2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl]quinazoline (tmq), a potent non-classical folate antagonist inhibitor--I effect on dihydrofolate reductase and growth of rodent tumors in vitro and in vivo.

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作者信息

Bertino J R, Sawicki W L, Moroson B A, Cashmore A R, Elslager E F

出版信息

Biochem Pharmacol. 1979 Jun 15;28(12):1983-7. doi: 10.1016/0006-2952(79)90655-5.

DOI:10.1016/0006-2952(79)90655-5

PMID:454469

Abstract

摘要

相似文献

2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl]quinazoline (tmq), a potent non-classical folate antagonist inhibitor--I effect on dihydrofolate reductase and growth of rodent tumors in vitro and in vivo.

Biochem Pharmacol. 1979 Jun 15;28(12):1983-7. doi: 10.1016/0006-2952(79)90655-5.

Uptake and efficacy of trimetrexate (TMQ, 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline), a non-classical antifolate in methotrexate-resistant leukemia cells in vitro.三甲曲沙（TMQ，2,4-二氨基-5-甲基-6-[(3,4,5-三甲氧基苯胺基)甲基]喹唑啉）在耐甲氨蝶呤白血病细胞中的体外摄取及疗效，一种非经典抗叶酸剂

Biochem Pharmacol. 1984 May 15;33(10):1697-9. doi: 10.1016/0006-2952(84)90298-3.

Quinazolines as inhibitors of dihydrofolate reductase. 4. Classical analogues of folic and isofolic acids.喹唑啉类作为二氢叶酸还原酶抑制剂。4. 叶酸和异叶酸的经典类似物。

J Med Chem. 1977 Apr;20(4):588-91. doi: 10.1021/jm00214a030.

Increased thymidylate synthase in L1210 cells possessing acquired resistance to N10-propargyl-5,8-dideazafolic acid (CB3717): development, characterization, and cross-resistance studies.对N10-炔丙基-5,8-二去氮叶酸（CB3717）产生获得性耐药的L1210细胞中胸苷酸合成酶增加：发育、特征及交叉耐药性研究

Cancer Res. 1986 Jun;46(6):2810-5.

Quinazolines as inhibitors of dihydrofolate reductase. 3. Analogs of pteroic and isopteroic acids.喹唑啉类作为二氢叶酸还原酶抑制剂。3. 蝶酸和异蝶酸类似物。

J Med Chem. 1975 Dec;18(12):1191-4. doi: 10.1021/jm00246a004.

Conformational analysis of antineoplastic antifolates: the crystal structure of trimetrexate and the aminopterine derivative 4-[N-[(2,4-diamino-6-pteridinyl)methyl]amino]benzoic acid.

J Med Chem. 1987 Oct;30(10):1843-8. doi: 10.1021/jm00393a027.

Establishment of methotrexate-resistant human acute lymphoblastic leukemia cells in culture and effects of folate antagonists.培养耐甲氨蝶呤人急性淋巴细胞白血病细胞系及叶酸拮抗剂的作用

Cancer Res. 1982 May;42(5):1655-60.

Evidence for a localized conversion of endogenous tetrahydrofolate cofactors to dihydrofolate as an important element in antifolate action in murine leukemia cells.内源性四氢叶酸辅因子局部转化为二氢叶酸作为小鼠白血病细胞中抗叶酸作用重要因素的证据。

Biochem Pharmacol. 1990 Jun 15;39(12):2005-14. doi: 10.1016/0006-2952(90)90622-r.

Inhibition of mammalian dihydrofolate reductase by selected 2,4-diaminiquinazolines and related compounds.某些2,4-二氨基喹唑啉及其相关化合物对哺乳动物二氢叶酸还原酶的抑制作用。

J Med Chem. 1974 Sep;17(9):943-7. doi: 10.1021/jm00255a007.

Inhibition of metabolism of the 'nonclassical' antifolate, trimetrexate (2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl]quinazoline) by drugs containing an imidazole moiety.

Pharmacology. 1985;30(5):266-72. doi: 10.1159/000138077.

引用本文的文献

Structure and dynamics in solution of the complex of Lactobacillus casei dihydrofolate reductase with the new lipophilic antifolate drug trimetrexate.干酪乳杆菌二氢叶酸还原酶与新型亲脂性抗叶酸药物三甲曲沙复合物在溶液中的结构与动力学

Protein Sci. 1999 Mar;8(3):467-81. doi: 10.1110/ps.8.3.467.

Cytotoxicity of trimetrexate against antifolate-resistant human T-cell leukemia cell lines developed in oxidized or reduced folate.三甲曲沙对在氧化型或还原型叶酸中培养出的抗叶酸人T细胞白血病细胞系的细胞毒性。

Jpn J Cancer Res. 1997 Sep;88(9):900-6. doi: 10.1111/j.1349-7006.1997.tb00467.x.

Phase II trial of trimetrexate in advanced esophageal cancer: a southwest oncology group study.三甲曲沙治疗晚期食管癌的II期试验：一项西南肿瘤协作组研究

Invest New Drugs. 1996;13(4):363-5. doi: 10.1007/BF00873146.

Differential alterations of dihydrofolate reductase gene in human leukemia cell lines made resistant to various folate analogues.对多种叶酸类似物产生抗性的人白血病细胞系中二氢叶酸还原酶基因的差异改变。

Jpn J Cancer Res. 1993 Jan;84(1):9-12. doi: 10.1111/j.1349-7006.1993.tb02776.x.

Phase II study of trimetrexate in previously untreated patients with hepatocellular carcinoma. Southwest Oncology Group study 8712.

Invest New Drugs. 1993 Feb;11(1):45-6. doi: 10.1007/BF00873909.

Phase II trial of trimetrexate in untreated advanced gastric carcinoma. A Southwest Oncology Group study.

Invest New Drugs. 1994;12(2):155-7. doi: 10.1007/BF00874448.

Biological and biochemical properties of new anticancer folate antagonists.新型抗癌叶酸拮抗剂的生物学和生物化学特性

Cancer Metastasis Rev. 1987;5(3):251-70. doi: 10.1007/BF00047000.

Trimetrexate: a new antifol entering clinical trials.

Invest New Drugs. 1985;3(1):71-5. doi: 10.1007/BF00176828.

Bioavailability of oral trimetrexate in patients with acquired immunodeficiency syndrome.获得性免疫缺陷综合征患者口服三甲曲沙的生物利用度。

Antimicrob Agents Chemother. 1988 Mar;32(3):324-6. doi: 10.1128/AAC.32.3.324.

Cell cycle effects of trimetrexate (CI-898).三甲曲沙（CI-898）对细胞周期的影响。

Cancer Chemother Pharmacol. 1986;16(2):116-20. doi: 10.1007/BF00256159.

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