- Synthesis and anti-proliferative activity of substituted- anilinoquinazolines and its relation to EGFR inhibition
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4-Anilinoquinazoline is a privileged scaffold in developing small molecule inhibitors of tyrosine kinases (TK) especially epidermal growth factor receptor (EGFR). 2 series belonging to 3'-substituted-4-anilinoquinazoline scaffold were synthesized and screened in vitro on isolated and a breast cancer cell line. The research aims at exploring the activity of compounds having diverse substituents at 3' position of the aniline moiety. Generally, the meta-substituted-anilinoquinazolines exhibited significant inhibitory activity against isolated enzyme as well as MCF-7 cancer cell line. For instance, compound 10b inhibited >99% of EGFR activities at 10 M concentration. 6 of the tested compounds exhibited range of anti-proliferative activity below 10 M potency. In particular, compounds 6e and 10b displayed the highest activity among the tested compounds with IC50 values equal to 8.6 and 4.84 M, respectively. Structure-based tools were utilized to rationalize EGFR-TK binding of compound 10b since it is the most active compound in the enzyme inhibition test. Georg Thieme Verlag KG Stuttgart.New York.
- El Ella,Saleh,Hassan,Hamdy,El-Araby,Abouzid
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p. 360 - 366
(2012/10/29)
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- Pyrrolopyrimidine Compounds and Their Uses
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The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrrolopyrimidine compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.
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Page/Page column 46
(2009/12/28)
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- 2-Pyrimidinyl Pyrazolopyridine Erbb Kinase Inhibitors
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The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.
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Page/Page column 54
(2008/06/13)
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- TRIAZOLE DERIVATIVES USEFUL AS AXL INHIBITORS
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Triazole derivatives and pharmaceutical compositions containing the derivatives are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the derivatives in treating diseases or conditions associated with Axl catalytic activity are also disclosed.
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Page/Page column 152-153
(2010/11/26)
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- CYCLOPENTENE DERIVATIVES USEFUL AS ANTAGONISTS OF THE MOTILIN RECEPTOR
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The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor disorders. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.
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- Novel substituted diamine derivatives useful as motilin antagonists
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The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the speci
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- 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines
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This disclosure describes novel 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines having anti-asthmatic activity.
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