ライフサイエンスコーパス: carbonitrile

1 ,5beta,17beta)-3-hydroxy-18-norandrostane-17-carbonitrile).

2 synthetic steroid PCN (pregnenolone-16alpha-carbonitrile).

3 ucleophilic cyclization to the corresponding carbonitrile.

4 uch as dexamethasone or pregnenolone-16alpha-carbonitrile.

5 ifampicin but not with pregnenolone-16 alpha-carbonitrile.

6 high concentrations of pregnenolone 16 alpha-carbonitrile.

7 of 4-imino-3-phenyl-3,4-dihydroquinazoline-2-carbonitrile.

8 but not the PXR ligand pregnenolone 16alpha-carbonitrile.

9 {[(tert-butyldimethylsilyl)oxy]methyl}phenyl)carbonitrile.

10 dition-methylations to 3-oxo-1-cyclohexene-1-carbonitrile.

11 everal 1-anilino-6,7-dimethoxyisoquinoline-4-carbonitriles.

12 , 6,7-dialkoxy-4-oxo-1, 4-dihydroquinoline-3-carbonitriles.

13 midopentanoate and 2, 4-diaminoquinazoline-6-carbonitriles.

14 electivity and leads to 2-hydroxy-2H-pyran-5-carbonitriles.

15 romophenyl)-4-imino-3,4-dihydroquinazoline-2-carbonitriles.

16 cyclization produces 5,6-dihydroindolizine-5-carbonitriles.

17 2-oxo-2,5-dihydrothiochromeno[4,3- b]pyran-3-carbonitriles.

18 tive monoarylation was observed with primary carbonitriles.

19 ative to the preparation of alpha-heteroaryl carbonitriles.

20 r two steps starting from 5-aminoimidazole-4-carbonitriles 1-8 in moderate to good yields.

21 midazo[1,2-b][1,2,4]triazin- 7-yl]biphenyl-2-carbonitrile (1), an orally active GABA(A) alpha(2/3)-se

22 oro-4'-(alpha-d-mannopyranosyloxy)biphenyl-4-carbonitrile (10j) a FimH antagonist with an optimal in

23 17(20)-ene modification as in 17(20)-ene-20-carbonitrile (14) did not increase activity in compariso

24 Eight 2-phenyl-3H-imidazo[4,5-b]quinoline-9-carbonitriles 15 are prepared in four steps from N'-aryl

25 ffords 2-phenyl-3H-imidazo[4,5-b]quinoline-9-carbonitriles 15 in near quantitative yields.

26 mediate 2,4-diaminopyrido[2,3-d]pyrimidine-6-carbonitrile 16 with the appropriate anilines afforded t

27 crease activity in comparison to the 20 beta-carbonitrile (16).

28 nyl)piperazine-1-carbonyl)-10H-phenoxazine-3-carbonitrile (16o), showed excellent antiproliferative p

29 4-diamino-5-methylpyrido[2, 3-d]pyrimidine-6-carbonitrile (18), with the appropriate anilines.

30 mino-7-benzylpyrrolo[2,3-d][1,2,3]triazine-5-carbonitrile (19) and 2-amino-1-benzylpyrrole-3,4-dicarb

31 fected mice with 4-phenyl-1,2,5-oxadiazole-3-carbonitrile-2-oxide led to marked reductions in worm bu

32 of 5-amino-1-(N-methylcarbamoyl)imidazole-4-carbonitrile (25).

33 bofuranosyl)pyrrolo[2,3-d][1,2,3]t riazine-5-carbonitrile (26) and 2-amino-1-(2,3,5-tri-O-benzoyl-bet

34 hydro-1 H-indol-5-yl)-1-methyl-1 H-pyrrole-2-carbonitrile 27 (WAY-255348), which demonstrated potent

35 7is prepared from either 5-diazoimidazole-4-carbonitrile (28) and methyl isocyanate or by diazotizat

36 -amines 3 gives 1H-pyrazolo[3,4-d]thiazole-5-carbonitriles 4.

