Drug intelligence / Profile preview

Compound III (2,7-substituted carbazole derivative)

Development stage
Preclinical
Lead developer
Shanxi University
Modality
Small Molecules
01

Overview

Compound III is a 2,7-substituted carbazole derivative featuring a boronic acid terminal group [-B(OH)2], developed as a small molecule inhibitor of Autotaxin (ATX). This compound is the result of a collaborative research effort between Shanxi University, Changzhi University, and the University of Memphis. It targets the Autotaxin-Lysophosphatidic Acid (ATX-LPA) signaling pathway, which is known to facilitate tumor progression, metastasis, and survival in various malignancies. In preclinical studies, Compound III demonstrated potent inhibition of ATX enzymatic activity (tested with FS-3 and Bis-pNpp substrates) and exhibited significant cytotoxicity against human colorectal (SW620, SW480), pancreatic (PANC-1), and ovarian (SKOV-3) cancer cell lines. Molecular docking studies have been used to characterize its binding interactions with the ATX enzyme, positioning it as a lead candidate for further development as an anticancer therapeutic.

Other names
2,7-substituted carbazole derivative with boronic acid terminal group
02

Targets

ENPP2 (Ectonucleotide pyrophosphatase/phosphodiesterase family member 2)

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