264208-72-2Relevant articles and documents
QUINAZOLINE COMPOUND SERVING AS EGFR TRIPLE MUTATION INHIBITOR AND APPLICATIONS THEREOF
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, (2021/02/18)
Related to a quinazoline compound serving as an EFGR triple mutation inhibitor and applications thereof. Specifically, disclosed are a compound as represented by the following formula (I), a pharmaceutical composition comprising the compound of formula (I
Anilinoquinazoline inhibitors of the RET kinase domain - Elaboration of the 7-position
Jordan, Allan M.,Begum, Habiba,Fairweather, Emma,Fritzl, Samantha,Goldberg, Kristin,Hopkins, Gemma V.,Hamilton, Niall M.,Lyons, Amanda J.,March, H. Nikki,Newton, Rebecca,Small, Helen F.,Vishwanath, Swamy,Waddell, Ian D.,Waszkowycz, Bohdan,Watson, Amanda J.,Ogilvie, Donald J.
, p. 2724 - 2729 (2016/05/09)
We have previously reported a series of anilinoquinazoline derivatives as potent and selective biochemical inhibitors of the RET kinase domain. However, these derivatives displayed diminished cellular potency. Herein we describe further optimisation of the series through modification of their physicochemical properties, delivering improvements in cell potency. However, whilst cellular selectivity against key targets could be maintained, combining cell potency and acceptable pharmacokinetics proved challenging.
A novel approach to quinazolin-4(3H)-one via quinazoline oxidation: an improved synthesis of 4-anilinoquinazolines
Marzaro, Giovanni,Guiotto, Adriano,Pastorini, Giovanni,Chilin, Adriana
experimental part, p. 962 - 968 (2010/03/25)
A novel strategy to prepare 4-anilinoquinazoline derivatives based on the oxidation of the quinazoline ring is described. Quinazoline oxidation has been investigated and improved, thus leading to an efficient and high yielding method to quinazolin-4(3H)-ones. Efficiency of this approach has been evaluated synthesizing four well known tyrosine kinase inhibitors and comparing the obtained yields with those achievable through conventional synthetic methods.