ライフサイエンスコーパス: quinazoline

1 oup, and (iii) of a hydrophobic group on the quinazoline.

2 er cells to undergo apoptosis in response to quinazolines.

3 ctions for the syntheses of benzoxazoles and quinazolines.

4 esis of a small library of alkyl-substituted quinazolines.

5 ne, and aldehyde for high yield syntheses of quinazolines.

6 bromo ketones/acetates, yielded high purity quinazolines.

7 These efforts originated from quinazoline 1 and through rational design led to the dev

8 same ring) - cinnolines (1,2-benzodiazine), quinazolines (1,3-benzodiazine), phthalazines (2,3-benzo

9 ntain a novel central core (7H-pyrrolo[3,2-f]quinazoline-1,3-diamine), which may significantly expand

10 ing expected 3'-phenyl-1'H-spiro[indene-2,2'-quinazoline]-1,3,4'(3'H)-triones were obtained.

11 azole (1a) with 1H-benzo[d]imidazole (1b) or quinazoline (1c).

12 f appropriate polar functional groups at the quinazoline 2-position, thus separating the F16Bpase inh

13 properties make the N(2),N(4)-disubstituted quinazoline-2,4-diamine compound series a suitable platf

14 A series of N(2),N(4)-disubstituted quinazoline-2,4-diamines has been synthesized and tested

15 A series of N(2),N(4)-disubstituted quinazoline-2,4-diamines has been synthesized and tested

16 he identification of N(2),N(4)-disubstituted quinazoline-2,4-diamines with minimum inhibitory concent

17 llowing main TPs: 1-(2-benzoic acid)-(1H,3H)-quinazoline-2,4-dione (BaQD), 1-(2-benzoic acid)-(1H,3H)

18 Methyl 9-anilinothiazolo[5,4-f]quinazoline-2-carbimidates 1 (EHT 5372) and 2 (EHT 1610)

19 d nonoxidative coupling of 4-(2-bromoanilino)quinazoline-2-carbonitrile; and (3) a nonoxidative Pd(Ar

20 2,4-dione (BaQD), 1-(2-benzoic acid)-(1H,3H)-quinazoline-2-one (BaQM), 9-aldehyde-acridine, 9-carboxy

21 osition 137, and the acceptor 4-aminobenzo[g]quinazoline-2-one (Cf) in lieu of cytidine22 in the i-mo

22 pirocyclic molecule, spiro[3H-indole-3,2'(1H)quinazoline]-2,4'(1H,3H)dione 8, which was also identifi

23 Quinazoline 23 also displayed efficacy in a murine model

24 the synthesis of a series of pyrazolo[1,5-a]quinazoline 3- and/or 8-substituted as 5-deaza analogues

25 to provide access to the core pyrazino[2,1-b]quinazoline-3,6-dione (1) scaffold, which is common to s

26 zoline compound, ethyl 5-aminopyrazolo[1,5-a]quinazoline-3-carboxylate, that specifically inhibits ad

27 inoxaline moiety in the lead compound (1) by quinazoline (4a-d), 1,2,4-benzotriazine (12a-18b), and q

28 Quinazoline 54 and pyrido[3,4-d]pyrimidine 71 were ident

29 tion and ring expansion to quinazolino[4,5-b]quinazoline-6,8-dione 7 rather than, as previously belie

30 Benzo[4,5]imidazo[1,2-c]quinazoline-6-carbonitriles are prepared in high yields

31 xy)-ethoxy}-ethoxy] -ethoxy)-ethoxy}-ethoxy]-quinazoline-6-yl-acrylamide ([(18)F]F-PEG6-IPQA), a radi

32 xy)-ethoxy}-ethoxy]- ethoxy)-ethoxy}-ethoxy]-quinazoline-6-yl-acrylamide) ((18)F-PEG(6)-IPQA) for non

33 es, 2-amino-4-(2'-deoxy-beta-D-ribofuranosyl)quinazoline (7) and 2-amino-6-fluoro-4-(2'-deoxy-beta-D-

34 rivatives of benzo[h]quinoline 6 and benzo[h]quinazoline 7a-e as mixed analogues of archetypal 1,8-bi

35 each case, the nitrogen at position-1 of the quinazoline accepted a hydrogen bond from a backbone NH

36 er doxazosin and terazosin (both piperazinyl quinazolines) affect prostate growth via an alpha1-adren

