|1.||Smetzer, L: 1 article (07/2001)|
|2.||Johnson, T R: 1 article (07/2001)|
|3.||Lampkin, T: 1 article (07/2001)|
|4.||Von Hoff, D D: 1 article (07/2001)|
|5.||Goetz, A: 1 article (07/2001)|
|6.||Hohneker, J A: 1 article (07/2001)|
|7.||Burris, H: 1 article (07/2001)|
|8.||Rowinsky, E K: 1 article (07/2001)|
|9.||Sailstad, J: 1 article (07/2001)|
|10.||Schwartz, G: 1 article (07/2001)|
07/15/1996 - "Duch et at., Cancer Res., 53:810-818, 1993), 1843U89 is 10-80-fold more cytotoxic than the close structural analogue 1031U89, which is an equipotent inhibitor of TS but is a less efficient substrate for FPGS. "
01/01/1994 - "The results of these experiments suggest that 1843U89 should have potent solid tumor activity in humans but should be less effective in mice due to differences in circulating thymidine levels (0.1 vs 1 microM, respectively)."
07/01/2001 - "Because folic acid pretreatment results in no diminution of the antitumor activity of 1843U89 in preclinical studies and ameliorates the toxic effects of 1843U89 in both preclinical models and cancer patients, the therapeutic index of 1843U89 may be enhanced by folic acid pretreatment and, therefore, the development of 1843U89 with folic acid is warranted. "
12/15/1995 - "The results show that an oral dose of folic acid 30 min prior to i.v. 1843U89 can block mouse and dog intestinal toxicity without decreasing efficacy of 1843U89 in two of three human tumor lines in the nude mouse. "
07/15/1996 - "1843U89 is a potent inhibitor (Ki = 0.09 nM) of thymidylate synthase (TS; EC 184.108.40.206) that is in clinical trial for the treatment of solid tumors. "
07/15/1996 - "In the current study, we measured intracellular levels of polyglutamated anabolites of 1031U89, 1843U89, and three other benzoquinazoline inhibitors of TS as well as anabolites of D1694 in HCT-8 ileocecal carcinoma cells. "
01/01/1994 - "The activity of a novel thymidylate synthase inhibitor, 1843U89, against WiDr human colon carcinoma multicellular tumor spheroids was investigated. "
06/01/1999 - "Transfection of multidrug resistance proteins (MRPs) MRP1 and MRP2 in human ovarian carcinoma 2008 cells conferred a marked level of resistance to short-term (1-4 h) exposure to the polyglutamatable antifolates methotrexate (MTX; 21-74-fold), ZD1694 (4-138-fold), and GW1843 (101-156-fold). "
10/06/2000 - "We have studied the molecular basis for the resistance of human CEM leukemia cells to GW1843, a thymidylate synthase inhibitor. "
08/01/1997 - "In contrast to MTX, both Tomudex (Zeneca Pharmaceuticals, Wilmington, DE) and 1843U89, potent inhibitors of thymidylate synthetase, have low Kms for folylpolyglutamate synthetase, and polyglutamate forms of these inhibitors are accumulated to the same degree in both myeloid and lymphoid acute leukemia cells, paralleling the equivalent cytotoxicity found between myeloid and lymphoid leukemia cell lines. "
|5.||T-Cell Leukemia (Leukemia, T Cell)
|1.||Folic Acid (Vitamin M)
|3.||raltitrexed (D 1694)
|7.||Glutamic Acid (Glutamate)
|9.||Tetrahydrofolate Dehydrogenase (Dihydrofolate Reductase)
|10.||Polyglutamic Acid (Polyglutamate)