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Antitumor agents against breast cancer

Composti furanoniciFurofuranone derivativesOrganic SynthesisSintesi organicaToxicology EvaluationTriple-negative breast cancerTumore mammario triplo negativoValutazione tossicologica

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.