Semisynthsis of novel sulfonamides, thioureas and biphenylsulfones as a new class of anticancer agents by using L-norephedrine as strategic starting material

In continuation of our work on synthesis of novel anticancer agents, a new series of sulfonamides carrying a biologically active thiourea 3, 4, biphenylsulfones bearing thiourea 8-10 and oxazole thione 11 were designed and synthesized using L-norephedrine [phenylpropanolamine (PPA)] as strategic starting material. The synthesized compounds were evaluated in vitro for their anticancer activity against the human breast (MCF- 7), human liver (HEPG2) and human colon (HCT116) cancer cell lines. Bisthiourea compound 8 is nearly as active as doxorubicin against (MCF-7 and HEPG2) cell lines with value (IC₅₀ = 6.93 and 4.0 μg/mL). Compounds 3, 4, 9-11 exhibited a moderate activity compared with doxorubicin as reference drug.