37 Vasicine, an abundantly available quinazoline alkaloid from the leaves of Adhatoda vasica,

38 l-Vasicine is a quinazoline alkaloid with an electron dense ring and add

39 d guanidines termed "lockamers" (cyclophane, quinazoline, aminopyrimidazolines, aminoimidazolines, az

40 In the 2,5-dimethoxybenzylamino substituted quinazoline analogues, replacement of the N9-CH 3 group

41 The net conversion of potent quinazoline and benztriazine inhibitors to cyanoquinolin

42 From models of SD complexed to quinazoline and benztriazine inhibitors, a new class of

43 of fluorescent nucleosides analogues such as quinazoline and oxophenothiazine that should find broad

44 We have developed potent quinazoline and pyrido-[3,4-d]-pyrimidine small molecule

45 rally related to 2-amino-4-oxo-5-substituted quinazolines and 2-amino-4-oxo-5-substituted pyrrolo[2,

46 pyrimido[1,6-a]benzimidazole, pyrimido[1,6-a]quinazoline, and pyrimido[1,6-a]benzo[b]6-bora-1,3-diazi

47 2, and erbB4 were determined for a series of quinazoline- and pyrido[3,4-d]pyrimidine-based analogues

48 ined for a series of alkynamide analogues of quinazoline- and pyrido[3,4-d]pyrimidine-based compounds

49 ut screening recently identified substituted quinazolines as potent SMN2 inducers.

50 ization can be induced by the interaction of quinazolines at the ATP site in the absence of receptor

51 ucture-property relationship studies on this quinazoline ATM kinase inhibitor in order to identify st

52 Previous evidence showed the ability of the quinazoline-based alpha(1)-adrenoreceptor antagonist dox

53 ic threshold of prostate cancer cells to the quinazoline-based alpha1-adrenoceptor antagonist doxazos

54 ntial therapeutic significance in the use of quinazoline-based alpha1-adrenoceptor antagonists (alrea

55 evidence that the apoptotic activity of the quinazoline-based alpha1-adrenoceptor antagonists (doxaz

56 Quinazoline-based alpha1-adrenoceptor antagonists such a

57 Recent evidence suggests that the quinazoline-based alpha1-adrenoceptor antagonists, doxaz

58 tive prostate cancer cells, LNCaP, to either quinazoline-based alpha1-agonist by androgens.

59 cycle perturbation in response to ZD1694, a quinazoline-based antifolate thymidylate synthase inhibi

60 This new class of quinazoline-based compounds provides considerable promis

61 FR inhibitors possess a structurally related quinazoline-based core scaffold and were identified as A

62 We have discovered a novel series of quinazoline-based CXCR4 antagonists.

63 old less potent against wild-type EGFR, than quinazoline-based EGFR inhibitors in vitro.

64 ions that are sensitive to existing covalent quinazoline-based EGFR/HER2 inhibitors, with implication

65 substituted with bulky groups, we developed quinazoline-based imaging tools by fluorescently labelin

66 Tandutinib (MLN518/CT53518) is a novel quinazoline-based inhibitor of the type III receptor tyr

67 es to dacomitinib and afatinib, two covalent quinazoline-based inhibitors of EGFR or HER2, respective

68 The model suggests that with the quinazoline-based inhibitors, the N3 atom is hydrogen-bo

69 lly more effective and better tolerated than quinazoline-based inhibitors.

70 ng ATP concentrations suggest that, like the quinazoline-based kinase inhibitors, the pyrrolotriazine

71 h led to the development of a class of lead (quinazoline-based) compounds with higher potency than do

72 BGC 945 is a cyclopenta[g]quinazoline-based, thymidylate synthase inhibitor specif

73 The NF-kappaB inhibitor quinazoline blocked p65 nuclear translocation and furthe

74 copper is overcome by 2-(6-benzyl-2-pyridyl)quinazoline (BPQ), providing a chemical-biology tool whi

75 chloro-2-(2-furyl)-1, 2, 4-triazolo [1, 5-c] quinazoline (CGS-15943).

76 e describe the optimization of the 2-anilino quinazoline class as antimalarial agents.

