Current time in Korea 23:50 Jun 13 (Sun) Year 2021 KCS KCS Publications
KCS Publications
My Journal  Log In  Register
HOME > Search > Browsing(BKCS) > Archives

Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 35, Number 5
BKCSDE 35(5)
May 20, 2014 

Synthesis of Hydroxylactams and Esters Derived from Thalidomide and Their Antitumor Activities
Guanglong Sun, Xiangchao Liu, Heng Zhou, Zenglu Liu, Zhenmin Mao*
Thalidomide derivatives, Hydroxylactams, Synthesis, Antitumor activity
A novel and convenient route for the synthesis of a series of thalidomide derivatives is described. Compound 2 was cyclized with different amines under alkaline condition to obtain 4-nitro substituted phthalimidines 3a-d. Hydroxylactams 4a-d were produced via bromination and hydroxylation. Different acyl chlorides were reacted with hydroxylactams to provide the desired esters 5a-d. All compounds were evaluated by MTT assay for their inhibitory activities against HCT-116, MG-63, MCF-7, HUVEC and HMVEC cell lines in vitro. Most of them showed no obvious cytotoxic effect on normal human cells, compounds 4a-d, 5a2, 5a4, 5a5, 5b2, 5c2 and 5d2 exhibited potent antitumor activities, among which compounds 5a2 and 5b2 were more effective than 5-FU.
1337 - 1342
Full Text
PDF / Supporting Information