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Volumn 18, Issue 6, 2008, Pages 2206-2210

Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors

Author keywords

Cancer; Metabolism; Pyrophosphate; Thiamine; Transketolase

Indexed keywords

3 (6 METHYL 2 AMINOPYRIDIN 3 YLMETHYL) 5 (2 HYDROXYETHYL) 4 METHYLTHIAZOL 3 IUM CHLORIDE; GLUCOSE 6 PHOSPHATE DEHYDROGENASE; OXOGLUTARATE DEHYDROGENASE; PENTOSE PHOSPHATE; RIBOSE; THIAMINE DERIVATIVE; TRANSKETOLASE; UNCLASSIFIED DRUG;

EID: 40749095542     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.11.101     Document Type: Article
Times cited : (44)

References (19)
  • 11
    • 0038552927 scopus 로고
    • This compound has been previously reported
    • This compound has been previously reported. Matsukawa T., and Matsuno T. Yakugaku Zasshi 64 (1944) 145
    • (1944) Yakugaku Zasshi , vol.64 , pp. 145
    • Matsukawa, T.1    Matsuno, T.2
  • 15
    • 40749097919 scopus 로고    scopus 로고
    • Boyd, S. A. WO2005095391.
    • Boyd, S. A. WO2005095391.
  • 17
    • 40749147429 scopus 로고    scopus 로고
    • note
    • Prior to performing the TPPK/apo-TK assay, each compound was evaluated for its ability to be pyrophosphorylated by TPPK using thiamine as a control substrate. The extent of substrate pyrophosphorylation relative to thiamine pyrophosphorylation was determined prior to competition with TPP in inhibiting TK activity according to methods described in WO2005/095391.
  • 18
    • 40749156069 scopus 로고    scopus 로고
    • Gyuris, J.; O'Hagan, R. C.; Han, M.; Robinson, M.; Weiler, S., WO2005094803.
    • Gyuris, J.; O'Hagan, R. C.; Han, M.; Robinson, M.; Weiler, S., WO2005094803.
  • 19
    • 40749153733 scopus 로고    scopus 로고
    • note
    • Though other compounds (e.g., 13 and 26) demonstrated comparable or better cellular potency to compound 1, the latter was tested in the xenograft model due to its synthesis being amenable to scaleup at the time the xenograft experiments were performed.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.