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举例 :可输入Filippa Pettersson 或者 Cancer Res. 75(6) , 1102-12, (2015) 或者10.1002/anie.201600521

Potential inhibitors of nucleotide biosynthesis. 1. Nitrosoureidonucleosides. 2

…, HJ Thomas, RW Brockman, GP Wheeler

文献索引：Montgomery, John A.; Thomas, H. Jeanette; Brockman, R. Wallace; Wheeler, Glynn P. Journal of Medicinal Chemistry, 1981 , vol. 24, # 2 p. 184 - 189

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被引用次数: 23

摘要

Several nitrosoureidonucleosides (9a, 9b, lla, llb, 18 and 20) designed as inhibitors of enzymes that metabolize purine and pyrimidine nucleotides have been prepared and their chemical and biological properties studied. The low level of biological activity observed may be due to the unexpected stability of these nitrosoureas compared to biologically active compounds such as N-methyl-N-nitrwurea (MNU), N~-bis (2-chloroethyl)-N'-nitrosourea ( ...

N-(2-aminoethyl)-N-cyclohexylurea结构式

N-(2-aminoethyl...

~%

N-[2-(cyclohexylcarbamoyl-nitroso-amino)ethyl]-3,4-dihydroxy-5-(6-oxo-3H-purin-9-yl)oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

环己基异氰酸酯结构式

环己基异氰酸酯

~%

N-[2-(cyclohexylcarbamoyl-nitroso-amino)ethyl]-3,4-dihydroxy-5-(6-oxo-3H-purin-9-yl)oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

b-D-Ribofuranuronic acid,1-deoxy-1-(1,6-dihydro-6-oxo-9H-purin-9-yl)-结构式

b-D-Ribofuranur...

~%

N-[2-(cyclohexylcarbamoyl-nitroso-amino)ethyl]-3,4-dihydroxy-5-(6-oxo-3H-purin-9-yl)oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

N-[2-(cyclohexylcarbamoylamino)ethyl]-3,4-dihydroxy-5-(6-oxo-3H-purin-9-yl)oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

~22%

N-[2-(cyclohexylcarbamoyl-nitroso-amino)ethyl]-3,4-dihydroxy-5-(6-oxo-3H-purin-9-yl)oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

b-D-Ribofuranuronamide,N-[2-[[(cyclohexylamino)carbonyl]amino]ethyl]-1-deoxy-1-(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)-结构式

b-D-Ribofuranur...

~38%

N-[2-(cyclohexylcarbamoyl-nitroso-amino)ethyl]-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxy-oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

N-(2-aminoethyl)-N-cyclohexylurea结构式

N-(2-aminoethyl...

~%

N-[2-(cyclohexylcarbamoyl-nitroso-amino)ethyl]-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxy-oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

环己基异氰酸酯结构式

环己基异氰酸酯

~%

N-[2-(cyclohexylcarbamoyl-nitroso-amino)ethyl]-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxy-oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

b-D-Ribofuranuronic acid,1-deoxy-1-(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)-结构式

b-D-Ribofuranur...

~%

N-[2-(cyclohexylcarbamoyl-nitroso-amino)ethyl]-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxy-oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

N-(2-aminoethyl)-N-cyclohexylurea结构式

N-(2-aminoethyl...

b-D-Ribofuranuronic acid,1-deoxy-1-(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)-结构式

b-D-Ribofuranur...

~52%

b-D-Ribofuranuronamide,N-[2-[[(cyclohexylamino)carbonyl]amino]ethyl]-1-deoxy-1-(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)-结构式

b-D-Ribofuranur...

环己基异氰酸酯结构式

环己基异氰酸酯

~%

b-D-Ribofuranuronamide,N-[2-[[(cyclohexylamino)carbonyl]amino]ethyl]-1-deoxy-1-(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)-结构式

b-D-Ribofuranur...

乙二胺结构式

异氰酸甲酯结构式

异氰酸甲酯

~30%

3-methyl-1-[2-(methylcarbamoylamino)ethyl]urea结构式

3-methyl-1-[2-(...

1-(2-aminoethyl)-3-methylurea结构式

1-(2-aminoethyl...

N-(2-aminoethyl)-N-cyclohexylurea结构式

N-(2-aminoethyl...

b-D-Ribofuranuronic acid,1-deoxy-1-(1,6-dihydro-6-oxo-9H-purin-9-yl)-结构式

b-D-Ribofuranur...

~71%

N-[2-(cyclohexylcarbamoylamino)ethyl]-3,4-dihydroxy-5-(6-oxo-3H-purin-9-yl)oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

环己基异氰酸酯结构式

环己基异氰酸酯

~%

N-[2-(cyclohexylcarbamoylamino)ethyl]-3,4-dihydroxy-5-(6-oxo-3H-purin-9-yl)oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

N-(2-aminoethyl)-N-cyclohexylurea结构式

N-(2-aminoethyl...

胸腺嘧啶脱氧核苷-5-羧酸结构式

胸腺嘧啶脱氧核苷-5-羧酸

~81%

b-D-erythro-Pentofuranuronamide,N-[2-[[(cyclohexylamino)carbonyl]amino]ethyl]-1,2-dideoxy-1-(3,4-dihydro-5-methyl-2,4-dioxo-1(2H)-pyrimidinyl)-结构式

b-D-erythro-Pen...

环己基异氰酸酯结构式

环己基异氰酸酯

~%

b-D-erythro-Pentofuranuronamide,N-[2-[[(cyclohexylamino)carbonyl]amino]ethyl]-1,2-dideoxy-1-(3,4-dihydro-5-methyl-2,4-dioxo-1(2H)-pyrimidinyl)-结构式

b-D-erythro-Pen...

b-D-Ribofuranuronic acid,1-deoxy-1-(1,6-dihydro-6-oxo-9H-purin-9-yl)-结构式

b-D-Ribofuranur...

