ライフサイエンスコーパス: macrocyclization

1 a bioactive conformation by ring formation (macrocyclization).

2 the folding effect of the multicomponent Ugi macrocyclization.

3 hoice to fold synthetic peptides by means of macrocyclization.

4 ), followed by selective ruthenium-catalyzed macrocyclization.

5 ntification of an efficient strategy for the macrocyclization.

6 itical parameter defining the success of the macrocyclization.

7 The key reaction is a palladium-catalyzed macrocyclization.

8 mino acid oligomer intermediates followed by macrocyclization.

9 ving a highly advantageous Heck reaction for macrocyclization.

10 ons upon being subjected to depolymerization-macrocyclization.

11 action of the amide synthase responsible for macrocyclization.

12 his propensity to act as nucleophiles in the macrocyclization.

13 ides ideal candidates for the entropy-driven macrocyclization.

14 govern polyketide assembly, processing, and macrocyclization.

15 y the N-heterocyclic carbenes liberated upon macrocyclization.

16 p-tolerant, and stereoselective Prins-driven macrocyclization.

17 xed control in both iterative elongation and macrocyclization.

18 to group processing, acyl chain release, and macrocyclization.

19 ly, providing examples of ene-yne metathesis macrocyclization.

20 luoroborates to establish conditions for the macrocyclization.

21 ss to the key trifluoroborate needed for the macrocyclization.

22 and 12 have been prepared via mixed Linstead macrocyclization.

23 ation, which is considerably rigidified upon macrocyclization.

24 preorganize linear peptides for head-to-tail macrocyclization.

25 al evaluation of molecules as candidates for macrocyclization.

26 plete rigidification of the molecule through macrocyclization.

27 f the plant enzyme PCY1 involved in orbitide macrocyclization.

28 plied to the formation of cyclic peptides by macrocyclization.

29 linear substrates is not a prerequisite for macrocyclization.

30 ase this intermediate rather than proceed to macrocyclization.

31 s are protected at their N- and C-termini by macrocyclization.

32 be regioselectively incorporated during the macrocyclization.

33 a partner protein that together catalyze the macrocyclization.

34 in this pathway, including the unprecedented macrocyclization.

35 l4 and CrCl3, was the key for the success of macrocyclization.

36 fications for helix stabilization or general macrocyclization.

37 ubvert the synthetic preferences for one-pot macrocyclizations.

38 reactions, including C-C cross-couplings and macrocyclizations.

39 le alternative to traditional cross-coupling macrocyclizations.

40 ition and antiviral activity effect of P1-P3 macrocyclization, 14- and 15-membered macrocyclic PIs we

41 lobal conformational constraint through beta-macrocyclization achieved higher affinity.

42 ular Larock indole synthesis for the initial macrocyclization, adopting conditions that permit utiliz

43 ptide fragments [34 + 35 --> 51] followed by macrocyclization afforded the fully protected motuporin

44 f three heterocyclic amino acids followed by macrocyclization afforded the natural product.

45 In macrocyclization and "ethenolysis" of methyl oleate (i.e

46 condensation, a spontaneous Wadsworth-Emmons macrocyclization and a directed epoxidation/elimination

47 f the minimum structural requirement for the macrocyclization and assembly process in forming nanopar

48 dienyl cobalt at high temperature leads, via macrocyclization and capture of the intermediate cyclobu

49 t late in thiopeptide biosynthesis to affect macrocyclization and cleavage of the N-terminal leader p

50 Here, we show how macrocyclization and further derivatization of the linke

51 Iterative macrocyclization and hydrolysis reactions lead to 68% of

52 ic tumors is achieved through intramolecular macrocyclization and in situ aggregation upon caspase-3

53 y active natural products are constrained by macrocyclization and modified with carbohydrates.

54 cycloadditions can be harnessed for peptide macrocyclization and stabilization within a range of pep

55 me target (e.g. caspase-3/7), which triggers macrocyclization and subsequent in situ self-assembly in

56 trated in the topical contexts of metathesis macrocyclization and the ethenolysis of renewable oils.

