ライフサイエンスコーパス: prodrug

1 DC1 were observed compared to ALDC3 and MMAE prodrug.

2 e of 1 and reduced levels of the circulating prodrug.

3 Fosmetpantotenate is an oral PPA prodrug.

4 on of tumor apoptosis by caspase-3 activated prodrug.

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

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

7 loads twenty-four paclitaxel molecules as a prodrug.

8 significant for the design of new antiviral prodrugs.

9 mplex mode of action of "multiaction" Pt(IV) prodrugs.

10 ic compounds and the metabolism of drugs and prodrugs.

11 cal release formulations of tenofovir or its prodrugs.

12 tiviral and antineoplastic nucleoside-analog prodrugs.

13 CLsu effectively modulates the properties of prodrugs.

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

15 n tumors compared to in situ albumin-binding prodrugs.

16 lamide (HPMA) to obtain 5 macromolecular Dex prodrugs.

17 k the first pharmacokinetic studies on these prodrugs.

18 om antibody-drug conjugates (ADCs) and caged prodrugs.

19 gether with its developed N-hydroxyguanidine prodrug 11, 8a will serve as a most widely applicable, p

20 Prodrug 12b showed rapid activation in a carboxylesteras

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

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

23 Our best prodrug 6 (isopropyl 2-(6-acetamido-2-(adamantane-1-carb

24 TML prodrug 9 provided superior in vivo performance, deliver

25 sphomethyl analog 2 and trimethyl-lock (TML) prodrug 9.

26 chieved through expression of a cytotoxic or prodrug-activating gene product in the cell type of inte

27 te the relationship between the chemistry of prodrug activation and HIV-1 inhibition for diverse praz

28 trategy, we have shown selective doxorubicin prodrug activation and instantaneous fluorescence imagin

29 Finally, CisPt-mediated prodrug activation of a propargyl derivative of 5-FU was

30 r-associated enzymes which are essential for prodrug activation usually limits the antitumor potency.

31 ntitumor efficacy by H(2)O(2) production and prodrug activation via combined oxidation-chemotherapy.

32 troduction of a methylene spacer facilitated prodrug activation, but parent exposure was lower than t

33 that a macrophage-targeted polyciprofloxacin prodrug acts as a surprisingly effective pre-exposure pr

34 stable RNA nanoparticles to deliver chemical prodrugs addresses issues with RNA unfolding and nanopar

35 ivity at submicromolar concentrations of the prodrugs against a panel of cancer cell lines, particula

36 ing on the lipophilicity of the TriPPPro-NTP prodrugs against HIV-1 and HIV-2 replication in cultures

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

38 Notably, these prodrugs also induce the expansion and activation of hum

39 llowing administration of simple alkyl ester prodrug and activated ester prodrug, respectively.

40 ng oral administration of simple alkyl ester prodrug and activated ester prodrug, respectively.

41 ulating a hydrolytically sensitive docetaxel prodrug and conjugated to an antibody specific for EphA2

42 e permeability to coload H(2)O(2)-responsive prodrug and GOD represent a novel strategy to realize pr

43 WR-2721 is a prodrug and is converted to its active metabolite, WR-10

44 Remdesivir is a phosphoramidate prodrug and is known to target viral RNA-dependent RNA p

45 The internal prodrug and SOS concentrations were optimized for their

46 s established to simulate PK profiles of the prodrug and the released PTX.

47 nly essential to develop customized inactive prodrugs and biocompatible metal catalysts but also the

48 CO prodrugs and their CO-released products were readily cle

49 rovide new insights into the binding mode of prodrugs and will assist the rational design of drugs wi

50 r prodrugs (e.g., camptothecin or paclitaxel prodrug) and hydrophilic glucose oxidase (GOD) in the me

51 ion enhancers such as alkanols, fatty acids, prodrugs, and vesicular delivery for steroids have been

52 Herein, we propose an advanced form of RIATC prodrug, AP1-DEVD-S-DOX, that could more actively target

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

54 the drug itself, demonstrating a successful prodrug approach to the oral delivery of 1.

