The synthesis and cytotoxic evaluation of 3-(alkyl)(alkyl-substituted) spiro[(dihydroimidazo-2,4-dione)-5,3′-(2′,3′-dihydrothieno[2, 3-b]naphtho-4′,9′-dione)]derivatives are described. Evaluation of these analogues against the MCF-7 human breast carcinoma and SW 620 human colon carcinoma cell lines uncovered for most of the compounds a cytotoxic potency comparable to or greater than that of doxorubicin. Compound 15 exhibited remarkable cytotoxic activity against several other human solid tumor cell lines. Interestingly, only a partial cross-resistance to compound 15 in selected tumor cell sublines known to be resistant to doxorubicin (MCF-7/Dx and A2780/Dx) was observed, whereas a total absence of cross-resistance in a tumor cell subline selected for resistance to cisplatin was found (A2780/DDP).
|Titolo:||Synthesis and cytotoxic evaluation of novel spirohydantoin derivatives of the dihydrothieno[2,3-b]naphtho-4,9-dione system.|
|Autori interni:||CAMPIGLIA, Pietro|
|Data di pubblicazione:||2005|
|Rivista:||JOURNAL OF MEDICINAL CHEMISTRY|
|Appare nelle tipologie:||1.1.2 Articolo su rivista con ISSN|