77 The quinazoline class was exploited to search for a new tran

78 Two of the compound classes, a quinazoline compound series and an indole compound, also

79 24 compounds tested, we have identified one quinazoline compound, ethyl 5-aminopyrazolo[1,5-a]quinaz

80 Here, we report a novel small molecule quinazoline compound, Inh2-B1, which specifically inhibi

81 hips (SAR) of a series of (iso)quinoline and quinazoline compounds that were synthesized and screened

82 lded a high selectivity toward ABCG2 for the quinazoline compounds.

83 stal structures of EphB3 in complex with two quinazolines confirmed the covalent linkage between the

84 ing of gene clusters for benzodiazepine- and quinazoline-containing polycyclic alkaloids with a wide

85 group of indole alkaloids which include the quinazoline-containing tryptoquivaline (2) that are capa

86 tructural class containing a 2-(pyridin-2-yl)quinazoline core has been discovered.

87 ubstitution in the 6- and 7-positions of the quinazoline core structure decreased potency.

88 te that despite chemical modification to the quinazoline core these probes still function as ERBB2 in

89 Extension of the aromatic quinazoline core with fluorophore "arms" through substit

90 rough substitution at the 6- position of the quinazoline core with phenyl, styryl, and phenylbutadien

91 modification to the metabolized site on the quinazoline core.

92 ional analysis dealing with N-methyl-NAHs, a quinazoline derivative (19) was designed as a conformati

93 ptophan derivatives of 1, including a unique quinazoline derivative (9).

94 In summary, the C5-quinazoline derivative D156844 increases SMN expression

95 Finally, a quinazoline derivative suitable to serve as a photoaffin

96 ll arylvinyl (styryl), aryl, and arylethynyl quinazoline derivatives by means of different straightfo

97 urvival mechanism, we developed new thiourea quinazoline derivatives that are dual inhibitors of both

98 s of new 6-substituted-4-(3-bromophenylamino)quinazoline derivatives that may function as irreversibl

99 An efficient protocol for the synthesis of quinazoline derivatives through nickel-catalyzed ligand-

100 inal agents to treat proliferative diseases, quinazoline derivatives were synthesized and evaluated p

101 A series of C5-quinazoline derivatives were tested for their ability to

102 is class of compounds led to a new series of quinazoline derivatives with single-digit nanomolar pote

103 ional studies on an "in-house" collection of quinazoline derivatives, featuring highly steric demandi

104 AR agonists in a group of 2-(3-methoxyphenyl)quinazoline derivatives.

105 SAR optimization campaign around a series of quinazoline derived BRAF(V600E) inhibitors.

106 Previous studies documented that the quinazoline-derived alpha1-adrenoceptor antagonist doxaz

107 Here, we show that BIBW2992, an anilino-quinazoline designed to irreversibly bind EGFR and HER2,

108 e use of high concentrations of irreversible quinazoline EGFR inhibitors such as PF299804.

109 inhibitors, methotrexate, flavopiridol, and quinazoline ErbB1 inhibitors.

110 Diprotonated pyrimidines, quinoxalines, and quinazolines exhibit an unusual regioelectronic effect t

111 n of an HSP70 enzyme, which yielded an amino-quinazoline fragment that was elaborated to a novel ATP

112 he order of 5-isoquinoline > 8-quinoline = 8-quinazoline > 8-isoquinoline > or = cinnoline approximat

113 2+2+2) modular synthesis of multisubstituted quinazolines has been realized by the direct reaction of

114 compounds, leading to the green synthesis of quinazolines in water.

115 In SKBR-3 cells, the quinazolines induced the formation of inactive EGFR/ErbB

116 Quinazoline-induced EGFR dimerization was abrogated in v

117 We have used quinazoline inhibitors of the epidermal growth factor re

118 Here we report a novel class of GCase quinazoline inhibitors, obtained in a high throughput sc

119 Structural studies of the quinazoline interaction with the EGFR tyrosine kinase do

120 adical-based method of making functionalized quinazolines is described, which relies on microwave-pro

121 potent selective small molecule piperazinyl quinazoline kinase inhibitor of the PDGFR, was identifie

122 late which effectively mimics the well-known quinazoline kinase inhibitor scaffold.

123 Crystal structures of amino-quinazoline ligands bound to the different conformationa

124 p27 protein in A431 cells and abrogated the quinazoline-mediated G(1) arrest.

125 cysteine residue and that our electrophilic quinazolines modulate the function of V-ATPase in cells.

