ライフサイエンスコーパス: prodrug

1 tically improved upon conjugation to a lipid prodrug.

2 arbamate bond was too stable to be used as a prodrug.

3 crocyclic esterase-cleavable (acyloxy)alkoxy prodrug.

4 s not cross-react with satraplatin, a Pt(IV) prodrug.

5 od) were achieved with the dodecanoate (C12) prodrug.

6 ical relevance, to validate the bioreductive prodrug.

7 sma membrane directly, like a small-molecule prodrug.

8 position of the exogenously administrated NO prodrug.

9 tration of the photorelease of an anticancer prodrug.

10 tion of the BBB and chemical modification of prodrugs.

11 ve enhancement in the cytotoxicity of Pt(IV) prodrugs.

12 ery to hypoxic regions by using bioreductive prodrugs.

13 y agent, leading to easy synthesis of hybrid prodrugs.

14 H-imidazole-based precursors of bioreductive prodrugs.

15 inal chemistry work in developing organic CO prodrugs.

16 s inhibitors of key metabolic pathways or as prodrugs.

17 evelop MMP-subtype-selective tumor-activated prodrugs.

18 subcellular components and the activation of prodrugs.

19 s, where the Pd-NP activated different model prodrugs.

20 tor (HIF-1) inhibitors and hypoxia-activated prodrugs.

21 stead hydrogen-bond assisted ring-closing to prodrugs.

22 ew class of donepezil-based "bio-oxidizable" prodrugs 1 designed to be converted into dual binding si

23 from Ac-gamma-Glu-gamma-secretase inhibitor prodrug 13a (gamma-GT-targeting and gamma-GCT-targeting)

24 from Ac-alpha-Glu-gamma-secretase inhibitor prodrug 15a (APA-targeting) accumulated in kidneys when

25 thesis of a set of pyrazolo[3,4-d]pyrimidine prodrugs (1a-8a and 9a-e) with higher aqueous solubility

26 Promisingly, whereas the selected prodrug 1r showed good permeability in the PAMPA-BBB mod

27 played high LD50 values in mice, making this prodrug 1r/drug 2r couple a good candidate for further i

28 5 can be fully loaded with doxorubicin (DOX) prodrug 2 via hetero-ternary complex formation to yield

29 HeLa cells than equimolar quantities of DOX prodrug 2.

30 ification of the corresponding phosphoramide prodrug (29) with an improved solubility and pharmacokin

31 ional esterase that is capable of activating prodrugs; (3) Mutations in PfPARE constitute a mechanism

32 Subsequently the toxicity of a selected prodrug (4) was investigated ex vivo using rat precision

33 studies demonstrated for the most promising prodrugs a better aqueous solubility, a favorable hydrol

34 repairs ICLs, are hypersensitive to most ABQ prodrugs, a phenotype exacerbated in cells also engineer

35 the bis((isopropoxycarbonyl)oxy)methyl ester prodrug (ACT-281959, 45).

36 lfonates (PAIB-SOs) that are antimicrotubule prodrugs activated by CYP1A1.

37 t a parasite esterase, PfPARE (P. falciparum Prodrug Activation and Resistance Esterase) is required

38 Longitudinal studies confirmed that prodrug activation by Pd-NP inhibits tumour growth, exte

39 etabolite of ifosfamide and does not require prodrug activation, thereby avoiding the generation of t

40 spare respiratory capacity are increased by prodrug administration.

41 The novel prodrug also induced T cell mediated leukemia cell lysis

42 ts indicate that some platinum(IV) cisplatin prodrugs, although cytotoxic, may not have the expected

43 The enhanced activity of the prodrug analog is due to its ability to bypass the pathw

44 lity of the use of dxG nucleoside or related prodrug analogs as selective inhibitors of Poltheta acti

45 cal application of putative TRPV4 antagonist prodrug analogs lowered IOP in glaucomatous mouse eyes a

46 rior profile compared to its phosphoramidate prodrug analogues (e.g., 4) described previously.

