We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Synthesis of Hydroxylactams and Esters Derived from Thalidomide and Their Antitumor Activities.
- Authors
Guanglong Sun; Xiangchao Liu; Heng Zhou; Zenglu Liu; Zhenmin Mao
- Abstract
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.
- Subjects
THALIDOMIDE; AMINES; BROMINATION; HYDROXYLATION; ACYL chlorides; ESTERS
- Publication
Bulletin of the Korean Chemical Society, 2014, Vol 35, Issue 5, p1337
- ISSN
0253-2964
- Publication type
Article
- DOI
10.5012/bkcs.2014.35.5.1337