Detail of "3432-99-3"

Reference

The formaldehyde-donating activity of N5,N10-methylenetetrahydrofolic acid in xenobiotic biotransformation

The formaldehyde-donating activity of N5,N10-methylenetetrahydrofolic acid in xenobiotic biotransformation. Kucharczyk, N.; Yang, J. T.; Wong, K.In this study，54063-54-6 is also used. K.; Sofia, R. D. (Wallace Lab., Carter-Wallace, Inc., Cranbury, NJ 08512, USA). Xenobiotica, 14(8), 667-76 (English) 1984. CODEN: XENOBH. ISSN: 0049-8254. DOCUMENT TYPE: Journal CA Section: 4 (Toxicology) Section cross-reference(s): 1 Reaction of reproterol (I) [54063-54-6] with HCHO [50-00-0] liberated in a soln. of N5,N10-methylenetetrahydrofolic acid [3432-99-3] at pH 7.3 led to the formation of 7-[3-(4,6,8-trihydroxy-1,2,3,4-tetrahydroisoquinolinyl-2)propyl]theophy lline (II) [72461-73-5], but no such reaction was obsd. in a soln. of N5-methyltetrahydrofolic acid. II was also formed by incubation of I with rat-liver subcellular fractions. The highest HCHO-donating activity was found in the sol. fraction but some activity was also obsd. with washed mitochondria and microsomes. Dimedone [126-81-8] was transformed to methylenebisdimedone [2181-22-8] by incubation with the sol. fraction. The amt. of HCHO liberated in the sol. fraction during a 4 h incubation at 22° was 1-3.6 mmol/g of liver. Metaproterenol [586-06-1] and terbutaline [23031-25-6], structurally related to I, reacted with HCHO to yield the corresponding tetrahydro-isoquinolines. The rate of this chem. reaction for the 3 drugs correlated with the amt. of the tetrahydroquinolines formed by incubation with the sol. fraction and in orally dosed rats. .

Cytotoxicity of 5-fluoro-2'-deoxyuridine: Requirement for reduced folate cofactors and antagonism by methotrexate

Cytotoxicity of 5-fluoro-2'-deoxyuridine: Requirement for reduced folate cofactors and antagonism by methotrexate. Ullman, Buddy; Lee, Melinda; Martin, David W., Jr.; Santi, Daniel V. (Dep. Biochem. Biophys., Univ. California, San Francisco, Calif., USA). Proc. Natl. Acad. Sci. U. S. A., 75(2), 980-3 (English) 1978. CODEN: PNASA6. ISSN: 0027-8424. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Potent in vitro inhibition of thymidylate synthase (EC 2.1.1.45) [9031-61-2] by 5-fluoro-2'-deoxyuridylate [964-26-1] required 5,10-methylenetetrahydrofolate [3432-99-3]. The cytotoxicity of 5-fluoro-2'-deoxyuridine (I) [50-91-9] towards cultured L1210 mouse leukemia cells was reduced when intracellular reduced folates were depleted, either by limiting the source in the media or by inhibition of dihydrofolate reductase with methotrexate [59-05-2]. Likewise, the intracellular amt. of 5-fluoro-2'-deoxyuridylate covalently bound to thymidylate synthase in L1210 cells treated with I was greatly diminished when cells were depleted of folate cofactors. The folate requirement for optimal growth of L1210 cells was lower than that required for maximal cytotoxicity of I. These findings provide a biochem. rationale that may be useful in designing clin. protocols that use 5-fluorinated uracil analogs.