- Synthesis and biological evaluation of allenic quinazolines using palladium-catalyzed hydride-transfer reaction
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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 μM, respectively), although a significant inhibition toward other three cell lines was not observed at a 100 μM concentration of compounds.
- Nakamura, Hiroyuki,Onagi, Shinya
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p. 2539 - 2542
(2007/10/03)
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- Quinazoline compounds and pharmaceutical compositions containing them
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The use of a compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, NH or NR8 where R8 is hydrogen or C1-6alkyl; Ra is a 3-quinoline group or a group of sub-formula (i) where R5, R6 and R7 are various specific organic groups, in the preparation of a medicament for use in the inhibtion of aurora 2 kinase. Novel compounds of formula (I) and pharmaceutical compositions useful in the treatment of cancer are also described and claimed.
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Page/Page column 37
(2008/06/13)
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- QUINAZOLINE DERIVATIVES
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A compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2 or NR10 where R10 is hydrogen or C1-6 alkyl, and R1, R2, R3, R4, R5, R6, R7, R8 and R9 are various specified organic groups. These compounds are inhibitors of aurora 2 kinase, and are useful in the treatment of cancer.
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Page/Page column 14
(2008/06/13)
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