ライフサイエンスコーパス: phosphoramidate

1 with ammonium hydroxide to form the desired phosphoramidate.

2 ation steps to obtain pure ammonium hydrogen phosphoramidate.

3 l phosphate, 2-methoxybenzoyl phosphate, and phosphoramidate.

4 r to that of the corresponding beta-anomeric phosphoramidate.

5 nophosphoimidazole and pH 7.8 (midpoint) for phosphoramidate.

6 described phosphodonors acetyl phosphate and phosphoramidate.

7 oavailability of the corresponding monoester phosphoramidate.

8 Both CPSs were shown to carry O-methyl-phosphoramidate.

9 hat can be directly transformed into allylic phosphoramidates.

10 de linkages as N, N -diethylethylene-diamine phosphoramidates.

11 strands, as well as with 2'-deoxy N3'-->P5' phosphoramidates.

12 n and phosphorus, leading to cyclic P-chiral phosphoramidates.

13 lly similar 3'-azido-3'-deoxythymidine (AZT) phosphoramidates 1-6 and 3'-fluoro-3'-deoxythymidine (FL

14 Phosphoramidate (1) and its fluorobenzamido conjugate (2

15 )hydroxyphosphorylamino) -pentanedioic acid (Phosphoramidate (1)), yielding S-2-((2-(S-4-(4-(18)F-flu

16 estinal microsomes and liver microsomes make phosphoramidate 16 a prospective candidate for further s

17 Phosphoramidate 16 in its 5'-triphosphate form specifica

18 Studies on the intracellular half-life of phosphoramidate 16-TP in live cells demonstrated favorab

19 Phosphoramidates (18-21) achieved a significant improvem

20 The results obtained with hypoxallene phosphoramidates 2b and 4b indicate that the aminosuccin

21 (18)F-labeled phosphoramidate (3) is a representative of a new class o

22 In general, hHint3s hydrolyze phosphoramidate 370- to 2000-fold less efficiently than

23 es 1-6 and 3'-fluoro-3'-deoxythymidine (FLT) phosphoramidates 7-10 are reported.

24 of a duplex formed by a 13mer ribo-N3'-->P5' phosphoramidate (84 degrees C) was higher than that obse

25 the two AZT aromatic amino acid methyl ester phosphoramidates 8a and 9a were found to be more cytotox

26 tions as high as 100 microM, whereas the FLT phosphoramidates 9 and 10 had CC50 values of 95.6 and 35

27 rate constants (kphos/KS) for reaction with phosphoramidate, acetyl phosphate, or monophosphoimidazo

28 The RNA phosphoramidates also showed similar rates of hydrolysis

29 We find that TFOs containing N3'-->P5' phosphoramidate (amidate), 5-(1-propynyl)-2'-deoxyuridin

30 ate, ADP.Mg(2+).phosphopantothenate, and AMP phosphoramidate (AMPPN).Mg(2+), revealed a large conform

31 Primer extensions with phosphoramidate analogs of dNTPs allowed for unambiguous

32 Piperidyl phosphoramidate analogues are also converted to nucleoti

33 Synthetic phosphoramidate analogues of nucleosides have been used

34 On the basis of these data, a series of phosphoramidate analogues with structural variation in t

35 phorus bond in both monophosphoimidazole and phosphoramidate and implied that CheY was not capable of

36 re unaffected by pH over this range, whereas phosphoramidate and monophosphoimidazole showed a steep

37 ith acetyl phosphate and faster (4-14x) with phosphoramidate and monophosphoimidazole.

38 orylation rate, especially for reaction with phosphoramidate and monophosphoimidazole.

