ライフサイエンスコーパス: aminopyrimidine

1 2-aminopyridine) and (R) in (26IO)3 (from 2-aminopyrimidine).

2 he substitution of the indazole in 1 for a 2-aminopyrimidine.

3 of the commercially available 4,6-dichloro-5-aminopyrimidine 1 with isothiocyanates.

4 -6-aminopyrimidines 4 via glycosylation of 4-aminopyrimidines 2 or 5 is described.

5 Silylated 4-aminopyrimidines 2 or 5 upon ribosylation with 1 provide

6 A family of sequence-related 2'-aminopyrimidine, 2'-hydroxylpurine aptamers, developed b

7 yrimidin-4-amines 3 or 4-(N-ribofuranosyl)-6-aminopyrimidines 4 via glycosylation of 4-aminopyrimidin

8 tivity of 4-mercaptophenylboronic acid and 2-aminopyrimidine-5-boronic acid was assessed with cis-1,2

9 sts for the fabrication of a wide range of 4-aminopyrimidine-5-carbonitrile derivatives (33 examples)

10 h the aid of X-ray structure-based analysis, aminopyrimidine amides 2 and 3 were designed from aminoq

11 -activity relationships of a series of novel aminopyrimidine amides 3 possessing improved cellular po

12 ns to design and synthesize a new library of aminopyrimidine analogues targeting site-2 of the plecks

13 s led to hybrid molecules which incorporated aminopyrimidine and aminopyridine moieties with ATP mime

14 The ability to detect both the aminopyrimidine and iminopyrimidine tautomeric forms of

15 of anti-Cdk inhibitors, we synthesized aryl aminopyrimidines and examined the effect of these compou

16 teroaromatic amines such as aminopyridine, 2-aminopyrimidine, and aminoquinoline to provide diverse m

17 arylglyoxal monohydrates, 2-aminopyridines/2-aminopyrimidine, and barbituric/N,N-dimethylbarbituric a

18 olism, is comprised of the thiazolium and 4'-aminopyrimidine aromatic rings, but only recently has pa

19 n electrophilic covalent catalyst and the 4'-aminopyrimidine as acid-base catalyst involving its 1',4

20 both rings of ThDP in YPDC catalysis (the 4'-aminopyrimidine as acid-base, and thiazolium as electrop

21 we describe the discovery of (4-pyrazolyl)-2-aminopyrimidines as a potent class of CDK2 inhibitors th

22 , we discovered a new class of highly potent aminopyrimidine-based B-Raf inhibitors with improved sol

23 In a designed series of aminopyrimidine-based inhibitors, we unexpectedly encoun

24 Here we have optimized 2-aminopyrimidine-based macrocycles to use these compounds

25 in described is the discovery of a series of aminopyrimidine-based selective CDK4 inhibitors.

26 based core differs structurally from that of aminopyrimidine-based third-generation EGFR inhibitors a

27 We hypothesized that nonexemplified aminopyrimidines bearing side chains from well-annotated

28 s, and pharmacological characterization of 2-aminopyrimidine carbamates, a new class of compounds wit

29 a focus on the functional profiling of the 2-aminopyrimidine chemotype that has advanced to the clini

30 The aminopyrimidine compounds were reported to disrupt dynam

31 to D2/D3 and 5-HT1A receptor binding of the aminopyrimidine, cycloalkyl, and phenylpiperazine portio

32 We have identified an aminopyrimidine derivative (CYT387), which inhibits JAK1

33 of the carbamate led to the highly potent 2-aminopyrimidine derivative 20j with a significantly impr

34 investigation, we describe novel substituted aminopyrimidine derivatives that inhibit human GSK-3 pot

35 e discovery and SAR of a series of 6-alkyl-2-aminopyrimidine derived histamine H4 antagonists that le

36 tennimide crystal structure (26IO)4 (from 2-aminopyrimidine) exhibits three discrete conformational

37 ocycle (d2APy) while the second contains a 2-aminopyrimidine heterocycle (d2APm).

38 of an arylaldehyde, nitromethane, and the 6-aminopyrimidine in acetic acid containing ammonium aceta

39 et out to investigate whether mildly basic 2-aminopyrimidines in combination with the appropriate lin

40 alyzed by the KOBu(t)/DMSO system leads to 2-aminopyrimidines in up to 80% yield.