47 A set of phosphatase-stable, cell-permeable prodrug analogues inhibited cytokine-stimulated STAT6 ph

48 re a l-aspartic acid diisoamyl ester phenoxy prodrug and a l-phenylalanine propyl ester phosphonobisa

49 bination of an endochin-like quinolone (ELQ) prodrug and atovaquone.

50 gh levels of mature miR-34a from pre-miR-34a prodrug and consequently reduction of protein levels of

51 to develop a novel platinum(IV) oxaliplatin prodrug and incorporate it into a three-drug-conjugated

52 SK9 lowering by oral dosing of the candidate prodrug and quantification of the drug fraction delivere

53 of synthesis of N-benzylaminoferrocene-based prodrugs and demonstrate its applicability by preparing

54 do not function as TbNTR or TbCPR-activated prodrugs and do not promote DNA damage.

55 responding tris-pivaloyloxymethyl (tris-POM) prodrugs and examined their effects on BTN3A1.

56 ilar approach, we synthesized bisphosphonate prodrugs and found that they efficiently limit tumor cel

57 NP prodrugs relative to their small molecule prodrugs and native drug mechanisms of action.

58 eved in both dog and minipig using nalmefene prodrugs and that the pharmacokinetic profile of nalmefe

59 ynthesis of two series of indenoisoquinoline prodrugs, and it also reveals how substituents on the O-

60 vo ADME study of macrocyclic (acyloxy)alkoxy prodrugs, and it remains to be established if the modest

61 The application of the prodrug approach demonstrated to be a successful strateg

62 The ProTide technology is a prodrug approach developed for the efficient intracellul

63 e strategized to mask the polar groups via a prodrug approach, increasing the likelihood of passive o

64 Phosphoramidate prodrugs are a critical component of pronucleotide (ProT

65 RNAi prodrugs are modified, self-delivering short interfering

66 of modified nucleosides and their phosphate prodrugs as treatments for neurodegenerative diseases.

67 a profitable pharmacokinetic profile of the prodrug associated with a good efficacy.

68 , these data suggest that the macromolecular prodrug-based micelle formulation of SIM may have great

69 n-species (ROS)-responsive doxorubicin (DOX) prodrug, BDOX, in polymeric nanoparticles.

70 We found that this prodrug binds tightly to human platelets even after gel

71 sphate (HMBPP) or a synthetic cell-permeable prodrug, bis (pivaloyloxymethyl) (E)-4-hydroxy-3-methyl-

72 vir disoproxil fumarate (TDF), the tenofovir prodrug, but not with the tenofovir microbicide gel util

73 pharmacokinetics, we synthesized a series of prodrugs by masking its hydrophilic hydroxamate group.

74 d afforded a series of diversely substituted prodrugs by O-conjugation of the hydroxyguanidine moiety

75 lated with combretastatin A-4 (CA-4) and its prodrug CA-4P support the therapeutic value of compounds

76 ear physiological conditions, the persulfide prodrug can be activated by an esterase to generate a "h

77 The polyethylene glycol (PEG)-based prodrug can spontaneously self-assemble to form micelles

78 Such persulfide prodrugs can be used either as chemical tools to study p

79 Additionally, such prodrugs can easily be conjugated to another non-steroid

80 ates the effect of a novel simvastatin (SIM) prodrug (capable of delivering high doses to periodontit

81 were treated with three weekly doses of: 1) prodrug carrier alone (mPEG); 2) 0.5 mg SIM dose equival

82 t disulfide reduction is not responsible for prodrug cleavage unless 3-exo-tet intramolecular cycliza

83 Here, we generated a chimeric prodrug composed of a single-chain version of the variab

84 e charged functional groups according to the prodrug concept to regain intestinal and oral permeabili

85 upported by the identification of a suitable prodrug concept.

86 tory nanomicellar carrier that is based on a prodrug conjugate of PEG with NLG919, an indoleamine 2,3

87 riggers drug release from an Fe(II)-reactive prodrug conjugate.

