.
Center of Drug Discovery, College of Pharmacy, China Pharmaceutical University, 24 Road Tongjia Xiang, Nanjing 210009, China.
Yao-Fu
YF
Zeng
Jia-Qiang
JQ
Wu
Lian-Yong
LY
Shi
Ke
K
Wang
Bin
B
Zhou
Yong
Y
Tang
Da-Yong
DY
Zhang
Yang-Chang
YC
Wu
Wei-Yi
WY
Hua
Xiao-Ming
XM
Wu
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004224:Diterpenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D009369:Neoplasms / Q000188:drug therapy; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D004224:Diterpenes; D007783:Lactones; C416683:methylene-lactone