41 as been also extended to 2-aminopyridines, 2-aminopyrimidine, indole, and isoquinoline with moderate

42 the optimization of highly ligand efficient aminopyrimidine lead compounds.

43 ut only recently has participation of the 4'-aminopyrimidine moiety in catalysis gained wider accepta

44 midines, the introduction of an additional 2-aminopyrimidine moiety in combination with the appropria

45 s that a chain of residues connecting the 4'-aminopyrimidine N1' atoms of thiamin diphosphates (ThDPs

46 des and an alkyne hydroamination employing 2-aminopyrimidine nucleophiles.

47 l also prefer this tautomer, and that the 4'-aminopyrimidine of ThDP participates in multiple steps o

48 ng the addition of SO(3)(2-) to C6' of the 4-aminopyrimidine of thiamin has also been proposed.

49 ctive pan-ErbB kinase inhibitor from a novel aminopyrimidine oxime structural class that blocks the p

50 An aminopyrimidine, PNU 112455A, was identified in a screen

51 thaloyl dichloride with 2-aminopyridine or 2-aminopyrimidine provides a facile entry into a new class

52 hese results suggest that biaryl substituted aminopyrimidines represented by compound 9l may serve as

53 ture-activity relationships of substituted 2-aminopyrimidines, representing a new class of reversible

54 by reaction of 2-aminopyridines or 2-(or 4-)aminopyrimidines, respectively, with 1,2-bis(benzotriazo

55 the 1',4'-iminopyrimidine tautomer of the 4'-aminopyrimidine ring in thiamin diphosphate.

56 binds a water molecule and points toward the aminopyrimidine ring of ThDP.

57 crystallographic studies suggest that the 4'-aminopyrimidine ring of the thiamin diphosphate coenzyme

58 odels for the 1',4'-imino tautomer of the 4'-aminopyrimidine ring of thiamin diphosphate recently fou

59 ntify the various tautomeric forms of the 4'-aminopyrimidine ring on four thiamin diphosphate enzymes

60 and three conserved hydrogen bonds to the 4'-aminopyrimidine ring to enforce the V conformation, even

61 f covalent bond formation and response in 4'-aminopyrimidine ring's tautomeric state to intermediate

62 is hydrogen bonded to the N1' atom of the 4'-aminopyrimidine ring), as well as its position are consi

63 t the identification of such a molecule - an AminoPYrimidine-Sulfonamide (APYS1) that has potent, bac

64 a charge-transfer transition between the 4'-aminopyrimidine tautomer (presumed electron donor) and t

65 oism band characteristic of the canonical 4'-aminopyrimidine tautomer of bound thiamin diphosphate (A

66 y, both the 1',4'-iminopyrimidine and the 4'-aminopyrimidine tautomers coexist on the E1 component of

67 ed with the discovery of a compound with a 2-aminopyrimidine template that targeted the Wnt beta-cate

68 emissive adenosine analogue thieno[3,4-d]-6-aminopyrimidine ((th)A).

69 sly identified a series of 4,6-substituted 2-aminopyrimidines that associate with this soluble surrog

70 ts and from the previously analyzed set of 2-aminopyrimidines that displayed distinct cooperative int

71 In the series of 2-aminopyrimidines, the introduction of an additional 2-am

72 behavior of a number of 4,6-disubstituted 2-aminopyrimidines to Lymnaea AChBP, with different molecu

73 binding to the enzymes activates both the 4'-aminopyrimidine (via pK(a) elevation) and the thiazolium

74 A series of 2-aminopyrimidines was synthesized as ligands of the hista

75 DC-0941) as templates, (thienopyrimidin-2-yl)aminopyrimidines were discovered as potent inhibitors of

76 ivity relationships (SAR) around a series of aminopyrimidines were evaluated utilizing biochemical an

77 modular sequences from 2-aminopyridine and 2-aminopyrimidine wherein aminations of intermediate pyri(

78 The screening identified an aminopyrimidine with affinity in the high micromolar ran

79 of a series of over 50 newly characterized 2-aminopyrimidines with affinity for AChBP showed only two

80 emerged from the structural modification of aminopyrimidine XCT0135908.

81 rporated into design of a second subset of 2-aminopyrimidines yielding several congeners that elicite