37 l assignment of 1H-pyrazolo[3,4-d]thiazole-5-carbonitriles 4.

38 phenyl)-furan-2-yl]-imidazo[1,2-a]pyridine-6-carbonitrile (4a), through the bis-O-acetoxyamidoxime fo

39 d 4-amino-7-allylpyrrolo-[2,3-d]pyrimidine-5-carbonitrile (4k).

40 mines 3, and 6H-pyrazolo[3,4-c]isothiazole-3-carbonitriles 5, together with several minor side produc

41 ituted 4,6-diaminopyrrolo[2,3-d]pyrimidine-5-carbonitrile, -5-carboxamide, and -5-thiocarboxamide ana

42 ubstituted 4-aminopyrrolo[2,3-d]pyrimidine-5-carbonitrile, -5-carboxamide, and -5-thiocarboxamide der

43 4,6-dimethyl-6H-pyrazolo[3,4-c]isothiazole-3-carbonitrile (5a) and helps resolve a previous incorrect

44 ring-contracted 1H-pyrazolo[3,4-d]thiazole-5-carbonitriles 6 (94-100%).

45 3,5-triazin-2-yl) amino)-1H-1,2,3-triazole-5-carbonitrile (6) and its perchlorate and nitrate energet

46 opyl-4,7-dihydropyrazolo[1,5-a]p yrimidine-3-carbonitrile 61 significantly raised the circulating lev

47 gives 5H-pyrazolo[3,4-e][1,2,4]dithiazine-3-carbonitriles 7 in good yields (74-85%) and 6H-pyrazolo[

48 methyl-5H-pyrazolo[3,4-e][1,2,4]dithiazine-3-carbonitrile (7a) gave 1,3-dimethyl-6H-pyrazolo[3,4-f][1

49 7-oxo-7,8-dihydro-pyrid o[2,3-d]pyrimidine-6-carbonitrile (7x), was found to be the most active, indu

50 d 6H-pyrazolo[3,4-f][1,2,3,5]trithiazepine-4-carbonitriles 9 as minor products (0-6%).

51 l-6H-pyrazolo[3,4-f][1,2,3,5]trithiazepine-4-carbonitrile (9a), but on prolonged reaction times, it g

52 icaciously activated by pregnenolone 16alpha-carbonitrile, a glucocorticoid receptor antagonist that

53 cile access to pyridinium, sulfonium, thiol, carbonitrile, acetoxy, and amino derivatives.

54 roid 3alpha-hydroxy-5alpha-androstane-17beta-carbonitrile (ACN).

55 3alpha,5alpha, 17beta-3-hydroxyandrostane-17-carbonitrile (ACN)] was studied in detail.

56 (+)-3alpha-hydroxy-5alpha-androstane-17beta-carbonitrile [(+)-ACN], a neuroactive steroid, had no ef

57 alpha,5alpha, 17beta)-3-hydroxyandrostane-17-carbonitrile [(+)-ACN].

58 M), 1-(2-amino-3-methyl-butyryl)-azetidine-2-carbonitrile (AMAC), which has shown efficacy in two est

59 ubstituted 4-aminopyrrolo[2,3-d]pyrimidine-5-carbonitrile analogs 4a-j,l.

60 the results obtained with the rigid 17 beta-carbonitrile analogs were analyzed using molecular model

61 sultant 7-phenylaminothieno[3,2-b]pyridine-6-carbonitrile analogues show potent inhibition of Src kin

62 (+)-3alpha-hydroxy-5alpha-androstane-17beta-carbonitrile and (+)-3alpha-hydroxy-5alpha-pregnan-20-on

63 oxyethoxy)methyl]pyrrolo[2,3-d]-pyrimidine-5-carbonitrile and -5-thiocarboxamide derivatives and seve

64 1-phenyl-2,3,5,6,7,8-hexahydroisoquinoline-4-carbonitrile and 1-alkyl-3-oxo-3,5,6,7-tetrahydro-2H-cyc

65 ioxo-4,5-dihydro-3H-benzo[e][1,4]diazepine-2-carbonitrile and 2-(4-substituted-1,2,5-thiadiazol-3-yl)

66 tocol is atom economical, involving only the carbonitrile and benzohydrazide synthons and producing o

67 the electronic environment of the heteroaryl carbonitrile and benzohydrazide.

