| Title : Synthesis and structure-activity relationship of (1-halo-2-naphthyl) carbamate-based inhibitors of KIAA1363 (NCEH1\/AADACL1) - Shreder_2012_Bioorg.Med.Chem.Lett_22_5748 |
| Author(s) : Shreder KR , Lin EC , Wu J , Cajica J , Amantea CM , Hu Y , Okerberg E , Brown HE , Pham LM , Chung de M , Fraser AS , McGee E , Rosenblum JS , Kozarich JW |
| Ref : Bioorganic & Medicinal Chemistry Lett , 22 :5748 , 2012 |
| Abstract : KIAA1363 is a serine hydrolase whose activity has been shown to be positively associated with tumor cell invasiveness. Thus, inhibitors of KIAA1363 represent a novel targeted therapy approach towards cancer. AX11890 ((1-bromo-2-naphthyl) N,N-dimethylcarbamate) was identified as a KIAA1363 inhibitor with an IC(50) value of 1.2 muM and was shown using ESI-MS to carbamylate the catalytic residue Ser(191). SAR studies explored both substitution of the 1-bromo group and derivatization of the 6-position. Activity-based protein profiling demonstrated AX13057 inhibited tumor-localized KIAA1363 in SK-OV-3 xenograft-bearing mice. |
| ESTHER : Shreder_2012_Bioorg.Med.Chem.Lett_22_5748 |
| PubMedSearch : Shreder_2012_Bioorg.Med.Chem.Lett_22_5748 |
| PubMedID: 22877630 |
| Gene_locus related to this paper: human-NCEH1 |
| Gene_locus related to this paper: human-NCEH1 |
Shreder KR, Lin EC, Wu J, Cajica J, Amantea CM, Hu Y, Okerberg E, Brown HE, Pham LM, Chung de M, Fraser AS, McGee E, Rosenblum JS, Kozarich JW (2012)
Synthesis and structure-activity relationship of (1-halo-2-naphthyl) carbamate-based inhibitors of KIAA1363 (NCEH1\/AADACL1)
Bioorganic & Medicinal Chemistry Lett
22 :5748
Shreder KR, Lin EC, Wu J, Cajica J, Amantea CM, Hu Y, Okerberg E, Brown HE, Pham LM, Chung de M, Fraser AS, McGee E, Rosenblum JS, Kozarich JW (2012)
Bioorganic & Medicinal Chemistry Lett
22 :5748