SONOCRYSTALLIZATION OF A NOVEL SYNTHESIZED ANTICANCER DERIVATIVE OF 2-THIOURACIL-6-SULPHONAMIDE TO ENHANCE ITS WATER SOLUBILITY.
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Abstract
A potent and promising anticancer agent, 2-thiouracil-5-(2,4,6-trimethylphenyl) sulphonamide 3, was synthesized by reacting 2-thiouracil-5-sulphonyl chloride 2 with 2,4,6-trimethylphenyl amine in the existence of pyridine as an acid scavenger. Its poor water solubility, however, limits the in vivo screening, which led us to employ a non-conventional and secure ultra-sonic-assisted process to solubilize it to improve its water solubility and bioavailability for use in future studies. Target compound 3 melt was added to deionized water that was kept at 60 degrees Celsius and simultaneously exposed to ultrasonic energy in a process known as melt sonocrystallization. After the distributed droplets solidified, the resulting agglomerates were filtered out, allowed to dry at room temperature, and then tested for saturated solubility. The target molecule was tested as an anticancer agent against human A-2780 ovarian, HT-29 colon, MCF-7 breast, and HEPG-2 liver carcinoma cells both before and after sonocrystallization. In comparison to 5-Fluorouracil, which was employed as a benchmark, it demonstrated an encouraging action.