Synthesis, SAR, and antitumor properties of diamino-C,N-diarylpyrimidine positional isomers: inhibitors of lysophosphatidic acid acyltransferase-beta.
2,4-Diamino-N(4),6-diarylpyrimidines were identified as potent, isoform specific inhibitors of lysophosphatidic acid acyltransferase-beta (LPAAT-beta). Active inhibitors also blocked proliferation of tumor cell lines in vitro. The effect of 2j in an in vivo tumor model was investigated.
Gong
Baoqing
B
Cell Therapeutics, Inc, 201 Elliott Ave W, Suite 400, Seattle, WA 98119, USA.
Hong
Feng
F
Kohm
Cory
C
Jenkins
Scott
S
Tulinsky
John
J
Bhatt
Rama
R
De Vries
Peter
P
Singer
Jack W
JW
Klein
Peter
P
D000217:Acyltransferases / Q000037:antagonists & inhibitors*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007536:Isomerism; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011743:Pyrimidines; D000217:Acyltransferases; C018764:2-acylglycerophosphate acyltransferase; C030986:pyrimidine