当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Synthesis and structure-activity relationship of (1-halo-2-naphthyl) carbamate-based inhibitors of KIAA1363 (NCEH1/AADACL1).

Synthesis and structure-activity relationship of (1-halo-2-naphthyl) carbamate-based inhibitors of KIAA1363 (NCEH1/AADACL1).

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 μM 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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

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

doi

10.1016/j.bmcl.2012.05.102

subject

Has Abstract

pub_date

2012-09-01 00:00:00

pages

5748-51

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00714-7

journal_volume

22

pub_type

杂志文章

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