ライフサイエンスコーパス: anilinoquinazoline

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1 [PhI(OTf)2] mediated oxidative coupling of 4-anilinoquinazoline-2-carbonitriles in neat trifluoroacet

2 The 4-anilinoquinazoline (4-AQ) derivative gefitinib (Iressa)

3 of pp60(c-src) tyrosine kinase (Src TK) by 4-anilinoquinazolines, an important class of chemicals as

4 , a direct comparison between 6-acrylamido-4-anilinoquinazoline and an equally potent but reversible

5 y, efforts have been made to develop novel 4-anilinoquinazoline and pyridopyrimidine derivatives to i

6 rugs in the trypanosome, and (b) offer the 4-anilinoquinazoline and pyrrolopyrimidines as scaffolds w

7 ial for the apoptosis-inducing activity of 4-anilinoquinazolines and substitution in the 6- and 7-pos

8 ity relationships (SAR) of a novel series of anilinoquinazolines as allosteric inhibitors of fructose

9 In contrast to the SAR of 4-anilinoquinazolines as EGFR kinase inhibitors, the methy

10 ssay, we have identified a novel series of 4-anilinoquinazolines as inducers of apoptosis.

11 ure-activity relationship (SAR) studies on 4-anilinoquinazolines as potent apoptosis inducers and to

12 F-R kinase with activity comparable to the 4-anilinoquinazoline-based inhibitors.

13 The 4-anilinoquinazolines canertinib and lapatinib, and the py

14 nvestigation is ZD1839 (Iressa), a synthetic anilinoquinazoline capable of inhibiting EGFR tyrosine k

15 inhibitors (TKIs), such as members of the 4-anilinoquinazoline class, competes for ATP binding.

16 mall-cell lung cancer who have a response to anilinoquinazoline EGFR inhibitors.

17 hat has led to synthesis of several potent 4-anilinoquinazolines, including NEU617, 23a, a highly pot

18 Here we show that CI-1033 and related 4-anilinoquinazolines inhibit SPGF-induced human cellular

19 n with and without an EGFR kinase-specific 4-anilinoquinazoline inhibitor (erlotinib, Tarceva), we hy

20 We demonstrated recently that the 4-anilinoquinazolines lapatinib (GW572016, 1) and canertin

21 3-aminopropanamide linked in position 6 to 4-anilinoquinazoline or 4-anilinoquinoline-3-carbonitrile

22 different SAR as inhibitors of F16Bpase than anilinoquinazolines previously reported.

23 4-Anilinoquinazolines represent an important class of prot

24 he selectivity profile of molecules in the 4-anilinoquinazoline series can be modified through specif

25 istant clones are cross-resistant to related anilinoquinazolines, they demonstrate sensitivity to a c

26 Previously, 4-anilinoquinazoline TKIs have been shown to inhibit the f

27 In both inhibitor/kinase structures, the 4-anilinoquinazoline was bound in the ATP site with the qu

28 4-Anilinoquinazolines with a bulky group at the 4'-positio

29 itors ZD1839 (Iressa) or PD153035, synthetic anilinoquinazolines with high specificity for EGFR, resu

30 pyrimidine PP1 and the clinically relevant 4-anilinoquinazoline ZD6474.

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