88 oxicity evaluation of self-assembling hybrid prodrugs containing both camptothecin (CPT) and a capeci

89 Daun02 is a prodrug converted into Daunorubicin by ss-galactosidase.

90 e editing to introduce the gene encoding the prodrug-converting enzyme herpes simplex virus type 1 th

91 Therefore, bisphosphonate prodrugs could enhance the effectiveness of adoptive can

92 cinoma cell lines compared with the two homo-prodrugs (dCPT-Sup35 and dCap-Sup35) as well as free par

93 35) to yield three different self-assembling prodrugs (dCPT-Sup35, CPT-Cap-Sup35 and dCap-Sup35).

94 e local 1.5-mg doses of a macromolecular SIM prodrug decreases amount of experimental periodontitis b

95 We conclude that prodrug-delivered succinate bypasses CI and supports ele

96 TTA core-shell-structured prodrug delivery capsules that benefit from these proper

97 All prodrugs demonstrated improved antiplasmodial in vitro a

98 abolic conversion to UTP analog are L-ala,SP prodrug-dependent in cardiomyocytes.

99 t the efficacy of treatments involving these prodrugs depends heavily on identifying the correct trea

100 cations in the active field of anthracycline prodrug design and development.

101 This strategy represents an original prodrug design with a dual mode of action for HDAC inhib

102 ct in an o-hydroxydihydrocinnamic acid based prodrug design.

103 honooxymethyl derivative fostemsavir (35), a prodrug designed to address dissolution- and solubility-

104 Using the persulfide prodrugs developed in this study, the reactivity between

105 Much of the chemistry in prodrug development relies on the ability to mask an app

106 ignaling by administration of the adrenergic prodrug dipivefrin at reactivation increased the strengt

107 Such prodrugs directly release hydrogen sulfide without the i

108 Unexpectedly, the most promising prodrug displayed only moderately higher oral bioavailab

109 The ester and carbamate prodrugs displayed equivalent potency to those of the pr

110 This new approach complements available prodrugs/donors that directly deliver a single species,

111 nuclear platinum(II) compounds, platinum(IV) prodrugs, dual-threat agents, and photoactivatable plati

112 tency was enhanced >600-fold in the tris-POM prodrug (EC50 = 0.041 muM).

113 er, once illuminated with far-red light, the prodrug effectively killed SKOV-3 ovarian cancer cells t

114 ents demonstrated that only certain HCV-NS5B prodrugs elicit bradycardia when combined with amiodaron

115 mice using ELQ-271, ELQ-316, and the ELQ-316 prodrug, ELQ-334, demonstrated excellent growth inhibito

116 Together, tris-POM prodrugs enhance the cellular activity of phosphinophosp

117 , to receive isavuconazonium sulfate 372 mg (prodrug; equivalent to 200 mg isavuconazole; intravenous

118 The best compound, the (S)-FPMPA amidate prodrug, exerts anti-HIV-1 activity in TZM-bl and periph

119 Furthermore, a representative prodrug exhibited potent cardioprotective effects in a m

120 The generated prodrugs exhibited low cytotoxicity and satisfactory liv

121 While these dual moiety prodrugs exhibited rapid metabolism in mouse plasma, sev

122 improve the in vivo anticancer activity of a prodrug for nanocarrier delivery by unshielding the este

123 ic potential as H2O2-activatable antioxidant prodrug for the treatment of I/R injuries.

124 endrimers being limited to carriers to being prodrugs for intracellular delivery of ROS with the pote

125 Its prodrug form, selexipag, augmented GSIS and preserved is

126 Tenofovir alafenamide is a novel prodrug formulated to deliver the active metabolite to t

127 a multikilogram scale to produce a tetrazole prodrug fragment for a leading clinical candidate that p

128 Hypoxia-activated prodrugs (HAPs) are compounds designed to penetrate to h

129 A dual-action bone-targeting prodrug has been designed, synthesized, and evaluated fo

130 ment of phosphate and phosphonate nucleotide prodrugs has led to important drugs for hepatitis C and

131 al of sofosbuvir, a nucleoside monophosphate prodrug, highlighted the success to be had by employing

132 zwitterions are converted easily to polymer prodrugs, hydrogels, and other derivatives that establis

133 ty profiles of a novel bioengineered miR-34a prodrug in orthotopic OS xenograft tumor mouse model.