39 Both phosphoramidate and phosphorothioate oligonucleotides we

40 Hydrolysis of N3'-P5' phosphoramidate and thiophosphoramidate oligonucleotides

41 droxamate by synthesizing a small library of phosphoramidates and evaluating their biological activit

42 Hint1 catalyzes the hydrolysis of purine phosphoramidates and lysyl-adenylate generated by lysyl-

43 several different deoxyguanosine nucleotide phosphoramidates and phosphomonoesters were synthesized

44 ese compounds relative to the beta-N3'-->P5' phosphoramidates and to the alpha-phosphodiester counter

45 honate, pinacolyl methylphosphonate, diethyl phosphoramidate, and 2-(butylamino)ethanethiol) and one

46 sphonate, diethyl ethyl phosphonate, diethyl phosphoramidate, and diethyl phthalate using laser fluen

47 s suggest that the oligonucleotide N3'-->P5' phosphoramidates, and particularly thio-phosphoramidates

48 Generation of the phosphoramidate anion leads to cyclization and subsequen

49 release of nucleotide via cyclization of the phosphoramidate anion to the aziridinium ion intermediat

50 ndergoes intracellular activation liberating phosphoramidate anion, which undergoes spontaneous cycli

51 racellularly with concomitant expulsion of a phosphoramidate anion.

52 )P NMR kinetics demonstrated that all of the phosphoramidate anions cyclized to the aziridinium ion a

53 led to rapid expulsion of the corresponding phosphoramidate anions in both series of compounds.

54 essed the inhibitory potential of morpholino phosphoramidate antisense oligonucleotides (morpholinos)

55 uniformly modified oligonucleotide N3'-->P5' phosphoramidates are apparently more potent antisense ag

56 Phosphoramidates are modified deoxyoligonucleotides that

57 In addition to their inherent value, the phosphoramidates are precursors to enantioenriched epoxy

58 Oligodeoxynucleotide N3'-->P5' phosphoramidates are promising candidates for antisense

59 RNA mimetics, oligoribonucleotide N3'-->P5' phosphoramidates, are described.

60 -anomeric oligodeoxyribonucleotide N3'-->P5' phosphoramidates, are described.

61 The present study uses N3'-phosphoramidate as a control to understand the changes i

62 The motivation of this work is to explore phosphoramidates as a new class of potent PSMA inhibitor

63 enzymes preferred guanosine versus adenosine phosphoramidates as substrates.

64 evaluated several oligonucleotide N3'-->P5' phosphoramidates as telomerase inhibitors.

65 C-myb antisense phosphoramidates at 5 microM caused sequence and dose-de

66 iously uncharacterized properties of the N3'-phosphoramidate backbone are also observed and explained

67 DNA-RNA molecules, both with and without the phosphoramidate backbone modifications, we show that the

68 hosphates has been developed that utilizes a phosphoramidate-based prodrug approach.

69 intracellular delivery of nucleotides using phosphoramidate-based prodrugs is described.

70 A series of phosphoramidate-based prostate specific membrane antigen

71 A series of thymidine and tetrahydrofurfuryl phosphoramidates bearing haloethyl or piperidyl substitu

72 onate (AmNS) to the terminal phosphate via a phosphoramidate bond.

73 C), extending the donor by one residue via a phosphoramidate bond.

74 rtate alpha-carboxyl group linked to AMP via phosphoramidate bond.

75 acid lability of the P( horizontal lineO)-N phosphoramidate bond.

76 e but resistant to alkali, consistent with a phosphoramidate bond.

77 ntaining acid-labile internucleotide P3'-N5' phosphoramidate bonds, either in a surface-bound form or

78 e phosphodonors such as acetyl phosphate and phosphoramidate, but it is phosphorylated by the cognate

79 int3-2 prefer AIPA over tryptamine adenosine phosphoramidate by factors of 33- and 16-fold, respectiv

80 ver, gel shift assays demonstrate that these phosphoramidates can specifically bind to peptides deriv

81 Herein, we describe the application of phosphoramidate chemistry to 1,3,4-O-acetylated N-acetyl

82 C) than that for the isosequential 2'-deoxy phosphoramidate complex.

83 Phosphoramidates composed of an amino acid and a nucleot

84 P NMR studies carried out on model haloethyl phosphoramidates confirm the release of nucleotide via c

85 ormly modified oligoribonucleotide N3'-->P5' phosphoramidates containing all four natural bases (urac

86 ec chimera does not exhibit a preference for phosphoramidates containing d- or l- tryptophan, while t

87 sults suggest that the lipid-conjugated thio-phosphoramidates could be important for improved pharmac

88 data indicate that oligonucleotide N3'-->P5' phosphoramidates could be used as specific and efficient

89 .0 degrees C), or for the 2'-deoxy-N3'-->P5' phosphoramidate counterpart (71.7 degrees C).

