KCS Publications

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

Title	Synthesis of Hydroxylactams and Esters Derived from Thalidomide and Their Antitumor Activities
Author	Guanglong Sun, Xiangchao Liu, Heng Zhou, Zenglu Liu, Zhenmin Mao*
Keywords	Thalidomide derivatives, Hydroxylactams, Synthesis, Antitumor activity
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.
Page	1337 - 1342
Full Text	PDF / Supporting Information

How to access to the WOL for The Bulletin of the Korean Chemical Society ?

The Bulletin of the Korean Chemical Society will be co-published with Wiley-VCH from 2015 towards. The online version of the Journal will thus be available on Wiley Online Library, Wiley(-VCH)'s global online platform.

KCS members can get a free online access to the Bulletin of the Korean Chemical Society in WOL.

Free Access to WOL