134 ala,SP + amiodarone effects, implicating the prodrugs in these effects.

135 redominantly responsible for activity of our prodrugs in vitro.

136 6-Thiopurine (6-TP) prodrugs include 6-thioguanine and azathioprine.

137 Co-applied with amiodarone, L-ala,SP prodrugs increased beating rate and decreased beat ampli

138 ntraperitoneal dosing of the clinically used prodrug irinotecan produces high initial and local conce

139 ue to the labile ester containing link, this prodrug is converted back into active colistin in vitro

140 Gd and gives rise to an enhancement when the prodrug is relatively hydrophilic.

141 This prodrug is stable in acid and human plasma media, but it

142 mg (as its intravenous or oral water-soluble prodrug, isavuconazonium sulfate) three times daily for

143 The lead prodrug, isopropyl 6-diazo-5-oxo-2-(((phenyl(pivaloyloxy

144 c gene cluster that codes for small molecule prodrugs known as precolibactins.

145 result, the in vivo application of phosphate prodrugs led to a substantially increased Cmax and prolo

146 HNPs promoted linker breakdown resulting in prodrug liberation.

147 As potential copper prodrugs, ligand-copper complexes were examined in a cel

148 provide insights into how hypoxia-activated prodrugs may be used to enhance therapeutic effectivenes

149 Prodrug-mediated utilization of the cytochrome P450 (CYP

150 , an observation attributable to inefficient prodrug metabolism which was found to be CYP3A4-dependen

151 psin A (CatA) inhibitors attenuated L-ala,SP prodrug metabolite formation, yet exacerbated L-ala,SP +

152 This redox-responsive prodrug micellar system provides an attractive strategy

153 a H2O2-responsive camptothecin (CPT) polymer prodrug micelle, which endowed the nanocarriers with sel

154 s facilitated efficient cleavage of DAS from prodrug micelles in tumor cells/tissues, leading to a hi

155 beta-Lap-dC3 prodrug micelles provide a promising strategy for NQO1-t

156 In addition, we anticipate that the prodrug Mipsagargin, which is currently in late-stage cl

157 allowed a controlled stepwise removal of the prodrug moieties to achieve a highly selective delivery

158 yl or a benzoylbenzyl group as bioreversible prodrug moieties were studied.

159 ssion in the system activates the anticancer prodrug molecules and shows effective tumor growth inhib

160 mphiphilic polymers encapsulating anticancer prodrug molecules as the shell.

161 he synthesis of polymer-drug conjugates from prodrug monomers consisting of a cyclic polymerizable gr

162 For therapeutic efficacy, the prodrug must hydrolyze to its parent drug after administ

163 e prepared from a biodegradable polycationic prodrug, named DSS-BEN, which was synthesized from a pol

164 onto PTX at the 7-OH position, forming ester prodrugs: o(LA)8-PTX and o(LA)16-PTX, respectively.

165 An ester prodrug of 3i was the most efficient derivative in achie

166 mall molecule GS-5734, a monophosphoramidate prodrug of an adenosine analogue, with antiviral activit

167 GS-5734 is a monophosphate prodrug of an adenosine nucleoside analog that showed th

168 e report the design and synthesis of a novel prodrug of aspirin, [6]-gingerol aspirinate (GAS).

