Abstract
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).
| Original language | English |
|---|---|
| Pages (from-to) | 1152-1157 |
| Number of pages | 6 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 48 |
| Issue number | 4 |
| DOIs | |
| Publication status | Published - Feb 24 2005 |
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ASJC Scopus subject areas
- Organic Chemistry
Cite this
Synthesis and cytotoxic evaluation of novel spirohydantoin derivatives of the dihydrothieno[2,3-b]naphtho-4,9-dione system. / Gomez-Monterrey, Isabel; Santelli, Giovanni; Campiglia, Pietro; Califano, Daniela; Falasconi, Fabiane; Pisano, Claudio; Vesci, Loredana; Lama, Teresa; Grieco, Paolo; Novellino, Ettore.
In: Journal of Medicinal Chemistry, Vol. 48, No. 4, 24.02.2005, p. 1152-1157.Research output: Contribution to journal › Article
}
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).
UR - http://www.scopus.com/inward/record.url?scp=13944260443&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=13944260443&partnerID=8YFLogxK
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 -