90 degrees C relative to the 2'-deoxy N3'-->P5' phosphoramidate counterpart.

91 han that for the corresponding beta-anomeric phosphoramidate counterpart.

92 Thus the N3'-->P5' phosphoramidate decamer containing only alpha-thymidine

93 f NarLN by a small-molecule phosphate donor, phosphoramidate, decreases this interaction about 25-fol

94 er, d(AnTnGnAnCn)rU, contains an N3' --> P5' phosphoramidate deoxysugar-phosphate backbone (n) that i

95 TS are preferentially sensitive to NB1011, a phosphoramidate derivative of (E)-5-(2-bromovinyl)-2'-de

96 X4430, an imino-C-nucleoside, and GS-6620, a phosphoramidate derivative of 1'-cyano-2'-C-methyl-4-aza

97 In addition, after oral dosing of several phosphoramidate derivatives of compound 21 to rats, subs

98 Moreover, tissue distribution of the phosphoramidate derivatives was undistinguishable from t

99 However, s-BuLi converted the dimethyl N-Boc-phosphoramidate derived from 1-phenylethylamine to the N

100 LiTMP metalated dimethyl N-Boc-phosphoramidates derived from 1-phenylethylamine and 1,2

101 actions of a variety of amino acids with the phosphoramidates derived from oligonucleotide 5'-phospha

102 ved for these prodrugs, but the intermediate phosphoramidate dianion underwent spontaneous hydrolysis

103 , we evaluate the impact of HCV-NS5B prodrug phosphoramidate diastereochemistry (D-/L-alanine, R-/S-p

104 , the discovery of beta-d-2'-Br,2'-F-uridine phosphoramidate diastereomers 27 and 28, as nontoxic pan

105 phoramidate monoester and positively charged phosphoramidate diester groups were synthesized.

106 amidate monoesters are distinct from that of phosphoramidate diesters.

107 ethod.1H NMR analysis of the alpha-N3'-->P5' phosphoramidate dimer structures indicates significant d

108 Poly(phosphoramidate-dipropylamine) (PPA) and Lipid-Protamine

109 we describe the synthesis of N3'-P5'-linked phosphoramidate DNA (3'-NP-DNA) by the template-directed

110 N3'-P5'-linked phosphoramidate DNA (3'-NP-DNA) is similar to RNA in its

111 a complementary strand composed of N3'->P5' phosphoramidate DNA (3'-NP-DNA) using 3'-amino-2',3'-did

112 structural and biochemical properties of N3'-phosphoramidate DNA analogs have been re-examined using

113 The N3'-phosphoramidate DNA backbone differs from the phosphodie

114 Solvation of N3'-phosphoramidate DNA is shown to be similar to RNA, consi

115 template copying and suggest that N2'-->P5'-phosphoramidate DNA may have the potential to function a

116 titution was performed via comparison of N3'-phosphoramidate DNA starting from both A- and B-form str

117 e-directed solid-phase syntheses for RNA and phosphoramidate DNA.

118 We now report that oligonucleotide N3'-->P5' phosphoramidates DNA analogs of HIV-1 RRE IIB and TAR RN

119 The tight binding of the phosphoramidate duplex under metal-free conditions and i

120 reased chemical shift dispersion in the free phosphoramidate duplex, the spectrum of the enzyme-bound

121 The AZT phosphoramidates exhibited no cytotoxicity toward CEM ce

122 A series of novel haloethyl and piperidyl phosphoramidate FdUMP prodrug analogues has been synthes

123 was 5-14 degrees C relative to the 2'-deoxy phosphoramidates for decanucleotides.

