Cytotoxicity of some 1-[2,4-dihydroxyphenyl]-3-[4-phenylpiperidin-1-yl] prop-2-en-1-one derivatives using MTT assay

Some N-substituted piperidine structures were synthesized and evaluated for cytotoxic activity against four different cell lines using the standard MTT assay method and Doxorubicin was used as the reference drug. The result of cytotoxic activity as a measurement of IC50 values revealed that three of the synthesized compounds were active against breast cancer cell line. Compound 6a bearing hydroxyl at para position of piperidine ring was the most active compound within this series. The N-subtituted piperidine with propene substructure could be considered as a lead structure for further studies of structure activity relationship to develop more potent compounds in future. The compounds were evaluated against four different cell lines using the standard MTT assay method and doxorubicin was used as the reference drug. The IC50 values were determined by constructing dose-response curves and revealed that three of the synthesized compounds were active against breast cancer cell lines. Compound 6a bearing hydroxyl at para position of piperidine ring was the most active compound within this series

Synthesis and antidiabetic evaluation of benzenesulfonamide derivatives

The complex metabolic syndrome, diabetes mellitus, is a major human health concern in the world and is estimated to affect 300 million people by the year 2025. Several drugs such as sulfonylureas and biguanides are presently available to reduce hyperglycemia in diabetes mellitus. These drugs have side effects and thus searching for a new class of compounds is essential to overcome this problems. A series of seven novel N-[4-phenylthiazol-2-yl]benzenesulfonamides derivatives were synthesized and assayed in-vivo to investigate their antidiabetic activities by streptozotocin-induced model in rat. These derivatives showed considerable biological efficacy when compared to glibenclamide, a potent and well-known antidiabetic agent, as a reference drug. Four of the compounds were effective, amongst which 13 show more prominent activity at 100 mg/Kg p.o. The experimental results are statistically significant at p < 0.05 level