55 A prodrug approach was deployed and proved effective in di

56 However, a combination of the lipophilic prodrug approach with lipid-based formulation resulted i

57 s work, we proposed a novel lipophilic ester prodrug approach, combined with oral lipid-based formula

58 beta-lactamase-producing bacteria using our prodrug approach, without adversely affecting bacteria t

59 Oligo(lactic acid) ester taxane prodrugs are in pre-clinical development as novel drug c

60 a result, acyl and oligo(lactic acid) ester prodrugs are less toxic and induce durable antitumor res

61 erted into bioreversibly modified lipophilic prodrugs at the gamma-phosphonate by the attachment of a

62 one (GSH)-activated photosensitizer, a chemo-prodrug based on combretastatin A-4 (CA4) with a singlet

63 In the present study, a prodrug-based nanocarrier delivery system was developed

64 Here, we demonstrate that NQO1-targeting prodrug beta-lapachone triggers tumor-selective innate s

65 or ASBT-targeting, including bile acid-based prodrugs, bile acid/drug electrostatic complexation and

66 of a protease-activated monoclonal antibody prodrug, called a Probody((R)) therapeutic, to tissue.

67 x vivo assays, we show that the designed CPT prodrug can be steadily released from its supramolecular

68 -concept is provided that nanoformulated RPV prodrugs can extend the apparent drug half-life and impr

69 Tumor-associated enzyme-activated prodrugs can potentially improve the selectivity of chem

70 ilitate further in vivo studies, a promising prodrug candidate for brain delivery was identified.

71 Subsequently, LPV and selected prodrug candidates were evaluated for their in vivo phar

72 Intravenous administration of a prodrug, chloramphenicol succinate (CLsu), is ineffectiv

73 the interplay among CO release kinetics, CO prodrug clearance, route of administration, and CO deliv

74 , we report our discovery and profile of the prodrug clinical compound, inhibitor 3, currently in pha

75 owing oral administration of activated ester prodrug compared to unmodified LPV.

76 upported by the identification of a suitable prodrug concept.

77 sign and synthesis of an amphiphilic polymer-prodrug conjugate of an imidazoquinoline TLR7/8 agonist

78 mpounds derived from colchicinoids including prodrugs, conjugates, and delivery systems.

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

80 ng with a patent survey on hypoxia-activated prodrugs containing nitro groups, are also covered.

81 Fast prodrug conversion of o(LA)(8)-PTX in vivo versus in vit

82 Unselected prodrug-converting activities were mostly unaffected, em

83 Notably, o(LA)(8)-PTX prodrug converts into PTX by a backbiting reaction in vi

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

85 hesized that liver-targeted delivery of 8-AQ prodrugs could maximize liver exposure and minimize eryt

86 tor agonist, that had not been designed as a prodrug, could prove pharmacologically active and contro

87 302) is a hypoxia-activated DNA-crosslinking prodrug currently in clinical development for cancer the

88 ProTides comprise an important class of prodrugs currently marketed and developed as antiviral a

89 Notably, acyl and oligo(lactic acid) taxane prodrugs delivered by PEG-b-PLA and PEG-b-PCL nano-assem

90 e applications to the development of a smart prodrug, delivering a highly cytotoxic chemotherapeutic

91 nd GOD represent a novel strategy to realize prodrug delivery and activation for enhanced therapeutic

92 ne permeability and structural stability for prodrug delivery and activation in diseased tissues.

93 SN22 prodrug delivery resulted in sustained intratumoral drug

94 CO prodrugs demonstrate promising pharmaceutical properties

95 Formulating antiretroviral prodrugs demonstrates improvements in cell and tissue ta

96 nistration and confirms incorporation of the prodrug-derived PPA into CoA.

97 We believe that the simplicity in prodrug design and the high efficacy in suppressing GBM

98 AA) rat model in order to identify the ideal prodrug design for the most effective and safe treatment

99 ated that the C3 hydrazone linker-containing prodrug design was the most effective in preserving join

100 e synthesized a series of tumor-targeted DON prodrugs designed to circulate inert in plasma and prefe

101 we report the synthesis of a library of RPV prodrugs designed to sustain drug plasma concentrations

102 trategy to address this problem based on LRA prodrugs, designed for controllable release of the activ

103 molecules and provide a template for further prodrug development.