68 for dexamethasone and pregnenolone 16 alpha-carbonitrile and may explain the mechanism by which low

69 accessible 1,2,3,4-tetrahydroisoquinoline-1-carbonitriles and 1,2-bis(bromomethyl)arenes is describe

70 of 2-oxo-5,6-dihydro-2 H-benzo[ h]chromene-3-carbonitriles and 2-oxo-2,5-dihydrothiochromeno[4,3- b]p

71 is applicable to both primary and secondary carbonitriles and a wide range of heteroaryl halides.

72 nctional group interconversion of heteroaryl carbonitriles and benzohydrazides via microwave-assisted

73 tosteroids or 3 alpha-hydroxysteroid-17 beta-carbonitriles and which contained various methyl group s

74 3alpha,5alpha,17beta)-3-hydroxyandrostane-17-carbonitrile) and B285 ((3alpha,5beta,17beta)-3-hydroxy-

75 e products, 4-amino-2,6-diphenylpyrimidine-5-carbonitrile, and a short synthesis of a cytosine antifu

76 g 3-methylcholanthrene, pregnenolone-16alpha-carbonitrile, and ciprofibrate.

77 roclor 1254, isoniazid, pregnenolone 16alpha-carbonitrile, and clofibrate) or the general P450 inhibi

78 coupling of 4-(2-bromoanilino)quinazoline-2-carbonitrile; and (3) a nonoxidative Pd(Ar3P)3 [Ar = 3,5

79 It was found that 4-anilinoquinoline-3-carbonitriles are effective inhibitors of EGF-R kinase w

80 propriately substituted 4-anilinoquinoline-3-carbonitriles are potent inhibitors of Src kinase, with

81 Benzo[4,5]imidazo[1,2-c]quinazoline-6-carbonitriles are prepared in high yields via three new

82 se 4-anilino-7,8-dialkoxybenzo[g]quinoline-3-carbonitriles are presented here.

83 , providing the 4-anilinobenzo[g]quinoline-3-carbonitriles as a series with enhanced Src inhibitory p

84 l)-6-hydroxy-[1,2,4]azolo[1,5-a]pyrimidine-5-carbonitriles as unexpected nucleophilic transformation

85 cocorticoid antagonist pregnenolone 16 alpha-carbonitrile at 100 microM blocks dexamethasone binding

86 enylacetones to substituted 2-oxo-2H-pyran-3-carbonitriles at room temperature under alkaline conditi

87 anilinoquinazolines and 4-anilinoquinoline-3-carbonitrile-based kinase inhibitors and their influence

88 bled monolayers of 1,3,5-tris(4'-biphenyl-4"-carbonitrile)benzene, a large functional trinitrile mole

89 -hydroxy ethyl)-3a-methyl-1H-benz[e]indene-3-carbonitrile (BI-2) using single-channel patch-clamp and

90 It is proposed that the quinoline-3-carbonitriles bind in a similar manner where the water m

91 (+)-3alpha-hydroxy-5alpha-androstane-17beta-carbonitrile blocked responses to acetylcholine (IC50, 1

92 ipine, clotrimazole, or pregnenolone 16alpha-carbonitrile, but not microsomes from control, dexametha

93 We show that the compound, carbonitrile-chalcone 4, blocks the recruitment of eosin

94 -alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitrile CHK1 inhibitors was generated by hybridizat

95 thin the 5-(2-oxoindolin-5-yl)-1 H-pyrrole-2-carbonitrile class of compounds.

