1007207-65-9Relevant academic research and scientific papers
Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability
Kawada, Hatsuo,Ebiike, Hirosato,Tsukazaki, Masao,Yamamoto, Shun,Koyama, Kohei,Nakamura, Mitsuaki,Morikami, Kenji,Yoshinari, Kiyoshi,Yoshida, Miyuki,Ogawa, Kotaro,Shinma, Nobuo,Tsukuda, Takuo,Ohwada, Jun
, p. 7650 - 7660 (2015/12/18)
Phosphoinositide 3-kinase (PI3K) is activated in various human cancer cells and well known as a cancer therapy target. We previously reported a dihydropyrrolopyrimidine derivative as a highly potent PI3K inhibitor that has strong tumor growth inhibition in a xenograft model. In this report, we describe further optimization to improve its bioavailability.
PYRROLOPYRIMIDIN DERIVATIVE FOR USE AS PI3K INHIBITOR, AND USE THEREOF
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Page/Page column 31-32, (2010/11/03)
A preventive or therapeutic agent of a proliferative disease such as cancer, having superior PI3K inhibitory effects, superior cell proliferation inhibitory action as well as superior stability in a body and water solubility, is provided. A compound represented by formula (I): [wherein, Q represents a linking group represented by -X-Y-; X represents a single bond -CO-, -CONH-, -CON(C1-4 alkyl)-, -CS-, -CSNH-, -CSN(C1-4 alkyl)-, or -SO2-; Y represents a single bond, arylene or heteroarylene; provided that X and Y are not simultaneously single bonds; and R1 represents -C0-6 alkylene-(A)m-C1-6 alkyl, or C0-6 alkylene-(A)m-C0-6 alkylene-(heterocycle)] or a pharmaceutically acceptable salt thereof.
