Synthesis and biological evaluation of allenic quinazolines using palladium-catalyzed hydride-transfer reaction
Synthesis and biological evaluation of allenic quinazolines using palladium-catalyzed hydride-transfer reaction
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DOI：
10.1016/j.tetlet.2006.02.043
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发表时间：
2006-04-10
影响因子：
1.8
通讯作者：
Onagi, S
中科院分区：
文献类型：
--
作者：
Nakamura, H;Onagi, S
Allenic quinazolines 13a-h were designed as mimics of Tarceva, which is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, and synthesized from the corresponding 4-(iodoanilino)quinazolines or 4-(iodophenoxy)quinazolines with N,N-dicyclohexylprop-2-ynylamine by the Sonogashira coupling followed by palladium-catalyzed hydride-transfer reaction. Cell growth inhibition of 13a-h toward A431, Kato III, SKBR3, and HepG2 was examined. Among the compounds synthesized, 13a showed a similar cell growth inhibition to Tarceva. Moreover, 13d and 13h exhibited a specific growth inhibition toward Kato III cells (IC50 = 12 and 4.7 mu M, respectively), although a significant inhibition toward other three cell lines was not observed at a 100 mu M concentration of compounds. (c) 2006 Elsevier Ltd. All rights reserved.
