TY - JOUR
T1 - Synthesis and cytotoxic evaluation of novel spirohydantoin derivatives of the dihydrothieno[2,3-b]naphtho-4,9-dione system
AU - Gomez-Monterrey, Isabel
AU - Santelli, Giovanni
AU - Campiglia, Pietro
AU - Califano, Daniela
AU - Falasconi, Fabiane
AU - Pisano, Claudio
AU - Vesci, Loredana
AU - Lama, Teresa
AU - Grieco, Paolo
AU - Novellino, Ettore
PY - 2005/2/24
Y1 - 2005/2/24
N2 - 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).
AB - 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).
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U2 - 10.1021/jm0408565
DO - 10.1021/jm0408565
M3 - Article
C2 - 15715481
AN - SCOPUS:13944260443
VL - 48
SP - 1152
EP - 1157
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 4
ER -