52791-04-5Relevant articles and documents
1,4-Dioxane-fused 4-anilinoquinazoline as inhibitors of epidermal growth factor receptor kinase
Lee, Jae Yeol,Park, Yong Kyu,Seo, Seon Hee,So, In-Seop,Chung, Hee-Kyung,Yang, Beom-Seok,Lee, Sook Ja,Park, Hokoon,Lee, Yong Sup
, p. 357 - 360 (2001)
The 4-anilinoquinazoline PD 153035 (1) is a potential antitumor agent which acts by inhibiting tyrosine kinase activity of epidermal growth factor receptor (EFGR) via competitive binding at the ATP site of enzyme. A series of cyclic analogues of PD 153035 bearing the 1,4-dioxane ring was prepared by reaction of 6-chloro derivative 5 with several aniline nucleophiles. These were evaluated for their ability to inhibit the EGFR kinase and the growth of primary human tumor cell cultures. All of the new 4-anilinoquinazolines exhibited less potency than PD 153035 against EGFR kinase. However, compounds 2b, 2c, 2e, 2g, and 2h showed higher inhibitory activities than PD 153035 against the growth of A431 tumor cell line. The compound 2b containing 3-chloroaniline ring was as potent as PD 153035 against EGFR kinase and showed about 5.4-fold better potency than PD1 53035 in the inhibition of growth of A431 cell line with good selectivity.
Quinazoline-based multi-tyrosine kinase inhibitors: Synthesis, modeling, antitumor and antiangiogenic properties
Conconi, Maria Teresa,Marzaro, Giovanni,Urbani, Luca,Zanusso, Ilenia,Di Liddo, Rosa,Castagliuolo, Ignazio,Brun, Paola,Tonus, Francesca,Ferrarese, Alessandro,Guiotto, Adriano,Chilin, Adriana
, p. 373 - 383 (2013/10/01)
In this work the synthesis and the biological evaluation of some novel anilinoquinazoline derivatives carrying modifications in the quinazoline scaffold and in the aniline moiety were reported. Preliminary cytotoxicity studies identified three derivatives
QUINAZOLINE DERIVATIVES AS RAF KINASE MODULATORS AND METHODS OF USE THEREOF
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Page/Page column 178, (2009/10/22)
Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.