104 the BRCA2-deficient DLD-1 colon cancer; the prodrug did not inhibit an isogenic DLD-1 tumor with wil

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

106 onjugating a diglycine (GG) to an antibiotic prodrug drastically accelerates intrabacterial ester-bon

107 ophobic phenylboronic ester-caged anticancer prodrugs (e.g., camptothecin or paclitaxel prodrug) and

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

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

110 rmulations examined had a high efficiency of prodrug encapsulation (as high as 114 mol% taxane per mo

111 LZ from a single safe, effective dose of the prodrug exceeded that of oral TLZ given daily over one m

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

113 As intended, these prodrugs exhibit comparable or superior in vitro activit

114 Visible and near IR-activatable prodrug, exhibiting the combined effects of PDT and loca

115 ging during the treatments revealed that the prodrug exhibits an intrinsic capability to prevent the

116 While the phosphate prodrug failed to release 1 in rats, the introduction of

117 ster (13) with FMCA gave its phosphoramidate prodrug FMCAP (14) in good yield.

118 adenosine (FMCA, 12) and its phosphoramidate prodrug (FMCAP, 14) have been proven as a potential anti

119 alpha-tocopherol to constitute an R848-Toco prodrug, followed by formulating with a tocopherol-modif

120 dingly, AP1-DEVD-S-DOX could be an efficient prodrug for concurrent chemoradiotherapy by selectively

121 We have synthesized a prodrug for PTX (7-OH), using oligo(lactic acid) as a no

122 After modification of these compounds into prodrugs for delivery into bacteria, we show that they k

123 A prodrug form is metabolized by cancer cells into an acti

124 gemcitabine (GEM), irinotecan (IRIN), and a prodrug form of 5-flurouracil (5FURW), paired with anoth

125 iscuss integrating the cancer specificity of prodrugs from classical chemotherapeutics and the potenc

126 ymidine promotes microbial conversion of the prodrug FUdR into toxic 5-fluorouridine-5'-monophosphate

127 transduced cells through treatment with the prodrug ganciclovir.

128 Hypoxia-activated prodrugs (HAPs) present a conceptually elegant approach

129 The macromolecular prodrug has no anesthetic effect itself unless irradiate

130 Remdesivir (GS-5734), a nucleoside analogue prodrug, has inhibitory effects on pathogenic animal and

131 cy and reduced toxicities, macromolecular GC prodrugs have been developed with promising outcomes for

132 une modulators, and antibody-directed enzyme prodrugs have been most extensively utilized as hematolo

133 injection, acyl and oligo(lactic acid) ester prodrugs have been synthesized for PEG-b-PLA and PEG-b-P

134 plantable devices and long-acting parenteral prodrugs have emerged which may provide more effective c

135 These prodrugs have good hydrolytic stability properties and i

136 These prodrugs have previously demonstrated efficacy in multip

137 and recurrence mouse model suggest that this prodrug hydrogel can release cancer therapeutics into br

138 ffective strategy for accelerating enzymatic prodrug hydrolysis and enhancing the antibacterial effic

139 Chemopreventive efficacy of oral curcumin: a prodrug hypothesis.

140 eptides to CLsu enhances the efficacy of the prodrugs; (ii) negative charges, high steric hindrance i

141 gineered ASCs in combination with irinotecan prodrug in the designed sequence and timeline eradicated

142 a rigid diester decreases the activities of prodrugs in comparison to CLsuGG; (iii) dipeptides appar

143 derstand the CO delivery efficiency of these prodrugs in relation to their efficacy, we undertook the

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

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

146 , the high exposure of TLZ released from the prodrug, increased tumor sensitivity upon continued expo

147 , which encodes the enzyme that converts the prodrug INH to its active form.

148 taken major efforts to identify neutral, non-prodrug inhibitors.

149 ing nanoplatforms to in situ transform inert prodrugs into active drugs.

150 les the rapid catalytic conversion of Pt(IV) prodrugs into their active Pt(II) counterparts, and driv

151 triggers in situ transformation of innocuous prodrugs into toxic parental drugs through cleavage of t

152 that the conjugation of GG to an antibiotic prodrug is an effective strategy for accelerating enzyma

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

154 hat the long-lasting antitumor effect of the prodrug is due to a combination of its long t (1/2), the

155 This new prodrug is effectively uncaged in cancer cell culture by

156 The prodrug is only bactericidal after activation by beta-la

157 tivation of relevant cancer chemotherapeutic prodrugs is of therapeutic relevance and noteworthy in p

158 ical and scalable synthesis of FMCA, and its prodrug, is reported via ketone 1.