57 y, the new trends in decarboxylative radical macrocyclizations and the interplay between photoredox a

58 n determined whether TE domains can catalyse macrocyclization (and elongation in the case of symmetri

59 loids were fashioned through a dimerization, macrocyclization, and four consecutive reductions.

60 Improvements to linear peptide isolation, macrocyclization, and peptide purification were demonstr

61 Herein, we present the P1-P3 macrocyclization approach followed for identification of

62 We report a double-click macrocyclization approach for the design of constrained

63 strating the application of the double-click macrocyclization approach to non-helical, extended, or i

64 re we implement a diversity-oriented peptide macrocyclization approach towards miniature tau, or 'min

65 Peptide ligation and macrocyclization are among the most relevant approaches

66 apling approach and heterocycle ring-forming macrocyclizations are included, along with multicomponen

67 l diversification of metal-catalyzed peptide macrocyclization as a special class of late-stage peptid

68 he development of the peptide multicomponent macrocyclization as a strategy capable to compete with t

69 Our findings support macrocyclization as an advantageous strategy to enhance

70 and atropodiastereoselective Dieckmann-type macrocyclization as key steps.

71 c ureas was developed with Grubbs metathesis macrocyclization as the key step.

72 the first time and shown to allow productive macrocyclization at concentrations up to 200 mM.

73 As such, macrocyclization at the chosen Phe(9)-D-Orn(10) site may

74 Macrocyclization at the highly successful Phe(9)-d-Orn(1

75 s synthetic route was designed to circumvent macrocyclization-based strategies to complex, cyclized c

76 Macrocyclization between tetrathiafulvalene (TTF) dithio

77 were synthesized on solid support employing macrocyclization by imine formation and subsequent stere

78 he C42-C46 segment and subsequent late-stage macrocyclization by installation of the (Z)-C2/C3 alpha,

79 also illuminated the scope and limitation of macrocyclization by intramolecular Reformatsky reaction

80 ct haliclamide has been synthesized based on macrocyclization by ring-closing olefin metathesis.

81 w years, since it has been demonstrated that macrocyclization can favorably alter the biological and

82 Macrocyclization can improve bioactive peptide ligands t

83 development of a novel hetero-pinacol-based macrocyclization cascade sequence.

84 provides evidence for TycC TE as a versatile macrocyclization catalyst and raises the prospect of usi

85 palladium(0)-mediated indole annulation for macrocyclization closure of the strained 16-membered bia

86 diasteroselectivity observed with analogous macrocyclizations conducted using a Suzuki biaryl coupli

87 Macrocyclization could also provide a less peptidic HCV

88 rease in the number of steps involved in the macrocyclization could lead to a larger number of possib

89 an (alpha-Me)Ppp-containing peptide by beta-macrocyclization did result in pronounced elevation of b

90 The synthesis features a key Sakurai macrocyclization/dimerization reaction that simultaneous

91 is (RCM), enabling a further increase in the macrocyclization efficiency under simulated high dilutio

92 d geometry of the building blocks affect the macrocyclization energy landscape.

93 Here we show that the macrocyclization enzyme of the cyanobactin family, PatGm

94 To date, known macrocyclization enzymes have been shown to be active on

95 l groups in the coupled product for a future macrocyclization event that would close the 15-membered

96 trile) (AIBN) triggers a 13-endo-dig radical macrocyclization followed by two sequential radical tran

97 The latter was used to effect a macrocyclization, form a C-C bond, and install a stereog

98 Subsequently, a Yamaguchi macrocyclization formed the core lactone, while a select

99 entapeptide inhibitor, 1, we envisioned that macrocyclization from the P2 proline to P3 capping could

100 Macrocyclization from the phosphotyrosyl (pTyr) mimetic'

101 ynthesis involving vinyllithium addition and macrocyclization gave way to a newer and more practical

102 ng with multicomponent methods incorporating macrocyclization handles and the one-pot syntheses of ma

103 The strategy of macrocyclization has been proved to be successful in imp

104 In these efforts, macrocyclization has been successfully utilized to take

105 roach to synthesize cyclic peptides via A(3)-macrocyclization has been used to make R- and S-configur

106 Peptide macrocyclization has traditionally relied on lactam, lac

107 strategies are available for their chemical macrocyclization, however, enzyme-mediated methods remai

108 with O-C bond-forming TE domains capable of macrocyclization, hydrolysis, transesterification, and p

109 ed and are also discussed; it was found that macrocyclization (i.e. intramolecular alkyne-aldehyde co

110 This finding highlights the importance of macrocyclization in combination with rigidifying post-tr

111 copper catalyzed azide-alkyne cycloaddition macrocyclization in flow at elevated temperature, could

112 r Nozaki-Hiyama-Kishi coupling to accomplish macrocyclization in improved yield.

