Pharmacophore generation and atom-based 3D-QSAR of novel 2-(4-methylsulfonylphenyl)pyrimidines as COX-2 inhibitors
β Scribed by Ujashkumar A. Shah; Hemantkumar S. Deokar; Shivajirao S. Kadam; Vithal M. Kulkarni
- Publisher
- Springer
- Year
- 2009
- Tongue
- English
- Weight
- 804 KB
- Volume
- 14
- Category
- Article
- ISSN
- 1381-1991
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A series of seven nonclassical three carbon atom bridged 2,4-diamino-5-substituted-pyrrolo[2,3-d]pyrimidines 1a-g were synthesized as potential inhibitors of dihydrofolate reductase. Selective oxidation of diols 7a-g affords Ξ±-hydroxy ketones 8a-g. Subsequent condensation with malononitrile gave the
## Abstract Receptor tyrosine kinases such as VEGFR2 (vascular endothelial growth factor receptor 2, KDR) or EGFR (epidermal growth factor receptor) play crucial roles in a variety of diseases, such as cancer. Recently, some pyrrolopyrimidines were shown to be potent EGFR inhibitors. Therefore, new