886499-03-2Relevant articles and documents
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer
Shirai, Fumiyuki,Mizutani, Anna,Yashiroda, Yoko,Tsumura, Takeshi,Kano, Yuko,Muramatsu, Yukiko,Chikada, Tsubasa,Yuki, Hitomi,Niwa, Hideaki,Sato, Shin,Washizuka, Kenichi,Koda, Yasuko,Mazaki, Yui,Jang, Myung-Kyu,Yoshida, Haruka,Nagamori, Akiko,Okue, Masayuki,Watanabe, Takashi,Kitamura, Kouichi,Shitara, Eiki,Honma, Teruki,Umehara, Takashi,Shirouzu, Mikako,Fukami, Takehiro,Seimiya, Hiroyuki,Yoshida, Minoru,Koyama, Hiroo
supporting information, p. 4183 - 4204 (2020/05/20)
Tankyrases (TNKS/TNKS2) belong to the poly(ADP-ribose) polymerase family. Inhibition of their enzymatic activities attenuates the Wnt/β-catenin signaling, which plays an important role in cancer pathogenesis. We previously reported the discovery of RK-287107, a spiroindoline-based, highly selective, potent tankyrase inhibitor. Herein we describe the optimization process of RK-287107 leading to RK-582, which exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered. In addition to the dose-dependent elevation and attenuation of the levels of biomarkers AXIN2 and β-catenin, respectively, results of the TCF reporter and cell proliferation studies on COLO-320DM are discussed.
ANTICANCER AGENT
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Paragraph 0161; 163-0164, (2020/11/26)
To provide an anticancer agent for preventing and/or treating cancer, comprising a tankyrase inhibitor containing a tankyrase inhibitory compound and a microtubule inhibitor containing a microtubule inhibitory compound as active ingredients.
PIPERIDINES OR PIPERIDONES SUBSTITUTED WITH UREA AND PHENYL
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Page/Page column 69-73, (2019/10/01)
The present invention relates to a compound according to general formula (I) which acts as a modulator of FPR2 and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by FPR2.
FUNGICIDAL PYRAZOLES AND THEIR MIXTURES
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Page/Page column 48, (2012/03/26)
Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula (1), N-oxides, and salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as
FUNGICIDAL PYRAZOLES
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Page/Page column 58, (2010/09/18)
Disclosed are compounds of Formula (1), including all geometric and stereoisomers, JV-oxides, and salts thereof, wherein Q1 is a phenyl ring, naphthalenyl ring system, a 5- to 6-membered fully unsaturated heterocyclic ring or an 8- to 10-membered heteroar