113 ), to enable a pyridine-thiazoline (pyr-thn) macrocyclization in mRNA display.

114 Improved reaction conditions for macrocyclization in the formation of 33 are also detaile

115 Macrocyclizations in exceptionally good yields were obse

116 A thermodynamic approach to peptide macrocyclization inspired by the cyclization of non-ribo

117 ncp reductase is the first to mediate imine macrocyclization involving peptide N- and C-termini.

118 ing IMes was found to be highly efficient in macrocyclizations involving ring-closing metatheses (RCM

119 Macrocyclization is a broadly applied approach for overc

120 Macrocyclization is a valuable tool for drug design and

121 High-dilution equilibrium macrocyclization is developed as a general approach to t

122 ormed intermolecularly at an early stage and macrocyclization is efficiently achieved by amide bond f

123 A mechanistic proposal for the macrocyclization is supported by computational studies o

124 the side chain on the energy barrier for the macrocyclization is very small.

125 el for the stereoselectivity observed in the macrocyclizations is also proposed.

126 modynamic control over the system, which are macrocyclization kinetics and imine reduction kinetics u

127 ugh enzymes responsible for N- to C-terminal macrocyclization, lanthipeptide formation or heterocycle

128 Somewhat surprisingly, however, macrocyclization leads to significant overall stabilizat

129 Similar beta-macrocyclization may potentially be extended to SH2 doma

130 substrates is consistent with the postulated macrocyclization mechanism(s) en route to (+)-delta-cadi

131 n, we report a generally applicable chemical macrocyclization method of unprecedented speed and selec

132 We developed a robust macrocyclization method using ring-closing metathesis an

133 port the discovery of a peptide stapling and macrocyclization method using thiol-ene reactions betwee

134 mporary developments in the field of peptide macrocyclization methodology are imperative for enabling

135 expands existing Richman-Atkins sulfonamide macrocyclization methodology, and it successfully enable

136 hallenging synthetic motifs with few general macrocyclization methods capable of accessing these type

137 sing steps to very recent 3d metal-catalyzed macrocyclization methods is highlighted.

138 des and imines, and featured eight different macrocyclization methods, two of which were novel.

139 cope of RaS enzymes and contributes a unique macrocyclization motif to the growing body of RiPP archi

140 s opposed to thioester hydrolysis or O-C/N-C macrocyclization observed in previously reported TE stru

141 The macrocyclization of 2 was accomplished through a Mitsuno

142 Structure-based macrocyclization of a 6-carboxylic acid indole chemotype

143 ve Suzuki coupling (17 + 23 --> 26; 84%) and macrocyclization of a beta-keto ester (30 --> 31; 77%).

144 umalides NA and NC were accomplished via the macrocyclization of a chlorovinylidene chromium carbenoi

145 synthesis, which employs a room-temperature macrocyclization of a diboronate precursor, single-elect

146 Macrocyclization of a known binder may stabilize its bio

147 autonomous ability to catalyze head-to-tail macrocyclization of a linear peptide thioester with the

148 tems, the thioesterase domain is involved in macrocyclization of a linear precursor presented as an a

149 It is also found that macrocyclization of a receptor can, unexpectedly, increa

150 Studies on the macrocyclization of alpha,omega-dialdehydes have reveale

151 Intramolecular macrocyclization of alpha,omega-polyyne precursors via C

152 The synthesis employs Linstead crossover macrocyclization of dimethyl 6,7-dicyano-5,8-dithia-6(Z)

153 Direct macrocyclization of diol 4 and 1,10-phenanthroline-2,9-d

154 Enzymes that can catalyze the macrocyclization of linear peptide substrates have long

155 The macrocyclization of linear peptides is very often accomp

156 enzymes capable of catalyzing regioselective macrocyclization of natural or synthetic substrates.

