Introduction

The invention provides new effective compounds with therapeutic action against breast cancer (BC) cells and in particular, against its most aggressive forms (triple-negative breast cancer – TNBCs). The antitumor efficacy of some compounds of the invention was evaluated by in vitro tests conducted on three breast tumor cell lines: MCF-7, MDA-MB-231 and MDA-MB-468.

Technical features

The dihydrofurofuranone derivatives were obtained in one step, starting from simple substrates (4-yne-1,3-diols, carbon monoxide, and  oxygen), under the catalytic action of PdI₂ in conjunction with an excess of potassium iodide (KI). The dihydrofurofuranones thus synthesized have significant antiproliferative activity in vitro on human breast adenocarcinoma cell lines, both hormone receptor positive (MCF-7) and triple negative (triple-negative breast cancer [TNBC]; MDA-MB-231 and MDAMB-468), while exhibiting practically no effects on normal MCF-10A (human mammary epithelial) and 3T3-L1 (murine fibroblasts) cells. Thus, these compounds have the potential to expand the therapeutic options against BC, and in particular, against its most aggressive forms (TNBCs).

Possible Applications

• Direct, rapid, and inexpensive synthesis of antitumor agents from simple substrates;
• Expanding the therapeutic options against BC, and in particular, against its most aggressive forms (TNBCs).

Advantages

• Novel catalytic double cyclization method leading to bioactive bicyclic heterocycles in one step.
• Significant antitumor activity against breast cancer cells, including the most aggressive triple-negative BC cells.
• Low degree of global toxicity and reduced side effects.