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Synthesis and initial SAR studies of 3,6-disubstituted pyrazolol[1,5-a]pyrimidines:: A new class of KDR kinase inhibitors

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 12, 期 19, 页码 2767-2770

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(02)00525-5

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We have synthesized and evaluated the activity of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines as a new class of KDR kinase inhibitors. Starting with screening lead 1, potency against isolated KDR was fully optimized with 3-thienyl and 4-methoxyphenyl substituents at the 6- and 3-positions (3g, KDR IC50 = 19 nM), respectively. The synthesis and SAR of these compounds are described. (C) 2002 Elsevier Science Ltd. All rights reserved.

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