124 des and derivatives thereof, including their phosphoramidates, for their therapeutic potential in the

125 experiments demonstrated that ribo-N3'-->P5' phosphoramidates form stable duplexes with a complementa

126 thermore, the oligopyrimidine ribo N3'-->P5' phosphoramidate formed an extremely stable triplex with

127 The covalent linkage is a phosphoramidate formed between the UMP moiety and the Hi

128 n contrast, the alpha-decaadenylic N3'-->P5' phosphoramidate formed duplexes with both RNA and DNA co

129 0.5 microM of FuGENE6 formulated 13-mer thio-phosphoramidates, fully complementary to hTR, resulted i

130 analog in which the mesyl (methanesulfonyl) phosphoramidate group is substituted for the natural pho

131 A task specific ionic liquid (TSIL) bearing phosphoramidate group, viz., N-propyl(diphenylphosphoram

132 ent method for the synthesis of radiolabeled phosphoramidate has not been developed, and this has lim

133 A series of novel nitroheterocyclic phosphoramidates has been evaluated for antitumor activi

134 A series of novel nitroheterocyclic phosphoramidates has been prepared, and the cytotoxicity

135 e boranophosphates and nucleoside amino acid phosphoramidates have been shown to be potent antiviral

136 well the carboxylate is poised to attack the phosphoramidate, helping to explain this reactivity.

137 able to cleave the native strand in a native:phosphoramidate heteroduplex at a rate comparable to tha

138 , which involves the formation of a covalent phosphoramidate histidine-DNA adduct for cell-to-cell tr

139 oxicity and DTD activity for the 2-series of phosphoramidates; however, there was no correlation betw

140 y Ala was shown to abolish the adenylate and phosphoramidate hydrolase activity for hHint3-1.

141 pared the aminoacyl-adenylate and nucleoside phosphoramidate hydrolase activity of hHint1 and Escheri

142 mical and structural bases for the adenosine phosphoramidate hydrolase activity of rabbit Hint, we sy

143 acts of CEM cells, further suggesting that a phosphoramidate hydrolase may be responsible for intrace

144 that hHint3-1 and hHint3-2 are adenylate and phosphoramidate hydrolases with apparent second-order ra

145 ilon-(N-alpha-acetyl lysine methyl ester) 5'-phosphoramidate) hydrolases related to the rabbit histid

146 We also report here the presence of O-methyl phosphoramidate in wild-type strain 81-176 capsular poly

147 he duplexes formed by the isosequential beta-phosphoramidates in antiparallel and parallel orientatio

148 cid-catalyzed hydrolysis of the newly formed phosphoramidates incorporates one oxygen atom from H2(16

149 perties of the oligoribonucleotide N3'-->P5' phosphoramidates indicate that these compounds can be us

150 The oligo-N3'-->P5' phosphoramidate inhibited telomerase activity in cells i

151 ster intermediate or formation of a circular phosphoramidate intermediate, using an internal RNA nitr

152 nucleoside residues and phosphorothioate and phosphoramidate internucleosidic linkages were synthesiz

153 These RNA analogs contain N3'-->P5' phosphoramidate internucleotide linkages which replaced

154 hanism of action of the piperidyl nucleoside phosphoramidates involves the intracellular release of t

155 observation is that the N3'-H moiety in N3'-phosphoramidate is a flexible moiety that can change the

156 lization of the C3'-endo conformation in N3'-phosphoramidate is primarily due to aqueous solvation ra

157 Activation of the benzotriazolyl piperidyl phosphoramidates is followed by P-N bond hydrolysis; thi

158 Hydrolysis of the phosphoramidate liberates the nucleotide, which can then

159 between iridium(III) and a 1,3-N,O-chelating phosphoramidate ligand has been used to develop a protoc

160 Pd(0)-systems modified with SPINOL-derived phosphoramidate ligands promote highly enantioselective

161 a "Trojan horse" antibiotic that contains a phosphoramidate linkage to adenosine monophosphate at it

162 -guanylyl intermediate that is most likely a phosphoramidate linkage to His(46).

163 ptide with a modified AMP attached through a phosphoramidate linkage to the alpha-carboxyl group of t

164 n of the normal phosphodiester of DNA into a phosphoramidate linkage yields a nucleic acid that behav

165 present study, GNA analogues with N2'-->P3' phosphoramidate linkages (npGNA) have been synthesized a

166 e 5' exon mimic with five internal N3'-->P5' phosphoramidate linkages binds 4-fold more tightly than

167 ies of oligonucleotides composed entirely of phosphoramidate linkages have been published, little is

168 phosphodiester bonds with positively-charged phosphoramidate linkages results in more efficient tripl

169 of the phosphodiester backbone with cationic phosphoramidate linkages, either N,N-diethylethylenediam

170 aminoribonucleosides connected via N3'-->P5' phosphoramidate linkages, replacing the native RNA O3'--

171 horothioate and of d(ATGAC)rU with N3'-->P5' phosphoramidate linkages.