169 Evofosfamide is a hypoxia-activated prodrug of bromo-isophosphoramide mustard.

170 The lipid-conjugated prodrug of cidofovir, brincidofovir, has improved oral b

171 Colistin methanesulfonate (CMS) is the only prodrug of colistin available for clinical use for the t

172 (+/-)-MRJF22 [(+/-)-2], a novel prodrug of haloperidol metabolite II (sigma-1 receptor a

173 Sacubitril is an ethyl ester prodrug of LBQ657, the active neprilysin (NEP) inhibitor

174 s, we prepared the far-red light-activatable prodrug of PTX by conjugating photosensitizer via single

175 We developed a prodrug of SAHA by appending a promoiety, sensitive to t

176 Salsalate is a prodrug of salicylate that lowers blood glucose in patie

177 In this study, an amphiphilic macromolecular prodrug of SIM was designed and synthesized to overcome

178 Tenofovir alafenamide fumarate (TAF), a new prodrug of tenofovir and a potential successor of tenofo

179 Tenofovir alafenamide (TAF) is a novel prodrug of tenofovir that efficiently delivers tenofovir

180 and Tenofovir alafenamide (TAF), an improved prodrug of TFV, interfere with wound healing in the huma

181 A disodium phosphonooxymethyl prodrug of the antitumor agent triptolide was prepared f

182 (DHED), a novel brain-targeting bioprecursor prodrug of the main human estrogen, 17beta-estradiol, al

183 This system contains SN-38-a prodrug of the topoisomerase I inhibitor irinotecan.

184 developed a liposomal delivery system for a prodrug of vinblastine (CPD100) which converts to the pa

185 st potent attachment inhibitor BMS-626529, a prodrug of which is currently undergoing phase III clini

186 l substituted N-(pivaloyloxy)alkoxy-carbonyl prodrugs of 14 designed to circulate inert in plasma and

187 Ester and carbamate prodrugs of aldehyde bisulfite adduct inhibitors were sy

188 Phosphate and amino acid prodrugs of both 78b and 90b were synthesized, of which

189 However, developing organic prodrugs of gasotransmitters represent unique challenges

190 phosphonomonoamidate and phosphonobisamidate prodrugs of PMDTA led to a boost in antiviral potency.

191 ere we describe that cell membrane-permeable prodrugs of the complex II substrate succinate increase

192 The most potent phosphoramidate prodrugs of these compounds have IC50 values in the low

193 preparation of a variety of potential ester prodrugs of these two compounds.

194 e ester bond and also facilitate loading the prodrug on gold nanorod (AuNR)-encapsulated graphitic na

195 owever, whether PDM functions as an inactive prodrug or has pharmacological activity on its own remai

196 ity is a general feature of this category of prodrugs or not.

197 omarker for tumor responses to dCK-dependent prodrugs or small-molecule dCK inhibitors, respectively.

198 ive biomarker for responses to dCK-dependent prodrugs or small-molecule dCK inhibitors.

199 e.g. polymer-drug conjugates, small molecule prodrugs, or drug amphiphiles) could involuntarily aggre

200 The antischistosomal prodrug oxamniquine is activated by a sulfotransferase (

201 nucleosides (DAPNs) to their phosphoramidate prodrug (PD) substantially blocks the conversion to the

202 Glucose-based prodrugs performed particularly well and delivered cellu

203 is study, we evaluate the impact of HCV-NS5B prodrug phosphoramidate diastereochemistry (D-/L-alanine

204 ionic liquid moieties are a simple, scalable prodrug platform for treating skin disease.

205 Two novel prodrug polymers POEG-b-PSSDas (redox-sensitive) and POE

206 d demand of one metric ton per annum for the prodrug, provides a compelling mandate to develop practi

207 utilize to synthesize the anti-inflammatory prodrug pyrene-aspirin (P-aspirin) with a cleavable este

208 chanism of action of multidrug-conjugated NP prodrugs relative to their small molecule prodrugs and n

209 Colibactin biosynthesis involves a prodrug resistance strategy where an N-terminal prodrug

210 Tenofovir alafenamide, a tenofovir prodrug, results in 90% lower tenofovir plasma concentra

211 Notably, the pyrimidine containing prodrug (S)-Asp-FPMPC is the only congener within this s

212 ocker valsartan and the neprilysin inhibitor prodrug sacubitril in a 1:1 ratio in a sodium supramolec

213 drug resistance strategy where an N-terminal prodrug scaffold (precolibactin) is assembled, transport

214 doximod (IND), to a phospholipid that allows prodrug self-assembly into nanovesicles or incorporation

215 Notably, the hybrid CPT-Cap prodrug showed a synergistic effect and significantly en

216 This type of H2 S prodrugs shows great potential as both research tools an

217 Highly purified pre-miR-34a prodrug significantly inhibited the proliferation of hum

218 tration of in vivo-jetPEI formulated miR-34a prodrug significantly reduced OS tumor growth in orthoto

219 n of vehicles and activation of bioreductive prodrugs simultaneously.

