Hybrid compounds with two redox centres: Modular synthesis of chalcogen-containing lapachones and studies on their antitumor activity

摘要: Chalcogen-containing β-lapachone derivatives were synthesized using a straightforward methodology and evaluated against several cancer cell lines (leukaemia, human colon carcinoma, prostate, metastatic ovarian, central nervous system breast), showing, in some cases, IC50 values below 1 μM. The cytotoxic potential of the lapachones was also assayed non-tumor cells: peripheral blood mononuclear cells, two murine fibroblast (L929 V79 cells) MDCK (canine kidney epithelial cells). These compounds could provide promising new lead for anticancer drug development. This manuscript reports important findings since few authors have described C-3 substituted with potent antitumor activity. employed allowed preparation from lapachol within minutes green approach.