96 triazine-2,4,6-triyl)tris(([1,1'-biphenyl]-3-carbonitrile)) (CN-T2T) (DeltaE(ST) = 30 meV) and BCzPh:

97 lanilino)-6-pyrrolidin-1-yl-1,3,5-triazine-2-carbonitrile (CP243522), showed a K(i) of 21 nM and was

98 -dimethylamino-3-methyl-butyryl)-azetidine-2-carbonitrile (DAMAC), that does not inhibit DPP IV, was

99 The dexamethasone- and pregnenolone 16alpha-carbonitrile-dependent induction of MRP2 expression was

100 l molecules, including a tetrahydroquinoline carbonitrile derivative (S010-0261), that inhibit the Mt

101 ation of a wide range of 4-aminopyrimidine-5-carbonitrile derivatives (33 examples) from readily avai

102 4-amino-6-bromopyrrolo++-[2,3-d]pyrimidine-5-carbonitrile derivatives 3a-k.

103 of of 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile derivatives that function as irreversible i

104 w 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitrile derivatives that function as irreversible i

105 ,5,6,7-tetrahydro-2H-cyclopenta[c]pyridine-4-carbonitrile distributes to the brain, indicating that i

106 4-anilinoquinazoline or 4-anilinoquinoline-3-carbonitrile driving portions.

107 r, (3beta,5alpha,17beta)-17-hydroxyestrane-3-carbonitrile (ECN), a novel neuroactive steroid and sele

108 f (3beta,5alpha, 17beta)-17-hydroxyestrane-3-carbonitrile [(+)-ECN] on GABAA receptors and Ca2+ chann

109 3-hydroxy-13,24-cyclo-18-norcholan-20-ene-21-carbonitrile, eltanolone, 5beta-pregnan-3alpha,21-diol-2

110 ng-annulation reaction of 2-chloroqunoline-3-carbonitriles enabled the direct synthesis of sulfur-sub

111 was further extended to o-ethynylquinoline-3-carbonitriles for the synthesis of alkoxy-substituted 3H

112 on a BN/Cu(111) template by codeposition of carbonitrile-functionalized porphyrin derivatives (2H-TP

113 f Grignard reagents to 3-oxocyclohex-1-ene-1-carbonitrile generates C-magnesiated nitriles whose alky

114 ich shows that the aniline group at C-4, the carbonitrile group at C-3, and the alkoxy groups at C-6

115 r polyphenyl molecular linkers with terminal carbonitrile groups on a smooth Ag(111) noble-metal surf

116 nicotinonitriles and 2,5-diaryl-1H-pyrrole-3-carbonitriles have been accomplished via a Pd-catalyzed

117 and modestly induced by pregnenolone 16alpha-carbonitrile in the RR strain but negligibly in the rr s

118 step 3-aryl-4-imino-3,4-dihydroquinazoline-2-carbonitriles in 53-81% yields.

119 reb amide), -carboxylate methyl esters, and -carbonitriles in excellent yields.

120 oxidative coupling of 4-anilinoquinazoline-2-carbonitriles in neat trifluoroacetic acid (TFA); (2) a

121 m easily accessible 3,4-dihydro-2H-pyrrole-2-carbonitriles in one-pot procedures.

122 ished the 4-anilino-6, 7-dialkoxyquinoline-3-carbonitrile inhibitors of EGF-R kinase.

123 series of 4-anilino-6, 7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor recep

124 amino-4-(3-pyridyl)-4H-naphtho(1,2-b)pyran-3-carbonitrile, is a potent antiproliferative compound tha

125 rpholin-4-yl-ethyl)phenylami no]pyrimidine-5-carbonitrile (JNJ-17029259) represents a novel structura

126 Initial 4-anilino-6-aminoquinoline-3-carbonitrile leads showed poor selectivity for Tpl2 over

127 position of our 4-anilino-6-aminoquinoline-3-carbonitrile leads.