172 ate for a self-replicating system based upon phosphoramidate linkages.

173 second, unique reaction, producing a stable phosphoramidate-linked analogue of acyl-adenylated aspar

174 hydrolyzes the naturally occurring aspartyl phosphoramidate McC7 and synthetic peptidyl sulfamoyl ad

175 dwide, produces a CPS with a unique O-methyl phosphoramidate (MeOPN) modification on specific sugar r

176 decorated nonstoichiometrically with methyl phosphoramidate (MeOPN).

177 nuclease-resistant oligonucleotide N3'-->P5' phosphoramidates might serve as RNA-like decoys and disr

178 >P5' phosphoramidates, and particularly thio-phosphoramidates, might be further developed as selectiv

179 are, and the pathway for the assembly of the phosphoramidate moiety in the CPS of C. jejuni is unknow

180 l-adenylate (AIPA) over tryptamine adenosine phosphoramidate monoester (TpAd).

181 ing alternating negatively charged N3'-->P5' phosphoramidate monoester and positively charged phospho

182 ociated with greater intracellular levels of phosphoramidate monoester and/or phosphorylated AZT.

183 as a substrate, but not tryptamine adenosine phosphoramidate monoester.

184 wed by enzymatic hydrolysis of the resulting phosphoramidate monoester.

185 is of the observed antiviral activity of AZT phosphoramidate monoesters 3a and 4a in PBMCs and CEM ce

186 y and intracellular metabolism of nucleoside phosphoramidate monoesters are distinct from that of pho

187 s and anticancer activity of a series of AZT phosphoramidate monoesters containing amino acid methyl

188 A series of phosphoramidate monoesters of 3'-azido-3'-deoxythymidine

189 The addition of a phosphoramidate motif to the gemcitabine can protect it

190 The phosphoramidate NH proton signal could be observed in DM

191 synthesis of radiolabeled ammonium hydrogen phosphoramidate [(NH(4))H(32)PO(3)NH(2)] which is achiev

192 stable oligonucleotides containing N3'->P5' phosphoramidate (NP) bonds, no such internucleotide link

193 N3'->P5' phosphoramidate (NP) DNA is defined by a conservative li

194 phodiester linker replaced by an N3' --> P5' phosphoramidate (NP) group have been used to establish a

195 the effect of oligonucleotide N3'-->P5' thio-phosphoramidate (NP), which targets template RNA compone

196 Using oligonucleotide N3'-->P5' phosphoramidates (NPs) we have identified a region of th

197 the discovery of a beta-d-2'-Cl,2'-F-uridine phosphoramidate nucleotide 16, as a nontoxic pan-genotyp

198 clic phosphate nucleotide, and PSI-353661, a phosphoramidate nucleotide, are prodrugs of beta-D-2'-de

199 The phenylmethoxyalaninyl phosphoramidate of abacavir was prepared in good yield i

200 illonite-catalyzed oligomerization of the 5'-phosphoramidate of adenosine are discussed.

201 Also prepared was the corresponding phosphoramidate of the guanine nucleoside analogue "carb

202 illonite-catalyzed oligomerization of the 5'-phosphoramidates of adenosine are investigated.

203 n reactions of the adenine derivatives of 5'-phosphoramidates of adenosine on montmorillonite are inv

204 Phosphoramidates of proline hydrolyzed fast, with a half

205 ed the rate of enzyme-free hydrolysis for 17 phosphoramidates of ribonucleotides with amino acids or

206 purification of uniformly modified N3'-->P5' phosphoramidate oligodeoxy-nucleotides, as well as their

207 A 22-nt anti-miR-21 mesyl phosphoramidate oligodeoxynucleotide specifically decrea

208 ow here that a lipid-modified N3'-->P5' thio-phosphoramidate oligonucleotide (GRN163L) inhibits telom

209 ifferences in the properties of N3'- and N5'-phosphoramidate oligonucleotide analogs.

