Chemotherapy is one of the major approaches for the treatment of cancer. Therefore,
the development of new chemotherapy drugs is an important aspect of medicinal
chemistry. Chemotherapeutic agents include isocoumarins, which are privileged
structures with potential antitumoral activity. Herein, a new 3-substituted
isocoumarin was synthesized from 2-iodo-3,5-dimethoxy-benzoic acid and oct-1-yne in a
cross-coupling Sonogashira reaction followed by a copper iodide-catalyzed
intramolecular cyclization as key step using MeOH/Et3N as the solvent
system. The present study also evaluated the leukometry, phagocytic activity,
genotoxic potential and cell death induction of three different doses (5 mg/kg, 10
mg/kg and 20 mg/kg) of this newly synthesized isocoumarin, alone and in combination
with the commercial chemotherapeutic agents cyclophosphamide (100 mg/kg) and
cisplatin (6 mg/kg) in male Swiss mice. The results suggest that the isocoumarin has
genotoxicity and causes cell death. Noteworthy, this new compound can increase
splenic phagocytosis and lymphocyte frequency, which are related to immunomodulatory
activity. When combined with either cyclophosphamide or cisplatin, chemopreventive
activity led to a reduction in the effects of both chemotherapeutic drugs. Thus, the
new isocoumarin is not a candidate for chemotherapeutic adjuvant in treatments using
cyclophosphamide or cisplatin. Nevertheless, the compound itself is an important
prototype for the development of new antitumor drugs.
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