220 We demonstrate for the first time that RNAi prodrugs (siRNNs) targeting Plk1, can enter pediatric T-

221 a following coadministration of the HCV-NS5B prodrug sofosbuvir with amiodarone was recently reported

222 they try to improve analog efficacy through prodrug strategies and drug combinations.

223 may further advance the development of other prodrug strategies for nucleosides, peptides, and beyond

224 , numerous monophosphate and monophosphonate prodrug strategies have been developed and applied in th

225 Prodrug strategies have been proven to be a very effecti

226 model substrate, we hybridized two disparate prodrug strategies to afford novel reduction-sensitive l

227 ystems, lipid-based formulations, as well as prodrug strategies.

228 ar Diels-Alder reaction, we have developed a prodrug strategy for preparations of organic CO prodrugs

229 hance DON's therapeutic index, we utilized a prodrug strategy to increase its brain delivery and limi

230 poorly permeable zwitterions was achieved by prodrugs susceptible to cleavage by carboxylesterase 1.

231 The effectiveness of the CO prodrug system in delivering a sufficient quantity of CO

232 -side evaluation and screening of the enzyme/prodrug systems at the preclinical level.

233 l line which is sensitive to all four enzyme/prodrug systems.

234 ted the success to be had by employing these prodrug technologies in the discovery of nucleotide ther

235 with renal and bone toxic effects; the novel prodrug tenofovir alafenamide achieves 90% lower plasma

236 The novel prodrug tenofovir alafenamide delivers the nucleotide re

237 The prodrug tenofovir alafenamide is associated with improve

238 lites are encoded by the clb gene cluster as prodrugs termed precolibactins.

239 arbonyloxymethyl (POC) ester 30 was the only prodrug that achieved substantial plasma levels of 1.

240 enylalanine propyl ester phosphonobisamidate prodrug that both display anti-HIV and anti-HBV activiti

241 Ours is the first PTX prodrug that can be activated by singlet oxygen using ti

242 Daun02 is an inactive prodrug that is converted to the inhibitory molecule dau

243 It is a prodrug that is rapidly converted to the active compound

244 Tenofovir alafenamide is a novel tenofovir prodrug that reduces tenofovir plasma concentrations by

245 Tenofovir alafenamide is a prodrug that reduces tenofovir plasma concentrations by

246 -302 is an investigational hypoxia-activated prodrug that releases the DNA alkylator bromo-isophospho

247 Here we show that ETC-1002 is a prodrug that requires activation by very long-chain acyl

248 PDM has been hypothesized to function as a prodrug that requires metabolism to the amphetamine-like

249 sbuvir (Sovaldi, SOF) is a nucleotide analog prodrug that targets the hepatitis C virus (HCV) nonstru

250 drug strategy for preparations of organic CO prodrugs that are stable during synthesis and storage, a

251 nucleoside monophosphate and monophosphonate prodrugs that can treat viral infections and cancer.

252 monophosphate and monophosphonate nucleoside prodrugs that entered clinical development, some of whic

253 Prodrugs that release hydrogen sulfide upon esterase-med

254 They are antitumor prodrugs that require cytochrome P450 bioactivation lead

255 cytochrome P450 reductase (TbCPR) dependent prodrugs that, following activation, generate metabolite

256 As a biological validation of the H2 S prodrugs, the anti-inflammatory effects of one such prod

257 In the case of NP-bound drugs, that is, NP-prodrugs, the current standard of practice is to assume

258 c drugs can be made into nanocarrier-encased prodrugs, the nanocarrier encasement must be boosted to