210 Collectively, these studies suggest that phosphoramidate oligonucleotides can serve as potent and

211 les rapid sequence confirmation of synthetic phosphoramidate oligonucleotides for quality control as

212 n of RNase H are the key advantages of mesyl phosphoramidate oligonucleotides, which may represent a

213 ated systemically with equal doses of either phosphoramidate or phosphorothioate c-myc antisense or m

214 Recently a new type of modified mesyl phosphoramidate (or u-) oligonucleotide was described th

215 between the N3 of A2451 and the nonbridging phosphoramidate oxygen by using chemical protection and

216 A) between the A2451 N3 and the nonbridging phosphoramidate oxygen of CCdApPmn suggested that the ca

217 -specific antibodies and the lability of the phosphoramidate (P-N) bond.

218 The mode of inhibition for phosphoramidate peptidomimetic inhibitors of prostate-sp

219 rmed by the all anionic alternating N3'-->P5'phosphoramidate-phosphodiester oligothymidylate and poly

220 All the phosphoramidates prepared were L-alanine derivatives wit

221 ene-carbocyclic adenosine (FMCA, 12) and its phosphoramidate prodrug (FMCAP, 14) have been proven as

222 6-diaminopurine nucleosides (DAPNs) to their phosphoramidate prodrug (PD) substantially blocks the co

223 displays a superior profile compared to its phosphoramidate prodrug analogues (e.g., 4) described pr

224 Remdesivir is a phosphoramidate prodrug and is known to target viral RNA

225 Thus, phosphoramidate prodrug derivatives of the monophosphate

226 citabine (2',2'-difluorodeoxycytidine, dFdC) phosphoramidate prodrug designed for the intracellular d

227 nine isopropyl ester (13) with FMCA gave its phosphoramidate prodrug FMCAP (14) in good yield.

228 A novel nitroheterocyclic bis(haloethyl)phosphoramidate prodrug linked through lysine to a ptero

229 A phosphoramidate prodrug of 2'-deoxy-2'-alpha-fluoro-beta

230 for the first time the stereochemistry of a phosphoramidate prodrug with biological activity.

231 Phosphoramidate prodrugs (8-10) of phosphate-containing

232 vitro evaluation of 5-fluoro-2'-deoxyuridine phosphoramidate prodrugs 2a and 3b against L1210 mouse l

233 We have synthesized a series of gemcitabine phosphoramidate prodrugs and screened for cytostatic act

234 Phosphoramidate prodrugs are a critical component of pro

235 These phosphoramidate prodrugs contain an ester group that und

236 Chemical reduction of the phosphoramidate prodrugs led to rapid expulsion of the c

237 We found that phosphoramidate prodrugs of 2'-deoxy-2'-spirooxetane rib

238 further extended the development of the aryl phosphoramidate prodrugs of 2,3-O-isopropylidene-4-eryth

239 Phosphoramidate prodrugs of a 2'-oxetane 2-amino-6-O-met

240 Phosphoramidate prodrugs of the 5'-phosphate derivative

241 Specifically, we have developed phosphoramidate prodrugs of the anticancer nucleotide 5-

242 The most potent phosphoramidate prodrugs of these compounds have IC50 va

243 series of 2- and 3-substituted indolequinone phosphoramidate prodrugs targeted to DT-diaphorase (DTD)

244 series of 2- and 3-substituted indolequinone phosphoramidate prodrugs was synthesized, and the compou

245 gate the activation mechanisms of nucleoside phosphoramidate prodrugs.

246 us to convert adenine derivative 1 into two phosphoramidate prodrugs.

247 rted racemic mixtures of chiral bioreductive phosphoramidate prodrugs.

248 We report the application of phosphoramidate pronucleotide (ProTide) technology to th

249 rase, raising the question as to whether our phosphoramidate ProTide approach could effectively deliv

250 We report the application of the phosphoramidate ProTide approach, developed by us for an

251 We herein report the application of phosphoramidate ProTide technology to bypass the rate-li

252 We report herein the application of the phosphoramidate ProTide technology to improve the metabo

253 We report the application of our phosphoramidate ProTide technology to the ribonucleoside

254 zidoadenosine (1) and the application of the phosphoramidate ProTide technology to this nucleoside.

255 irals as it offers many of the advantages of phosphoramidate ProTides but without the chirality issue

256 These results confirm that phosphoramidate ProTides can deliver monophosphates of r

257 rent nucleosides was compared to that of the phosphoramidate ProTides.