128 proposed 8-oxo-8H-acenaphtho[1,2-b]pyrrol-9-carbonitrile led to a structural revision, and the produ

129 ships for additional thieno[3,2-b]pyridine-6-carbonitriles, modifying the substituents on the C-2 phe

130 und based on a 2-hydroxy-4-phenylthiophene-3-carbonitrile moiety.

131 4-diazepan-1- yl)sulfonyl)phenyl)quinoline-3-carbonitrile (NEU-924, 83) for T. cruzi and N-(3-chloro-

132 with dexamethasone or pregnenolone-16 alpha-carbonitrile only if consensus II sequences were include

133 given the PXR agonist, pregnenolone-16alpha-carbonitrile, or the herbal medicine, St John's wort, ch

134 ce with the PXR agonist pregnenolone-16alpha-carbonitrile (PCN) activated Akr1b7 gene expression, whe

135 ries to the PXR ligands pregnenolone-16alpha-carbonitrile (PCN) and dexamethasone increased p-glycopr

136 sing the mPXR activator pregnenolone-16alpha-carbonitrile (PCN) and was subsequently downregulated us

137 ment with PXR activator pregnenolone 16alpha-carbonitrile (PCN) down-regulated the mRNA levels of car

138 he activation of PXR by pregnenolone 16alpha-carbonitrile (PCN) in AKR/J mice can prevent the develop

139 activated the PXR with pregnenolone 16alpha-carbonitrile (PCN) in wild-type mice, which greatly redu

140 phenobarbital (PB) and pregnenolone-16alpha-carbonitrile (PCN) occurs via increased hepatic expressi

141 ne X receptor activator pregnenolone-16alpha-carbonitrile (PCN) or the Ah receptor ligand 2,3,7,8-tet

142 response to PXR ligand pregnenolone 16alpha-carbonitrile (PCN) treatment in mouse liver in vivo both

143 Treatment of rats with pregnenolone-16alpha-carbonitrile (PCN), a ligand for the rodent pregnane X r

144 tment with 5-pregnen-3beta-ol-20-one-16alpha-carbonitrile (PCN), followed by an increase in Cyp3a11 m

145 atoxic steroids such as pregnenolone 16alpha-carbonitrile (PCN), which induce cytochrome P450 3A (CYP

146 nd 20-day pregnant, and pregnenolone-16alpha-carbonitrile (PCN)-treated rats using in vivo metabolic-

147 activator 5-pregnen-3beta-ol-20-one-16alpha-carbonitrile (PCN, 25 mg/kg) or its vehicle over 7 d.

148 activator 5-pregnen-3beta-ol-20-one-16alpha-carbonitrile (PCN, 25 mg/kg) or its vehicle over 7 days.

149 lamino)phenyl)imino)methyl)-[1,1-biphenyl]-4-carbonitrile (PEBP) for Cu(2+) detection was fabricated

150 -substituted analogue 1-phenylisoquinoline-4-carbonitrile (piqCN), which both result in red phosphore

151 ,5,6,7-tetrahydro-2H-cyclopenta[c]pyridine-4-carbonitrile PREPL inhibitors that are able to block PRE

152 ydroxy-aryl-5,6,7,8-tetrahydroisoquinoline-4-carbonitriles represent interesting chemical scaffolds,

153 )]benzene (TCPOBOP) and pregnenolone 16alpha-carbonitrile, respectively.

154 of 5-((4-aminopyridin-2-yl)amino)pyrazine-2-carbonitriles resulted in the identification of a potent

155 5-methyl-2-((2-nitrophenyl)amino)thiophene-3-carbonitrile (ROY), the most polymorphic small molecule

156 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile series results from the relative malleabili

157 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile series that bind to both CDK9/cyclin T and

158 roxy-2-methyl-3-phenoxypropanoyl)-indoline-4-carbonitriles showed potent binding to the androgen rece

159 analogously substituted 4-anilinoquinoline-3-carbonitrile SKI-606, which is undergoing evaluation in

160 We were interested in whether carbonitrile substitution at other ring positions might

161 6,7,8,13-tetrahydro-5H-dibenzo[c,f]azonine-5-carbonitriles takes place.

