Výsledky vyhledávání

Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent

Autor: Toshiyuki Nomura, Hiroshi Sugimoto, Noriko Uchiyama, Akihiro Ohashi, Hideto Hara, Takashi Imada, Yukiko Yamamoto, Isaac Hoffman, Kenichi Iwai, Momoko Ohori, Misaki Homma, Osamu Kurasawa, Nobuo Cho, Tohru Miyazaki, Yuya Oguro, Kentaro Iwata, Robert J. Skene

Publikováno v: Journal of Medicinal Chemistry. 63:1084-1104

In our pursuit of developing a novel, potent, and selective cell division cycle 7 (Cdc7) inhibitor, we optimized the previously reported thieno[3,2-d]pyrimidinone analogue I showing time-dependent Cdc7 kinase inhibition and slow dissociation kinetics

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::302cc8787b4b0af51ff2d819e10565ac
https://doi.org/10.1021/acs.jmedchem.9b01427

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2-Aminomethylthieno[3,2- d ]pyrimidin-4(3 H )-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase

Autor: Hideto Hara, Misaki Homma, Akihiro Ohashi, Yuya Oguro, Kouji Mori, Osamu Kurasawa, Nobuo Cho, Tohru Miyazaki, Sei Yoshida, Kenichi Iwai, Noriko Uchiyama

Publikováno v: Bioorganic & Medicinal Chemistry. 25:3658-3670

In order to increase the success rate for developing new Cdc7 inhibitors for cancer therapy, we explored a new chemotype which can comply with the previously-constructed pharmacophore model. Substitution of a pyridine ring of a serendipitously-identi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbf0cb711b3289b52763b9b0437e281f
https://doi.org/10.1016/j.bmc.2017.04.044

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Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones

Autor: Isaac Hoffman, Sei Yoshida, Osamu Kurasawa, Kenichi Iwai, Tomoyasu Ishikawa, Kouji Mori, Akihiro Ohashi, Hideto Hara, Nobuo Cho, Tohru Miyazaki, Robert J. Skene, Yuya Oguro, Misaki Homma

Publikováno v: Bioorganicmedicinal chemistry. 25(7)

Cell division cycle 7 (Cdc7) is a serine/threonine kinase that plays important roles in the regulation of DNA replication process. A genetic study indicates that Cdc7 inhibition can induce selective tumor-cell death in a p53-dependent manner, suggest

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f0f9a7ca7899e8598f82eecd7960b9a
https://pubmed.ncbi.nlm.nih.gov/28284870

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Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: Discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics

Autor: Douglas R. Cary, Akira Hori, Hiroshi Miki, Michiko Tawada, Hidehisa Iwata, Naoki Miyamoto, Shinichi Imamura, Yuya Oguro

Publikováno v: Bioorganic & Medicinal Chemistry. 21:4714-4729

For the purpose of discovering novel type-II inhibitors of vascular endothelial growth factor receptor 2 (VEGFR2) kinase, we designed and synthesized 5,6-fused heterocyclic compounds bearing a anilide group. A co-crystal structure analysis of imidazo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a99580c5b065df47f323965fd837e241
https://doi.org/10.1016/j.bmc.2013.04.042

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Discovery of N -[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2- b ]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1 H -pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor

Autor: Akira Hori, Yoshiko Awazu, Terufumi Takagi, Yuya Oguro, Nozomu Sakai, Takaharu Hirayama, Kengo Okada, Naoki Miyamoto, Hideyuki Oki, Hiroshi Miki, Shinichi Imamura, Hidehisa Iwata, Toshiyuki Takeuchi, Seiji Yamasaki, Kazuhiro Miwa

Publikováno v: Bioorganic & Medicinal Chemistry. 21:2333-2345

Vascular endothelial growth factor (VEGF) plays important roles in tumor angiogenesis, and the inhibition of its signaling pathway is considered an effective therapeutic option for the treatment of cancer. In this study, we describe the design, synth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db8a3cc876ef7cb28cf6dbe5c21fb1c5
https://doi.org/10.1016/j.bmc.2013.01.074

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Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors

Autor: Shinichi Imamura, Hiroshi Miki, Hidehisa Iwata, Akira Hori, Terufumi Takagi, Naoki Miyamoto, Yuya Oguro

Publikováno v: Bioorganic & Medicinal Chemistry. 20:7051-7058

The vascular endothelial growth factor (VEGF) signaling pathway has been implicated in tumor angiogenesis, and inhibition of the VEGF pathway is considered an efficacious method for treating cancer. Herein, we describe synthetic studies of imidazo[1,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::68f4e359559c7c10bd73a9fc1ee947a7
https://doi.org/10.1016/j.bmc.2012.10.004

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