259 As with prodrugs, the nascent esters are substrates for endogeno

260 that emerge in patients receiving tenofovir prodrugs, the nonnucleoside reverse transcriptase inhibi

261 hanisms into a single self-assembling hybrid prodrug to construct self-deliverable nanomedicines for

262 ctionalized vascular graft that can catalyze prodrug to release NO locally and sustainably, indicatin

263 ed conjugate for targeting of bisphosphonate prodrugs to bone and slow release liberation of the acti

264 n enzyme that is capable of activating known prodrugs to their active form, which suggests a possible

265 ld domain and mediates the activation of the prodrug TP053, a thienopyrimidine derivative that kills

266 versatile, permitting the synthesis of many prodrug types with the ability to incorporate an additio

267 iazin-3-yl]ace tate (ETTA), a new anticancer prodrug, using adsorptive stripping voltammetry (AdSV) w

268 t HSV-2 suppressive therapy using ACV or its prodrug valacyclovir (valACV) reduced plasma HIV-1 viral

269 pt of the ability of the caspase-1 inhibitor prodrug VX-765 to mitigate alpha-syn pathology and to me

270 pancreatic adenocarcinoma cells, showed the prodrug was 4.3 times less cytotoxic than gemcitabine, b

271 Finally, the 4-4a couple of drug/prodrug was also evaluated in vivo, revealing a profitab

272 ults demonstrated that bioengineered miR-34a prodrug was effective to control OS tumor growth which i

273 The investigated prodrug was extracted from serum using SPE method.

274 lowing a single oral dose indicated that the prodrug was rapidly absorbed and converted to 1 with a t

275 the nontoxic, vinyl ether duocarmycin double prodrug was successfully decaged in live cells to reinst

276 The synthesis of select tetrazole prodrugs was crucial.

277 (HIV) activity of acyclovir (ACV) phosphate prodrugs, we herein report the ProTide approach applied

278 s, the anti-inflammatory effects of one such prodrug were examined by studying its ability to inhibit

279 t therapeutic doses of bioengineered miR-34a prodrug were well tolerated in these animals.

280 lymerization enhancement and cytotoxicity of prodrugs were dramatically reduced.

281 Prodrugs were evaluated for oral availability in mice an

282 Unexpectedly, simple alkyl ester-based prodrugs were ineffective due to chemical instability cy

283 tivation profile revealed that glucose-based prodrugs were more efficiently bioactivated than their g

284 Two homologous prodrugs were synthesized and displayed high solubilitie

285 A total of 39 new phosphate prodrugs were synthesized and evaluated against HIV-1 (i

286 population, a number of potential nalmefene prodrugs were synthesized with the aim of providing a fo

287 Many of the indenoisoquinoline prodrugs were very potent antiproliferative agents with

288 Herein we describe a PEGylated colistin prodrug whereby the PEG is attached via a cleavable link

289 2'-deoxy-2'-spirooxetane uridine nucleotide prodrugs which are known as inhibitors of the HCV NS5B R

290 evitalize the potential of disulfide-bearing prodrugs which have seen limited in vitro and in vivo su

291 Water-soluble platinum(IV) prodrugs, which proved kinetically stable to reduction i

292 and pharmacokinetic evaluation of phosphate prodrugs, which show an improved aqueous solubility of u

293 ng directed their conversion to phospholipid prodrugs, which were subsequently self-assembled to pro-

294 er, our data suggest a model wherein PL is a prodrug whose intracellular hydrolysis initiates the for

295 Here we describe RCB-185, a lipophilic prodrug with nanomolar activity against asexual parasite

296 Subsequently, para-acetoxybenzyl-based prodrugs with additional ester promoiety(ies) on carboxy

297 lagatran and dabigatran etexilat, are double prodrugs with low bioavailability in humans.

298 clusion, PAIB-SOs are novel chemotherapeutic prodrugs with no equivalent among current antineoplastic

299 Esterase- and phosphatase-sensitive H2S2 prodrugs with tunable release rates have been synthesize

300 The development of stable and bioavailable prodrugs would provide a pharmacologically valuable stra