162 2-benzylamino-pyrazolo[1,5-a]pyrimidinone-3-carbonitrile template.

163 ntermediate, 6-acetamido-4-chloroquinoline-3-carbonitrile, that involved a safer cyclization step.

164 [(3beta,5beta,17beta)-3-hydroxyandrostane-17-carbonitrile] that was also the most effective blocker o

165 ,3,4-tetrahydrobenzo[b][1,6]naph thyridine-8-carbonitrile, the most potent compound, has an excellent

166 P mice over 7 days with pregnenolone-16alpha-carbonitrile to activate the nuclear receptor pregnane X

167 sequently, conversion of benzo[b]carbazole-6-carbonitrile to carbazole quinone is observed upon prolo

168 The inability of pregnenolone 16 alpha-carbonitrile to fully compete with dexamethasone for cyt

169 ats, dexamethasone and pregnenolone-16 alpha-carbonitrile treatment elevated ring hydroxylation up to

170 es from easily accessible 2-alkynyl indole-3-carbonitriles under mild reaction conditions has been de

171 generation FAPIs comprising an electrophilic carbonitrile warhead, which in turn translates into exte

172 When N-(propargyl)indole-2-carbonitrile was first combined with aniline and LiHMDS

173 routes were studied, and N-(allenyl)indole-2-carbonitrile was identified as the key intermediate.

174 totypical CYP3A inducer pregnenolone 16alpha-carbonitrile was restricted to constructs containing the

175 A library of trans-4,5-dihydrofuran-3-carbonitriles was synthesized in a diastereoselective ma

176 (1-(3-(2-chlorophenoxy) propyl)-1H-indole-3-carbonitrile) was identified as a small molecule that bl

177 amino-4-(3-pyridyl)-4H-naphtho(1,2-b)pyran-3-carbonitrile] was characterized.

178 (-)-3alpha-hydroxy-5alpha-androstane-17beta-carbonitrile were consistent with the hypothesis that po

179 tained or replaced with a 4-aminoquinoline-7-carbonitrile were synthesized in an effort to improve dr

180 halophenyl)-2-benzoylthieno[2,3-b]pyridine-5-carbonitriles were discovered as a new class of PfGSK-3

181 e 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles were prepared from the appropriate 2-subst

182 -phenyl-7-phenylaminothieno[3,2-b]pyridine-6-carbonitriles were recently reported to be inhibitors of

183 ides [1,2,3]triazolo[1,5-a]quinoxaline-5(4H)-carbonitriles, whereas in the presence of an excess of t

184 yl-1H-imidazol-4-yl)methylamin o]quinoline-3-carbonitrile, which demonstrated in vitro as well as in

185 a 6,7-dialkoxy-4-oxo-1,4-dihydroquinoline-3-carbonitrile, which was transformed as before.

186 eactions of 1-amino-2-imino-4-arylpyridine-3-carbonitriles with benzocyclic ketones such as benzosube

187 dative couplings of 3,4-dihydro-2H-pyrrole-2-carbonitriles with copper(II)-salts furnished 2,2'-bipyr

188 he one-pot reaction of N-(propargyl)indole-2-carbonitriles with methanol and LiHMDS on heating, follo

189 ation of 4-chloro-6-(crotonamido)quinoline-3-carbonitriles with monocyclic or bicyclic anilines.

190 Interactions of N-(propargyl)indole-2-carbonitriles with nitrogen nucleophiles were studied.

191 cylation of 6-amino-4-(arylamino)quinoline-3-carbonitriles with unsaturated acid chlorides or by amin

192 cylation of 6-amino-4-(arylamino)quinoline-3-carbonitriles with unsaturated acid chlorides or mixed a