1269028-74-1Relevant articles and documents
Synthesis and evaluation of hedgehog signaling inhibitor with novel core system
Ohashi, Tomohiro,Tanaka, Yuta,Shiokawa, Zenyu,Banno, Hiroshi,Tanaka, Toshio,Shibata, Sachio,Satoh, Yoshihiko,Yamakawa, Hiroko,Yamamoto, Yukiko,Hattori, Harumi,Kondo, Shigeru,Miyamoto, Maki,Tojo, Hideaki,Baba, Atsuo,Sasaki, Satoshi
, p. 4777 - 4791 (2015)
As we previously reported, N-methylpyrrolo[3,2-c]pyridine derivatives 1 (TAK-441) was discovered as a clinical candidate of hedgehog (Hh) signaling inhibitor by modification of the upper part. We next focused on modification of the lower part including core skeletons to discover new Hh signaling inhibitors with novel core rings. Efforts to find novel chemotypes by using X-ray single crystal structure analysis led to some potent Hh signaling inhibitors (2c, 2d, 2e, 2f) with novel core ring systems, which had benzamide moiety at the 5-position as a key component for potent activity. The suppression of Gli1 expression with these new Hh signaling inhibitors were weaker than that of compound 1 (TAK-441) because of low pharmacokinetic property. We recognized again TAK-441 is a good compound as clinical candidate with good structural and pharmacokinetic advantages.
FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF
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, (2012/07/14)
The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.