258 Conclusion: CTT1057 is a promising novel phosphoramidate PSMA-targeting (18)F-labeled PET radioph

259 Structural assignments for thymidine phosphoramidate reaction products were made by analogy t

260 8) was also carried out in the hope that the phosphoramidates released might be phosphatase-resistant

261 potent than the unsubstituted bis(haloethyl)phosphoramidate, respectively.

262 series of fluorogenic tryptamine nucleoside phosphoramidates revealed that hHint3-1 and hHint3-2 are

263 on of aminohexanoic acid (AH) linkers in the phosphoramidate scaffold improved their PSMA binding and

264 with a urea backbone, CTT1057 is based on a phosphoramidate scaffold that irreversibly binds to PSMA

265 The 5'-triphosphate formed from these phosphoramidates selectively inhibited HCV NS5B polymera

266 otently than its parental nonconjugated thio-phosphoramidate sequence (GRN163).

267 Phosphoramidate serves as a useful phosphodonor reagent

268 ay structure was determined establishing the phosphoramidate stereochemistry as Sp, thus correlating

269 Comparison of phosphodiester and phosphoramidate structures suggests that their backbones

270 Ca(II)-stimulated PvuII binding for a phosphoramidate-substituted oligonucleotide is comparabl

271 Oligonucleotide duplexes containing a phosphoramidate substitution at the scissile phosphates

272 onformational perturbation caused by the N5'-phosphoramidate substitution is identified and suggested

273 little is known about how singly substituted phosphoramidate substitutions affect the thermodynamics

274 drolysis of adenylylated and/or guanylylated phosphoramidate substrates by hinT.

275 racterized with respect to purine nucleoside phosphoramidate substrates.

276 er, that DNA analogs with modified N3'-->P5' phosphoramidate sugar-phosphate backbones are stable and

277 Results with a phosphoramidate tetramer and thiophosphoramidate hexamer

278 ly all the CheY variants reacted faster with phosphoramidate than acetyl phosphate.

279 10-400-fold less cytotoxic in vitro than the phosphoramidate that lacks the lysine-pteroyl moiety.

280 fied peptides release the positively charged phosphoramidate that via gas-phase intramolecular elimin

281 eloped to provide a library of Ac(3)ManNAc-6-phosphoramidates that were evaluated in a series of stud

282 The ability of zwitterionic phosphoramidates to form complexes with complementary DN

283 ility of the alpha-oligonucleotide N3'-->P5' phosphoramidates to form duplexes was studied using ther

284 r the installation of phosphorus-stereogenic phosphoramidates to nucleosides through a dynamic stereo

285 NUC-1031 (Acelarin), a phosphoramidate transformation of gemcitabine, was the f

286 day for 6 consecutive days), survival of the phosphoramidate-treated mice was significantly longer th

287 oceeds with a wide range of phosphonates and phosphoramidates under mild conditions and gives straigh

288 ized and used to prepare the oligonucleotide phosphoramidates using a solid phase methodology based o

289 phosphoserine peptides to the corresponding phosphoramidates, using 2-aminobenzylamine.

290 isosequential oligonucleotide N3'-->P5' thio-phosphoramidate was able to inhibit telomerase activity

291 osition of the abacavir phenylethoxyalaninyl phosphoramidate was evaluated in Cynomolgus monkeys.

292 n HME50-5E cells by the oligonucleotide thio-phosphoramidates was also sequence specific.

293 AZT-MP and substantial amounts of either phosphoramidate were detected in PBMCs and CEM cells tre

294 Twenty-two phosphoramidates were prepared, including variations in

295 veral mixed base 9-13mer oligoribonucleotide phosphoramidates were synthesized with step-wise couplin

296 eactivity between N-aliphatic and N-aromatic phosphoramidates were verified by electrochemistry.

297 groups on phosphopeptides, are converted to phosphoramidates with carbodiimide assistance.

298 as converted to a series of 06 arylaminoacyl phosphoramidates with ester and amino acid variation.

299 ng peptides and their subsequent reaction to phosphoramidates with phosphite esters before they are c

300 stimulated up to 8-fold by the phosphodonor phosphoramidate, with stimulation again dependent on Asp