title: Identification of 5,6-substituted 4-aminothieno[2,3-d]pyrimidines as LIMK1 inhibitors.
abstract: 4-Aminobenzothieno[3,2-d]pyrimidines were previously identified in a high throughput screening campaign as LIMK1 inhibitors. Scaffold reversal led to the identification of a series of simple 5,6-substituted 4-aminothieno[2,3-d]pyrimidines with low micromolar inhibition of LIMK1.
authors.affiliation: The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia.
authors.forename: Brad E
authors.initials: BE
authors.lastname: Sleebs
authors.forename: George
authors.initials: G
authors.lastname: Nikolakopoulos
authors.forename: Ian P
authors.initials: IP
authors.lastname: Street
authors.forename: Hendrik
authors.initials: H
authors.lastname: Falk
authors.forename: Jonathan B
authors.initials: JB
authors.lastname: Baell
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004354:Drug Screening Assays, Antitumor; D057166:High-Throughput Screening Assays; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D020128:Inhibitory Concentration 50; D054461:Lim Kinases / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D058990:Molecular Targeted Therapy; D008970:Molecular Weight; D009362:Neoplasm Metastasis / Q000188:drug therapy; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D054461:Lim Kinases