165669-11-4Relevant articles and documents
Integrin expression inhibitors
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, (2008/06/13)
The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them. In the formula, B means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated; K means a single bond, —CH═CH— or —(CR4bR5b)mb— (wherein R4b and R5b are the same as or different from each other and each means hydrogen atom or a C1-C4 alkyl group; and mb means an integer of 1 or 2); R1 means hydrogen atom or a C1-C6 alkyl group; Z means a single bond or —CO—NH—; and R means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated, respectively.
Synthesis and biological evaluation of N-(7-indolyl)-3-pyridinesulfonamide derivatives as potent antitumor agents.
Owa, Takashi,Yoshino, Hiroshi,Okauchi, Tatsuo,Okabe, Tadashi,Ozawa, Yoichi,Hata Sugi, Naoko,Yoshimatsu, Kentaro,Nagasu, Takeshi,Koyanagi, Nozomu,Kitoh, Kyosuke
, p. 2097 - 2100 (2007/10/03)
We herein report the synthesis and antitumor activity of E7070 analogues containing a 3-pyridinesulfonamide moiety. E7070 was selected from our sulfonamide-based compound collections, currently undergoing Phase II clinical trials because of its tolerable toxicity profile and some antitumor responses in the Phase I setting. Of the analogues examined, ER-35745, a 6-amino-3-pyridinesulfonamide derivative, demonstrated significant oral efficacy against the HCT116 human colon carcinoma xenograft in nude mice.
Discovery of novel antitumor sulfonamides targeting G1 phase of the cell cycle
Owa, Takashi,Yoshino, Hiroshi,Okauchi, Tatsuo,Yoshimatsu, Kentaro,Ozawa, Yoichi,Sugi, Naoko Hata,Nagasu, Takeshi,Koyanagi, Nozomu,Kitoh, Kyosuke
, p. 3789 - 3799 (2007/10/03)
Described herein is the discovery of a novel series of antitumor sulfonamides targeting G1 phase of the cell cycle. Cell cycle control in G1 phase has attracted considerable attention in recent cancer research, because many of the important proteins invol