157 Here we show that TycC TE can catalyze macrocyclization of peptide substrates that are dramatic

158 erein, we report the first gold(I)-catalyzed macrocyclization of peptide-EBXs (ethynylbenziodoxolones

159 fective synthetic tools for the ligation and macrocyclization of peptides arising from isocyanide-bas

160 A method for the decarboxylative macrocyclization of peptides bearing N-terminal Michael

161 novel rapid arene triazene strategy for the macrocyclization of peptides that generates an inbuilt c

162 we report a novel "CyClick" strategy for the macrocyclization of peptides that works in an exclusivel

163 rovide a basis for understanding the related macrocyclization of peptides with aziridine aldehydes.

164 hain-to-side chain and side chain-to-termini macrocyclization of peptides, thus enabling not only acc

165 The key macrocyclization of phenol alcohol 7 was achieved throug

166 ve been identified for the efficient Ullmann macrocyclization of phenol and imidazole nucleophiles wi

167 udies, this procedure can be applied for the macrocyclization of small molecules and peptides and eve

168 Macrocyclization of suitably functionalized tri-, tetra-

169 icoplanin ABCD ring system and sequential DE macrocyclization of the 16-membered ring with formation

170 omophore, symmetrical tetrapeptide coupling, macrocyclization of the 26-membered octadepsipeptide con

171 Base mediated macrocyclization of the acetate ester 16 followed by bas

172 Stepwise macrocyclization of the all syn-trans-1,15-quinquecyclop

173 te [2]rotaxane was assembled in 61% yield by macrocyclization of the bis-olefin ligand about an appro

174 Pd(0)-mediated indole annulation for the key macrocyclization of the complex core peptide, utilizes a

175 de in a different conformation and catalyzes macrocyclization of the N-terminal eight residues.

176 e in a productive conformation to facilitate macrocyclization of the N-terminal fragment.

177 with the iodobenzothiazole 7 and subsequent macrocyclization of the open-chain derivatives 22-24 usi

178 ing one macrocycle and carrying out a single macrocyclization of the second bis-olefin with both liga

179 valid technique for overcoming challenges to macrocyclization of this kind.

180 Double macrocyclization of two such ligands bound to Co(III) af

181 hesized by palladium(II)-catalyzed oxidative macrocyclizations of bis(vinyl boronate esters) or ring-

182 P-domain subfamily, catalyzes intramolecular macrocyclizations of its core peptide during the sequent

183 Macrocyclizations of NRP, PK, and hybrid NRP-PK scaffold

184 To study P1-P3 macrocyclizations of previously reported tertiary-alcoho

185 airs, allowing us to pinpoint the effects of macrocyclization on binding affinity, selectivity, and A

186 features of the natural products, including macrocyclization or proline mimicry strategies.

187 ick" reaction) as the protocol for the final macrocyclization or stoppering reactions of the entwined

188 complexity of the substrate and the reverse macrocyclization order did not diminish the atropodiaste

189 Post-macrocyclization oxidation of the bridging sulfur moieti

190 angement, Wacker oxidation, ligand-free Heck macrocyclization, oxidative cleavage of indole, synthesi

191 Macrocyclization proceeds efficiently, inducing folding

192 ification of the hydrogen-bond synthon after macrocyclization proceeds smoothly to furnish porphyrin

193 yclic depsipeptides using an oligomerization/macrocyclization process governed by a series of Mitsuno

194 this area involve orchestrating the desired macrocyclization process in the presence of unprotected

195 study has been carried out to understand the macrocyclization process, and the results obtained nicel

196 und to be the most efficient template in the macrocyclization process, producing improved macrocycliz

197 g four coupled substitution reactions in the macrocyclization process.

198 g four coupled substitution reactions in the macrocyclization process.

199 ligomerization pathways and resulted in less macrocyclization products.

200 The macrocyclization protocol employed a phase separation/co

201 idic and fluorescently labeled amines and in macrocyclization protocols.