159 with nifuroxazide (NFX) to self-assemble co-prodrug-loaded micelles (CLM).

160 The lead prodrug M3RPV was nanoformulated into the stable LA inje

161 A single dose of the polymeric prodrug maintained high lung drug levels and targeted an

162 Our results suggest that tenofovir prodrugs may be particularly effective as inhibitors of

163 Fine-tuning the activation kinetics of these prodrugs may further improve their therapeutic efficacy

164 gs including nucleoside analogs, such as the prodrugs mericitabine and sofosbuvir, which get metaboli

165 tic P450s and consequently enhanced drug and prodrug metabolism, a feature that could be therapeutica

166 knockout mice that were shown to mimic human prodrug metabolism, systemic administration of 6 deliver

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

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

169 e take a novel approach to produce a miR-127 prodrug (miR-127(PD)), which we demonstrate is processed

170 lloproteinase 9 (MMP9)-activated doxorubicin prodrug (MMP9-DOX-NPs) is developed.

171 The prodrug moiety is attached to a benzimidazole nitrogen a

172 ty to recognize amino acid and peptide-based prodrug molecules, thereby providing a rational approach

173 A successful strategy has been to develop prodrug molecules, which hijack solute carrier (SLC) tra

174 The prodrug monomers are synthetically incorporated into hom

175 rization was exploited to copolymerize these prodrug monomers with hepatocyte-targeting GalNAc monome

176 ides apparently increase the efficacy of the prodrugs most effectively; and so forth.

177 Another key finding is that prazole prodrugs must be activated inside the cell, while their

178 Here, we evaluate a unique prodrug/nanoparticle formation strategy to facilitate se

179 formation strategy to facilitate semi-solid prodrug nanoparticles (SSPNs) of the highly water-solubl

180 ration of the glycolytic inhibitor WP1122, a prodrug of 2-deoxy-d-glucose.

181 he combination of CB-839 and capecitabine, a prodrug of 5-FU, was well tolerated at biologically-acti

182 Herein, we designed an ester prodrug of 666-15 through a long-range O,N-acyl transfer

183 -101 (4-chlorokynurenine, 4-Cl-KYN), an oral prodrug of 7-chlorokynurenic acid (7-Cl-KYNA), an N-meth

184 e, we developed a multivalent, polymer-based prodrug of a structurally optimized camptothecin (SN22)

185 AL-794 is an orally active prodrug of ALS-033719, which selectively inhibits the en

186 Baloxavir marboxil (formerly S-033188) is a prodrug of baloxavir acid (S-033447) and inhibits cap-de

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

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

189 We synthesized previously a succinate ester prodrug of Cur, curcumin diethyl disuccinate (CurDD) wit

190 The ester prodrug of ETX1317, ETX0282, is orally bioavailable and,

191 Synthesis of a macromolecular prodrug of talazoparib (TLZ) was achieved by covalent co

192 Fostemsavir is the prodrug of temsavir, a first-in-class investigational HI

193 Fostemsavir, a prodrug of the first-in-class attachment inhibitor, tems

194 report that JHU-083, our recently developed prodrug of the glutaminase inhibitor 6-diazo-5-oxo-L-nor

195 ate that a single injection of a long-acting prodrug of the PARP inhibitor talazoparib in murine xeno

196 Recently, Minnelide, a water-soluble prodrug of triptolide, was shown to have potent antitumo

197 e introduce conjugation between platinum(IV) prodrugs of cisplatin and perfluoroaryl peptide macrocyc

198 More generally, selected prodrugs of PKC modulators avoid the bolus toxicities of

199 describe two new series of cyclic phosphate prodrugs of PPA capable of regenerating excellent levels

200 A research program to discover solubilizing prodrugs of the HCV NS5A inhibitor pibrentasvir (PIB) id

201 Phosphate and amino acid prodrugs of the HIV-1 protease inhibitor (PI) atazanavir

202 tivity against Dengue virus serotype 2 using prodrugs of the inhibitors was observed.

