Synthesis and evaluation of novel substituted 5-hydroxycoumarin and pyranocoumarin derivatives exhibiting significant antiproliferative activity against breast cancer cell lines.

A library of novel 5-hydroxycoumarin and pyranocoumarin derivatives was constructed via silica sulfuric acid-catalyzed pechmann reaction and Pd(0)-catalyzed suzuki coupling in tandem, and their antiproliferative activities against breast cancer cells MCF-7 and MDA-MB-231 were evaluated. The results showed that compounds such as 6b, 6d, 6h, and 6k possess significant antiproliferative activity against MCF-7 cell line with the IC(50) values of 7.2, 5.3, 3.3, and 6.5 microM, respectively.