Synthesis of selenophene derivatives as novel CHK1 inhibitors.
A series of selenophene derivatives 3 were synthesized as potential CHK1 inhibitors. The effects of substitution on the 4'- or 5'-position of selenophene moiety and shifting the hydroxyl group position on C6- phenolic ring of oxindole were explored. This study led to the discovery of the most potent CHK1 inhibitors 29-33 and 39-43, which had IC(50) values in the subnanomolar range.
Hong
Pao-Chiung
PC
Development Center for Biotechnology, Xizhi City, Taipei County, Taiwan. pchong@mail.dcb.org.tw
Chen
Li-Jung
LJ
Lai
Tzu-Yun
TY
Yang
Huei-Yu
HY
Chiang
Shih-Jan
SJ
Lu
Yann-Yu
YY
Tsai
Ping-Kuei
PK
Hsu
Hung-Yi
HY
Wei
Win-Yin
WY
Liao
Chu-Bin
CB
D000071877:Checkpoint Kinase 1; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011494:Protein Kinases / Q000187:drug effects*; D018036:Selenium Compounds / Q000138:chemical synthesis* / Q000494:pharmacology
D047428:Protein Kinase Inhibitors; D018036:Selenium Compounds; D011494:Protein Kinases; D000071877:Checkpoint Kinase 1