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- W1978697462 abstract "A novel quinoline derivative, TAS-103 (6-[[2-(dimethyIamino)ethyl]amino]-3-hydroxy-7H-indeno[2,l-c]quinolin-7-one dihydrochloride), was developed as an anticancer agent targeting topoisomerases (topo) I and II, with marked efficacy in solid tumors. TAS-103 inhibited topo I and II (IC50: 2 μM, 6.5 μM) at a concentration similar to or lower than those of previous agents, and had a strong cytotoxic effect on P388 and KB cells (IC50,: 0.0011 μM, 0.0096 μM). TAS-103 stabilized topo I and II-DNA cleavable complexes in KB cells, generating a similar amount of topo II-DNA complex to that induced by etoposide (VP-16) but a smaller amount of topo I-DNA complex than that produced by camptothecin (CPT). In the in vivo study, intermittent i.v. administration was markedly effective against s.c.-implanted murine tumors. Furthermore, TAS-103 had marked efficacy against various lung metastatic tumors, and a broad antitumor spectrum in human tumor xenografts (derived from lung, colon, stomach, breast, and pancreatic cancer). The efficacy of TAS-103 was generally greater than that of irinotecan (CPT-11), VP-16, or cis-diamminedichloroplatinum (CDDP)." @default.
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- W1978697462 date "1997-10-01" @default.
- W1978697462 modified "2023-09-26" @default.
- W1978697462 title "Antitumor Activity of a Novel Quinoline Derivative, TAS-103, with Inhibitory Effects on Topoisomerases I and II" @default.
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- W1978697462 doi "https://doi.org/10.1111/j.1349-7006.1997.tb00320.x" @default.
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