Novel N-phenyl-2-(aniline) benzamide hydrochloride salt development for colon cancer therapy.

ABSTRACT:

Introduction

N-phenyl-2-(aniline) analog N53 is a previously discovered dual inhibitor of Topo I and COX-2, which exhibited significant anti-colon cancer activity in vitro, but the poor solubility and moderate anti-cancer activity in vivo hindered its further development.

Methods

To rectify the suboptimal drug properties of N53, a series of salt forms were developed and further evaluated through in vivo and in vitro experiments.

Results

The hydrochloride (N53·HCl) has a well-characterized crystal structure and its solubility reached 540.1 μg/mL, which is nearly 1,700 times higher than that of N53 (0.32 μg/mL). Increasing the N53 solubility consistently promotes its effective concentration, further e

SUBMITTER: Peng Y 

PROVIDER: S-EPMC11570809 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature