Current time in Korea 16:22 Aug 23 (Fri) Year 2019 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 33, Number 5
BKCSDE 33(5)
May 20, 2012 

Design and Synthesis of an Anticancer Diarylurea Derivative with Multiple-Kinase Inhibitory Effect
Mohammed I. El-Gamal, Chang-Hyun Oh*
Anticancer, Diarylurea, Multiple-kinase, Pyrrolo[3,2-c]pyridine
A diarylurea compound 1 possessing pyrrolo[3,2-c]pyridine nucleus was designed and synthesized with structure similarity to Sorafenib. Compound 1 was tested over 60-cancer cell line panel at a single dose concentration of 10 μM and showed high activity. It was further tested in a five-dose mode to determine its IC50, TGI, and LC50 values over the 60 cell lines. Compound 1 showed high potency and good efficacy, and was accordingly tested at a single dose concentration of 10 μM over a panel of 40 kinases. At this concentration, it completely inhibited the enzymatic activities of a number of oncogenic kinases, including ABL, ALK, c-RAF, FLT3, KDR, and TrkB. The target compound was subsequently tested over these 6 kinases in 10-dose testing mode in order to determine its IC50 values.
1571 - 1576
Full Text