203 A series of acyloxybenzyl-prodrugs of these gamma-ketobenzyl nucleoside triphospha

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

205 The antischistosomal prodrug oxamniquine is activated by a sulfotransferase (

206 e, we design and synthesize a macromolecular prodrug (P407-CM-T) in which the local anesthetic tetrac

207 d biodistribution of SN22 as a polymer-based prodrug (PEG-[SN22](4)) compared with SN38 was determine

208 ting that all three components of the Pt(IV) prodrugs (platinum moiety and axial ligands) contribute

209 ed dissolution properties of these phosphate prodrugs provide them the potential to simplify drug dos

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

211 t pyrazinoic acid, the bioactive form of the prodrug pyrazinamide (PZA), interrupts biosynthesis of c

212 6-bromo-7-(11)C-methylpurine ((11)C-BMP), a prodrug radiotracer that is intracellularly conjugated w

213 that idebenone behaves as an NQO1-dependent prodrug, raising the possibility that lack of neuronal N

214 his 1,18-octadecanedioic acid-PTX (ODDA-PTX) prodrug readily forms a noncovalent complex with human s

215 However, the structural basis for prodrug recognition has remained elusive.

216 The valacyclovir structure reveals that prodrug recognition is mediated through both the amino a

217 ice led to slow and sustained release of the prodrug, reduced exposure of active docetaxel in the cir

218 olation (IVIVE) modelling predicts sustained prodrug release, with activation in relevant biological

219 sis reveals that bacteria treated with these prodrugs resemble those after conditional IspH knockdown

220 mple alkyl ester prodrug and activated ester prodrug, respectively.

221 mple alkyl ester prodrug and activated ester prodrug, respectively.

222 SN22 administered as a multivalent polymeric prodrug resulted in increased and protracted tumor drug

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

224 f a camptothecin (CPT)-based self-assembling prodrug (SAPD) hydrogel that can be used as an adjunct t

225 nt (wt%) and also are hydrophobized in these prodrug segments to drive depot formation upon injection

226 Lipidised analgesic peptide prodrugs self-assemble into peptide nanofibers; with the

227 0 mg taxane/kg, ephrin A2-targeted liposomal prodrug showed greater antitumor activity than 10 mg/kg

228 These prodrugs showed excellent stability in human serum (t(1/

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

230 yo-electron microscope images revealed dense prodrug-SOS complex in the aqueous core of the immunolip

231 persed in aqueous solution, the designed CPT prodrug spontaneously assembles into supramolecular fila

232 iretrovirals into lipophilic and hydrophobic prodrugs stabilized into biocompatible surfactants can p

233 Our results demonstrate that this prodrug strategy can be generalized to a variety of carb

234 vations offer promise that a tumor-activated prodrug strategy might exploit the essentiality of SCD f

235 This prodrug strategy targets a specific amidase, fatty acid

236 Herein is described a prodrug strategy that directs the biodistribution of par

237 leotide analogue are critical metabolites of prodrugs, such as remdesivir.

238 The depot is a polymeric prodrug synthesized from monomers that incorporate an AR

239 tion in beta-cells to develop a Zn(II)-based prodrug system to selectively and tracelessly deliver bi

240 poxia-activatable phototherapeutic polymeric prodrug system with a high potential for cancer therapy.

241 This prodrug system, with modular components that allow for f

242 to the metabolites of three different enzyme/prodrug systems were assessed, and the most effective on

243 th DTG combined with either of two tenofovir prodrugs (TAF and TDF) showed noninferior efficacy to tr

244 e (FTC) and DTG plus either of two tenofovir prodrugs - TAF (TAF-based group) or tenofovir disoproxil

245 n, chlorzoxazone, and acetaminophen) and the prodrug (tamoxifen) as P450 substrates, reveal that P450

246 ntravaginal ring that releases the tenofovir prodrug, tenofovir disoproxil fumarate, provided 100% pr

247 The active metabolite of tenofovir prodrugs, tenofovir-diphosphate, inhibited the incorpora

248 ell as their aryloxy diester phosphonamidate prodrugs, termed ProPAgens.

249 Treatment with hypoxia-activated prodrug TH-302 potently reduces NEPC tumor growth.

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

251 we describe the development of an antibiotic prodrug that combines ciprofloxacin with a beta-lactamas

252 vir is a broad-spectrum antiviral nucleotide prodrug that has been clinically evaluated in Ebola viru

253 nt analysis revealed that this compound is a prodrug that is bioactivated by the mycobacterial enzyme

254 ronide is an inflammation-responsive natural prodrug that is converted back to curcumin on demand at

255 e tumor and anticancer effect than the RIATC prodrug that lacks apoptotic cell-binding property but h

256 ribe the discovery of a glutamine antagonist prodrug that provides selective tumor exposure.

