K. Harrap

Publications193
h-index43
Citations6,479
Highly Influential Citations118
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Pharmacokinetics of cis-diammine-1,1-cyclobutane dicarboxylate platinum(II) in patients with normal and impaired renal function.
cis-Diammine-1,1-cyclobutane dicarboxylate platinum(II) (CBDCA, JM8) is a nonnephrotoxic analogue of cisplatin currently undergoing clinical evaluation. Pharmacokinetic studies have been performed in… Expand
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A potent antitumour quinazoline inhibitor of thymidylate synthetase: synthesis, biological properties and therapeutic results in mice.
Abstract We describe the synthesis and some biological properties of N-(4-N-[2-amino-4-hydroxy-6-quinazolinyl)methyl]prop-2-ynylaminobenzoyl)- l -glutamic acid (CB 3717), a potent antifolate… Expand
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Biological properties of ten human ovarian carcinoma cell lines: calibration in vitro against four platinum complexes.
Ten human ovarian carcinoma cell lines have been studied as a potential in vitro screen for the development of novel anticancer platinum complexes. Lines have been established and developed both from… Expand
  • 179
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ZD1694 (Tomudex): a new thymidylate synthase inhibitor with activity in colorectal cancer.
ZD1694 (Tomudex) is a new antifolate which is a specific inhibitor of thymidylate synthase (TS). Evidence suggests that ZD1694 has a spectrum of activity that only partially overlaps with… Expand
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Studies with a mathematical model of folate metabolism.
Abstract A system of integrated kinetic equations has been constructed which attempts to provide a quantitative description of the principal reactions of folate metabolism in cells of the mouse… Expand
  • 108
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Modulation of anti-metabolite effects. Effects of thymidine on the efficacy of the quinazoline-based thymidylate synthetase inhibitor, CB3717.
CB3717 (N-(4-(N-((2-amino-4- hydroxy-6-quinazolinyl)methyl)prop-2-ynylamino ) benzoyl)-L-glutamic acid) is an antitumour agent that inhibits thymidylate synthetase (TS). A dose-dependent fall in… Expand
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Changes in the deoxyribonucleoside triphosphate pools of mouse 5178Y lymphoma cells following exposure to methotrexate or 5-fluorouracil.
Changes are reported in the deoxyribonucleoside triphosphate pools of L5178Y cells during their exposure to methotrexate or 5-fluorouracil. For both drugs the intracellular deoxythymidine… Expand
  • 86
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The relationships between glutathione, glutathione-S-transferase and cytotoxicity of platinum drugs and melphalan in eight human ovarian carcinoma cell lines.
The role of glutathione (GSH) and GSH-S-transferase (GST) activity in modulating the cytotoxicity of four platinum drugs and melphalan was evaluated in eight human ovarian carcinoma cell lines. The… Expand
  • 252
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A novel trans-platinum coordination complex possessing in vitro and in vivo antitumor activity.
As part of a drug discovery program to discover more effective platinum-based anticancer drugs, a series of platinum complexes of trans coordination geometry centered on… Expand
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Establishment and characterization of an in vitro model of acquired resistance to cisplatin in a human testicular nonseminomatous germ cell line.
Clinically, human testicular nonseminomatous germ cell tumors exhibit remarkable sensitivity to platinum-based chemotherapy. To define better the mechanistic basis for this unusual sensitivity, the… Expand
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