title: Synthesis, SAR, and antitumor properties of diamino-C,N-diarylpyrimidine positional isomers: inhibitors of lysophosphatidic acid acyltransferase-beta.
abstract: 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.
authors.affiliation: Cell Therapeutics, Inc, 201 Elliott Ave W, Suite 400, Seattle, WA 98119, USA.
authors.forename: Baoqing
authors.initials: B
authors.lastname: Gong
authors.forename: Feng
authors.initials: F
authors.lastname: Hong
authors.forename: Cory
authors.initials: C
authors.lastname: Kohm
authors.forename: Scott
authors.initials: S
authors.lastname: Jenkins
authors.forename: John
authors.initials: J
authors.lastname: Tulinsky
authors.forename: Rama
authors.initials: R
authors.lastname: Bhatt
authors.forename: Peter
authors.initials: P
authors.lastname: De Vries
authors.forename: Jack W
authors.initials: JW
authors.lastname: Singer
authors.forename: Peter
authors.initials: P
authors.lastname: Klein
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011743:Pyrimidines; D000217:Acyltransferases; C018764:2-acylglycerophosphate acyltransferase; C030986:pyrimidine