202 uence of various factors on the direction of macrocyclization provided the optimal conditions for the

203 es help to define the enzymatic mechanism of macrocyclization, providing evidence against the water e

204 s of the framework include the efficiency of macrocyclization (quantitative), the solution- and solid

205 A more modest, but acceptable macrocyclization reaction at the Gly(14)-Leu(15) site (4

206 unprecedented 15-membered chloronium-induced macrocyclization reaction converting merochlorin D to me

207 Central to the synthesis of largazole is a macrocyclization reaction for formation of the strained

208 The macrocyclization reaction has been studied experimentall

209 sobactin that relies upon a highly efficient macrocyclization reaction to assemble the 28-membered cy

210 n-templated synthesis was used to direct the macrocyclization reaction to the [2+2] product, while hi

211 The key cyclophane-forming macrocyclization reaction was accomplished during the co

212 had a clear catalytic template effect in the macrocyclization reaction, and surprisingly, the chlorid

213 pically associated with classical end-to-end macrocyclization reactions are avoided.

214 Macrocyclization reactions generated Z-products from eas

215 thesis of cyclophanes 18-20 by ester-forming macrocyclization reactions of diols 15 and 16 with 1,4-b

216 Crossover-Linstead macrocyclization reactions of two norbornenyl-tagged dia

217 the preorganization of the substrate for the macrocyclization reactions on one side, and for easier N

218 a template to enhance the synthetic yield of macrocyclization reactions that produce the tetralactam

219 tatin are detailed in which the order of the macrocyclization reactions was reversed from our first-g

220 esterification and Nozaki-Hiyama-Kishi (NHK) macrocyclization reactions were employed in the key step

221 cope and define the generality of its use in macrocyclization reactions, its use in directly accessin

222 lds obtained in the CB[6] and CB[7] analogue macrocyclization reactions, we performed mechanistic stu

223 ptoids undergo highly efficient head-to-tail macrocyclization reactions.

224 ed catalysts can have in promoting efficient macrocyclization reactions.

225 e 1,3-disubstituted dienes produced from the macrocyclizations represent a previously unreported subs

226 Protein macrocyclization represents a very efficient strategy to

227 a molecule in its bioactive conformation via macrocyclization represents an attractive strategy to ra

228 The success of the macrocyclization required that C(7)-OH be unprotected.

229 Macrocyclization resulted in significantly improved pote

230 zuki-Miyaura/4pai-electrocyclic ring-opening macrocyclization, resulting in a concise, unified, and s

231 y relationship studies demonstrated that the macrocyclization retains full Chk1 inhibition activity a

232 Alkyne metathesis provided an efficient macrocyclization route to a cycloparaphenyleneacetylene

233 high-yielding product formation, even for a macrocyclization scan with 14 variants.

234 hat utilizes spatial confinement to increase macrocyclization selectivity in the ring-closing metathe

235 into ribosomal peptides in conjunction with macrocyclization should enhance the drug-like features o

236 The rates of macrocyclization show a dependence on the nature of the

237 y altering the order of final couplings, two macrocyclization sites, Phe(9)-d-Orn(10) and Gly(14)-Leu

238 uents were introduced after a yield-limiting macrocyclization step (65-98%).

239 synthetase that also performs the subsequent macrocyclization step at the carbonyl group of this amin

240 The high efficiency of the macrocyclization step can be attributed to the structura

241 The key macrocyclization step in the synthesis of simeprevir, a

242 The key macrocyclization step to form the 65-membered ring is ac

243 The key macrocyclization step was achieved using a sequential ri

244 The imine-forming macrocyclization step was carried out under a variety of

245 n the metal (Cu or Pd) catalyst used for the macrocyclization step.

246 eta-ketoesters without performing a discrete macrocyclization step.

247 c substitution reaction was used for the key macrocyclization step.

248 glington-Glaser coupling was applied for the macrocyclization step.

249 anions by copper(I) iodide were used for the macrocyclization step.

250 mplated amide bond formation reaction at the macrocyclization step.

251 adds to the growing list of Nature's peptide macrocyclization strategies and expands the already impr

252 and high dilution, drawbacks of traditional macrocyclization strategies, and it effectively removes

253 A macrocyclization strategy designed to lock the active co

254 Here, we describe a novel, on-resin macrocyclization strategy for the synthesis of potent in

255 We have developed a two-component macrocyclization strategy that allows these structures t

256 ery of a spontaneous Horner-Wadsworth-Emmons macrocyclization strategy, and the development of a nove

257 in analogues using a highly convergent Prins-macrocyclization strategy.