257 in (NKTR-214) is an engineered IL-2 cytokine prodrug that provides sustained activation of the IL-2 p

258 cently, we developed such a paclitaxel (PTX) prodrug that targets folate receptors.

259 long this line, we have developed organic CO prodrugs that allow for packing this gaseous molecule in

260 ert antineoplastic activity because they are prodrugs that are bioactivated in cancer-specific enviro

261 acylfuroxans can act as masked nitrile oxide prodrugs that inhibit GPX4 covalently with unique cellul

262 rs, yielding peptide epoxyketone-doxorubicin prodrugs that remained selective and active toward immun

263 ays, the excellent antiviral activity of the prodrugs that was found in CEM/0 cells was completely ke

264 therapy modality: exosome-directed catalyst prodrug therapy, whose first steps are presented herein

265 ced tumor cells, which could accumulate more prodrugs, thereby allowing more effective in situ activa

266 s optimized to a highly potent, neutral, non-prodrug thrombin inhibitor by designing, synthesizing, a

267 ted in the bioactivation of chemotherapeutic prodrugs through design and development of novel short-t

268 ) fusion protein as a liver-specific protein prodrug to achieve a glucose-lowering effect in type 1 d

269 tment based on the plasma/tumor ratio of the prodrug to achieve V-PDT (vascular targeted-PDT, 0.5 h),

270 onstrates the potential of this new class of prodrugs to deliver PPA to the brain following oral admi

271 We synthesized both paclitaxel and docetaxel prodrugs to formulate as ephrin A2-targeted liposomes st

272 Replenishment of GSH by its prodrugs treatment beneficially altered epigenetic enzym

273 The antitumor effects of the LIP-activated prodrug TRX-CBI, which releases the DNA alkylator CBI, w

274 Photochemical activation of the prodrug upon green light irradiation led to the photosub

275 n transporters in complex with the antiviral prodrug valacyclovir and the peptide-based photodynamic

276 esolution) and in complex with the antiviral prodrug valganciclovir (at 2.65 angstrom resolution) sup

277 ncluding BMS-626529, also called temsavir, a prodrug version of which is currently in phase III clini

278 ne and tafenoquine were first synthesized as prodrug vinyl monomers with self-immolative hydrolytic l

279 This study demonstrated that the prodrug was effective in three different models of hypox

280 The anti-tumor efficacy of the PTX prodrug was greatly influenced by the DLI.

281 The taxane prodrug was stabilized with extraliposomal citric acid a

282 A series of prodrugs was designed using an in-silico model for predi

283 of the parent, although the exposure of the prodrugs was high, reflecting good absorption.

284 The prodrugs we describe here synergize the direct killing o

285 tic index of current in situ albumin-binding prodrugs, we developed albumin-drug conjugates with a co

286 PK profiles of the prodrug were determined in key organs and a quantitative

287 both tumor and plasma concentrations of the prodrug were sufficient, showed the best antitumor effec

288 The prodrugs were activated inside the tumor, where they can

289 oliposomes incorporating pH-sensitive taxane prodrugs were developed for sustained delivery of active

290 The prodrugs were potent inhibitors of HIV-1/2 in cultures o

291 5FC acts as a prodrug, which is converted into toxic 5-fluorouracil (5

292 n summary, acyl and oligo(lactic acid) ester prodrugs widen the range of anticancer drugs that can be

293 emdesivir (GS-5734) is a nucleotide analogue prodrug with broad antiviral activity(1,2) that is curre

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

295 on in the past decades, only a single double prodrug with very modest oral bioavailability has reache

296 In doing so, we selected five representative prodrugs with different CO release kinetics and examined

297 yl) to prepare dual-action and triple-action prodrugs with known inhibitors of histone deacetylase, c

298 ition metal complexes offer photoactivatable prodrugs with novel targeted mechanisms of action.

299 chanisms may help to identify macromolecular prodrugs with the most potent therapeutic efficacy and s

300 in a reducing environment with these dimeric prodrugs, with the superior leaving group promoting more