ライフサイエンスコーパス: macrocyclization

1 a bioactive conformation by ring formation (macrocyclization).

2 action of the amide synthase responsible for macrocyclization.

3 his propensity to act as nucleophiles in the macrocyclization.

4 ides ideal candidates for the entropy-driven macrocyclization.

5 f the plant enzyme PCY1 involved in orbitide macrocyclization.

6 govern polyketide assembly, processing, and macrocyclization.

7 y the N-heterocyclic carbenes liberated upon macrocyclization.

8 plied to the formation of cyclic peptides by macrocyclization.

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

10 xed control in both iterative elongation and macrocyclization.

11 linear substrates is not a prerequisite for macrocyclization.

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

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

14 luoroborates to establish conditions for the macrocyclization.

15 ss to the key trifluoroborate needed for the macrocyclization.

16 and 12 have been prepared via mixed Linstead macrocyclization.

17 ase this intermediate rather than proceed to macrocyclization.

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

19 ation, which is considerably rigidified upon macrocyclization.

20 a partner protein that together catalyze the macrocyclization.

21 in this pathway, including the unprecedented macrocyclization.

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

23 fications for helix stabilization or general macrocyclization.

24 the folding effect of the multicomponent Ugi macrocyclization.

25 hoice to fold synthetic peptides by means of macrocyclization.

26 ), followed by selective ruthenium-catalyzed macrocyclization.

27 ntification of an efficient strategy for the macrocyclization.

28 itical parameter defining the success of the macrocyclization.

29 The key reaction is a palladium-catalyzed macrocyclization.

30 mino acid oligomer intermediates followed by macrocyclization.

31 ving a highly advantageous Heck reaction for macrocyclization.

32 ons upon being subjected to depolymerization-macrocyclization.

33 le alternative to traditional cross-coupling macrocyclizations.

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

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

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

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

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

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

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

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

42 Iterative macrocyclization and hydrolysis reactions lead to 68% of

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

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

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

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

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

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

49 Peptide ligation and macrocyclization are among the most relevant approaches

50 and atropodiastereoselective Dieckmann-type macrocyclization as key steps.

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

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

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

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

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

56 Macrocyclization between tetrathiafulvalene (TTF) dithio

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

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

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

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

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

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

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

64 Macrocyclization could also provide a less peptidic HCV

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

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

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

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

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

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

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

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

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

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

75 Macrocyclization from the phosphotyrosyl (pTyr) mimetic'

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

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

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

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

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

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

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

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

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

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

86 Macrocyclizations in exceptionally good yields were obse

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

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

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

90 Macrocyclization is a broadly applied approach for overc

91 Macrocyclization is a valuable tool for drug design and

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

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

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

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

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

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

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

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

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

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

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

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

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

105 The macrocyclization of 2 was accomplished through a Mitsuno

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

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

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

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

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

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

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

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

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

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

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

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

118 The macrocyclization of linear peptides is very often accomp

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

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

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

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

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

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

125 The key macrocyclization of phenol alcohol 7 was achieved throug

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

127 Macrocyclization of suitably functionalized tri-, tetra-

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

144 Post-macrocyclization oxidation of the bridging sulfur moieti

145 Macrocyclization proceeds efficiently, inducing folding

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

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

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

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

150 ligomerization pathways and resulted in less macrocyclization products.

151 The macrocyclization protocol employed a phase separation/co

152 idic and fluorescently labeled amines and in macrocyclization protocols.

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

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

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

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

157 The macrocyclization reaction has been studied experimentall

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

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

160 Macrocyclization reactions generated Z-products from eas

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

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

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

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

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

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

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

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

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

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

171 Macrocyclization resulted in significantly improved pote

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

173 Alkyne metathesis provided an efficient macrocyclization route to a cycloparaphenyleneacetylene

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

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

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

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

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

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

180 The key macrocyclization step was achieved using a sequential ri

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

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

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

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

185 mplated amide bond formation reaction at the macrocyclization step.

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

187 eta-ketoesters without performing a discrete macrocyclization step.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

210 Notably, DE macrocyclization via diaryl ether formation on substrate

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

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

213 The macrocyclization was achieved under Mitsunobu conditions

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

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

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

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

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

219 Macrocyclization was typically performed using HCTU and

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

221 Suzuki-Miyaura macrocyclizations were successfully achieved both in sol

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

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

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