258 step-economical and convergent Prins-driven macrocyclization strategy.

259 ple of what will prove to be a useful Larock macrocyclization strategy.

260 ist beta-sheet preorganization of an acyclic macrocyclization substrate for 49-membered ring closure.

261 ilizes a Lewis acid-catalyzed intramolecular macrocyclization that installs the tetrahydropyran ring

262 , including halogenation, hydroxylation, and macrocyclization, the biochemical properties and catalyt

263 ntly, in this work, the first intramolecular macrocyclization through a Passerini reaction is describ

264 Here we describe the utility of peptide macrocyclization through perfluoroaryl-cysteine SNAr che

265 formation, Yamaguchi esterification, and RCM macrocyclization to access five C11/C12 Z-configured, 2-

266 Bilanes underwent oxidative macrocyclization to afford a new class of trans-A(2)B-co

267 y has been broadened by elaborating the A(3)-macrocyclization to include various di-amino carboxylate

268 benzyl protecting group is necessary for the macrocyclization to occur.

269 f a study of the Heck reaction as a tool for macrocyclization to provide strained paracyclophanes, no

270 ce of stepwise syntheses relative to one-pot macrocyclizations to offer new approaches for greater un

271 ced transition metal catalysis as a powerful macrocyclization tool with relevant applications in chem

272 xperienced a renaissance as powerful peptide macrocyclization tools enabling the rapid creation of sk

273 e use of aziridine aldehyde-mediated peptide macrocyclization toward the design of cyclic peptides an

274 er underwent a different sequence of cascade macrocyclization-transannulation reactions producing the

275 yde 116 to vinylboronate 122 was followed by macrocyclization under Suzuki conditions to yield 123.

276 e current study examined the effects of such macrocyclization using a dicarboxymethyl-based pTyr mime

277 w-Evans rearrangement, cross-metathesis, and macrocyclization using a Roush-Masamune protocol.

278 oupled with dipeptides and then subjected to macrocyclization using diethylcyanophosphonate to furnis

279 tion from a diketodioxinone intermediate and macrocyclization using Furstner ring-closing alkyne meta

280 The first report of Z-selective macrocyclizations using a ruthenium-based metathesis cat

281 Herein, a rapid macrocyclization utilizing a two-step, one-pot approach

282 esis of linear peptoids and their subsequent macrocyclization via Click chemistry is described.

283 Notably, DE macrocyclization via diaryl ether formation on substrate

284 cursor, but this substance failed to undergo macrocyclization via intramolecular Suzuki-Miyaura coupl

285 an advanced C(1-19) vinyl iodide followed by macrocyclization via Suzuki-Miyaura cross-coupling compl

286 The macrocyclization was achieved under Mitsunobu conditions

287 ing a one-step olefination protocol, and the macrocyclization was carried out using a Horner-Emmons o

288 An underutilized late-stage SmI(2)-mediated macrocyclization was employed to construct the 23-member

289 A recently developed dimerization/macrocyclization was employed to synthesize a series of

290 Finally, N-aryl macrocyclization was performed on a p53 peptide inhibito

291 The following macrocyclization was realized in a coil reactor made of

292 Macrocyclization was typically performed using HCTU and

293 onsistent with theoretical models of polymer macrocyclization, we have demonstrated that, in the pres

294 Suzuki-Miyaura macrocyclizations were successfully achieved both in sol

295 s, and a challenging ring-closing metathesis macrocyclization with an unusual Stewart-Grubbs catalyst

296 synthesized through a facile fourfold Suzuki macrocyclization with aromatic linkers and a tetraboryla

297 matic nucleophilic substitution reaction for macrocyclization with biaryl ether formation completed t

298 A systematic study of macrocyclization with its dependence on concentration an

299 a-Kishi coupling that significantly improved macrocyclization yields (90-96%) and allowed for differe

300 macrocyclization process, producing improved macrocyclization yields with regard to the nontemplated