126 The structure with CB3717 reveals that the quinazoline moiety binds in similar fashion to the pteri

127 ent screens also identified several new lead quinazoline Mps1 inhibitors, including a low-affinity co

128 illus fumigatus Af293 is a known producer of quinazoline natural products, including the antitumor fu

129 antibody, or NF-kappaB activation inhibitor quinazoline (NF-kappaB-I).

130 rase I (Top1) inhibitors, the pyrazolo[1,5-a]quinazoline nucleus, structurally related to the indenoi

131 nd high proteomic specificity, the described quinazolines offer a powerful set of chemical probes to

132 Consistent with the inhibitory effect of quinazolines on receptor kinase activity, the dimers for

133 as isoquinolines, quinoline, phenanthridine, quinazoline, phthalazine, and beta-carboline, and electr

134 This approach resulted in quinazoline-quinoline derivatives as potent inhibitors o

135 ociated with sensitivity to first generation quinazoline reversible EGFR tyrosine kinase inhibitors (

136 Likewise, similar groups on the quinazoline ring also reduced inhibitory activity.

137 e with the phenyl group perpendicular to the quinazoline ring and positioned in the region of the act

138 ds, which are characterized by an acetylated quinazoline ring connected to a 6-5-5 imidazoindolone ri

139 nist NECA 3 and the 1H-[1,2,4]triazolo[1,5-c]quinazoline ring in antagonist CGS15943 1 overlapped, an

140 of Asn-221 still hydrogen bonds to N3 of the quinazoline ring of CB3717, which must be in the enol fo

141 d compound was essentially coplanar with the quinazoline ring system and occupied a pocket between Ly

142 he phenyl group oriented in the plane of the quinazoline ring system and positioned adjacent to the C

143 inazoline was bound in the ATP site with the quinazoline ring system oriented along the peptide stran

144 5,16-hexahydroazepino[4',5':2,3]indolo[1,2-c]quinazoline ring system that has not previously been syn

145 of biologically active compounds contain the quinazoline ring system.

146 e, [1,2,5]-thiadiazolo[3,4-d]pyrimidine, and quinazoline ring systems and evaluated for their ability

147 Several compounds, including quinazoline ring-containing compounds, have been identif

148 preparation of several replacements for the quinazoline scaffold and report these inhibitors' biolog

149 tivity relationship (SAR) exploration of the quinazoline scaffold represented by BIX01294 (1).

150 For comparison, the quinazoline scaffold was reduced to the significantly sm

151 Some of the electrophilic quinazolines selectively and potently inhibited EphB3 bo

152 um for activity in both the isoquinoline and quinazoline series.

153 hown excellent inhibition of TS and, for the quinazoline, significant promise as clinically useful an

154 ubstitution in the 6- and 7-positions of the quinazoline, so that 32 is not the optimal inhibitor for

155 molar concentrations of AG-1478 and AG-1517, quinazolines specific for inhibition of the EGFR kinase,

156 e rapid assembly of either benzimidazoles or quinazolines starting from aryl- or benzyl-substituted c

157 ossessing combinations of similar phenyl and quinazoline substituents do not show this "supra-additiv

158 developed through modifications of the novel quinazoline template I.

159 those employing a therapeutically validated quinazoline template.

160 We have discovered electrophilic quinazolines that covalently modify a soluble catalytic

161 ve method for the synthesis of 2-substituted quinazolines through an oxidative workup step.

162 and characterized a series of electrophilic quinazolines to target this unique, reactive feature in

163 ZD1839 ("Iressa"), a quinazoline tyrosine kinase inhibitor selective for the

164 ophenones, acridinones and quinazolinones or quinazolines was identified and measured by liquid chrom

165 s active compound, a series of 2-substituted quinazolines was synthesized and evaluated in several an

166 , NSC194598, a derivative of indeno[1,2,3-de]quinazoline, was found to be a novel G-quadruplex intera

167 A series of 7,8-dialkylpyrrolo[3,2-f]quinazolines were prepared as inhibitors of dihydrofolat

168 uded in the reaction mixture, fully aromatic quinazolines were produced in high yields by a rapid and

169 y acylation of 6-amino-4-(3-bromophenylamino)quinazoline with unsaturated acid chlorides or mixed anh

170 This study led to the identification of quinazolines with EC50 values in the single digit microm