~%

3,4-dihydroxy-N-[2-[(methyl-nitroso-carbamoyl)amino]ethyl]-5-(6-oxo-3H-purin-9-yl)oxolane-2-carboxamide结构式

3,4-dihydroxy-N...

3,4-dihydroxy-N-[2-(methylcarbamoylamino)ethyl]-5-(6-oxo-3H-purin-9-yl)oxolane-2-carboxamide结构式

3,4-dihydroxy-N...

~%

(2S,3S,4R,5R)-3,4-dihydroxy-N-(2-(3-methyl-1-nitrosoureido)ethyl)-5-(6-oxo-1,6-dihydro-9H-purin-9-yl)tetrahydrofuran-2-carboxamide结构式

(2S,3S,4R,5R)-3...

3,4-dihydroxy-N-[2-[(methyl-nitroso-carbamoyl)amino]ethyl]-5-(6-oxo-3H-purin-9-yl)oxolane-2-carboxamide结构式

3,4-dihydroxy-N...

3-hydroxy-N-[2-(methylcarbamoylamino)ethyl]-5-(5-methyl-2,4-dioxo-pyrimidin-1-yl)oxolane-2-carboxamide结构式

3-hydroxy-N-[2-...

~41%

(2S,3S,5R)-3-hydroxy-5-(2-hydroxy-5-methyl-4-oxopyrimidin-1(4H)-yl)-N-(2-(3-methyl-1-nitrosoureido)ethyl)tetrahydrofuran-2-carboxamide结构式

(2S,3S,5R)-3-hy...

3-hydroxy-5-(5-methyl-2,4-dioxo-pyrimidin-1-yl)-N-[2-[(methyl-nitroso-carbamoyl)amino]ethyl]oxolane-2-carboxamide结构式

3-hydroxy-5-(5-...

胸腺嘧啶脱氧核苷-5-羧酸结构式

胸腺嘧啶脱氧核苷-5-羧酸

~%

3-hydroxy-5-(5-methyl-2,4-dioxo-pyrimidin-1-yl)-N-[2-[(methyl-nitroso-carbamoyl)amino]ethyl]oxolane-2-carboxamide结构式

3-hydroxy-5-(5-...

b-D-Ribofuranuronic acid,1-deoxy-1-(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)-结构式

b-D-Ribofuranur...

~%

5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxy-N-[2-[(methyl-nitroso-carbamoyl)amino]ethyl]oxolane-2-carboxamide结构式

5-(2,4-dioxopyr...

1-(2-aminoethyl)-3-methylurea结构式

1-(2-aminoethyl...

b-D-Ribofuranuronic acid,1-deoxy-1-(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)-结构式

b-D-Ribofuranur...

~44%

b-D-Ribofuranuronamide,1-deoxy-1-(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)-N-[2-[[(methylamino)carbonyl]amino]ethyl]-结构式

b-D-Ribofuranur...

b-D-erythro-Pentofuranuronamide,N-[2-[[(cyclohexylamino)carbonyl]amino]ethyl]-1,2-dideoxy-1-(3,4-dihydro-5-methyl-2,4-dioxo-1(2H)-pyrimidinyl)-结构式

b-D-erythro-Pen...

~58%

N-[2-(cyclohexylcarbamoyl-nitroso-amino)ethyl]-3-hydroxy-5-(5-methyl-2,4-dioxo-pyrimidin-1-yl)oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

N-(2-aminoethyl)-N-cyclohexylurea结构式

N-(2-aminoethyl...

~%

N-[2-(cyclohexylcarbamoyl-nitroso-amino)ethyl]-3-hydroxy-5-(5-methyl-2,4-dioxo-pyrimidin-1-yl)oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

环己基异氰酸酯结构式

环己基异氰酸酯

~%

N-[2-(cyclohexylcarbamoyl-nitroso-amino)ethyl]-3-hydroxy-5-(5-methyl-2,4-dioxo-pyrimidin-1-yl)oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

胸腺嘧啶脱氧核苷-5-羧酸结构式

胸腺嘧啶脱氧核苷-5-羧酸

~%

N-[2-(cyclohexylcarbamoyl-nitroso-amino)ethyl]-3-hydroxy-5-(5-methyl-2,4-dioxo-pyrimidin-1-yl)oxolane-2-carboxamide结构式

N-[2-(cyclohexy...

胸腺嘧啶脱氧核苷-5-羧酸结构式

胸腺嘧啶脱氧核苷-5-羧酸

1-(2-aminoethyl)-3-methylurea结构式

1-(2-aminoethyl...

~74%

3-hydroxy-N-[2-(methylcarbamoylamino)ethyl]-5-(5-methyl-2,4-dioxo-pyrimidin-1-yl)oxolane-2-carboxamide结构式

3-hydroxy-N-[2-...

乙二胺结构式

异氰酸甲酯结构式

异氰酸甲酯

~59%

3-methyl-1-[2-(methylcarbamoylamino)ethyl]urea结构式

3-methyl-1-[2-(...

1-(2-aminoethyl)-3-methylurea结构式

1-(2-aminoethyl...

1-(2-aminoethyl)-3-methylurea结构式

1-(2-aminoethyl...

b-D-Ribofuranuronic acid,1-deoxy-1-(1,6-dihydro-6-oxo-9H-purin-9-yl)-结构式

b-D-Ribofuranur...

~79%

3,4-dihydroxy-N-[2-(methylcarbamoylamino)ethyl]-5-(6-oxo-3H-purin-9-yl)oxolane-2-carboxamide结构式

3,4-dihydroxy-N...