Výsledky vyhledávání - "Tatsushi Osawa"

Antineoplastic effect of a single oral dose of the novel Flt3 inhibitor KRN383 on xenografted human leukemic cells harboring Flt3-activating mutations

Autor: Motoko Fujisawa, Masako Ozai, Mineo Kurokawa, Yukiko Komeno, Tatsushi Osawa, Kazuo Kubo, Tomoaki Kuwaki, Atsushi Miwa, Hisamaru Hirai, Tetsuya Yoshino, Yuko Ogasawara, Shigeru Chiba, Seishi Ogawa, Rieko Yoshioka, Uichi Nishiyama, Miyuki Kitahori, Eiji Yoshioka

Publikováno v: Leukemia Research. 30:1541-1546

Activating mutations of Fms-like tyrosine kinase 3 (Flt3) are the most common genetic abnormalities found in acute myeloid leukemia (AML) and represent potential therapeutic targets. The novel Flt3 inhibitor KRN383 inhibited the autophosphorylation o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f226167c88056810494921673b99d50b
https://doi.org/10.1016/j.leukres.2006.02.028

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Synthesis and structure–activity relationship for new series of 4-Phenoxyquinoline derivatives as specific inhibitors of platelet-derived growth factor receptor tyrosine kinase

Autor: Kazuo Kubo, Mikio Yagi, Shinichi Ohyama, Toshiyuki Isoe, Kazuhide Nakamura, Hideko Murooka, Tsuyoshi Nishitoba, Noriko Iinuma, Toshiyuki Shimizu, Shinichiro Kato, Toshio Izawa, Yoshiko Kobayashi, Tatsushi Osawa, Hiroshi Iijima, Atsuya Takami

Publikováno v: Bioorganic & Medicinal Chemistry. 11:5117-5133

We discovered a new series of 4-phenoxyquinoline derivatives as potent and selective inhibitors of the platelet-derived growth factor receptor (PDGFr) tyrosine kinase. We researched the highly potent and selective inhibitors on the basis of both PDGF

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07b323098a712c99f3aef4c26d510242
https://doi.org/10.1016/j.bmc.2003.08.020

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Effects of ortho-substituent groups of sulochrin on inhibitory activity to eosinophil degranulation

Autor: Tatsushi Osawa, Masaharu Ishikawa, Toyoo Nakao, Hiroshi Iijima, Kaname Kimura, Junko Ito, Hiroyuki Kawai, Akihiro Ueno, Hiroshi Ohashi

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 9:1945-1948

Sulochrin, a metabolite of fungi, has been shown to have an inhibitory activity to eosinophil degranulation. A series of sulochrin derivatives substituted at ortho-positions to the 10-carbonyl group was examined the activity. The importance of alkyle

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dcfe195697d9be66d3d1994dd135b506
https://doi.org/10.1016/s0960-894x(99)00305-4

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A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation

Autor: Toshio Izawa, Toshiyuki Isoe, Toshiyuki Shimizu, Kazuo Kubo, Tatsushi Osawa, Mikio Yagi, Yoshiko Kobayashi, Shinichiro Kato, Shinichi Ohyama, Kazuhide Nakamura, Hideko Murooka, Tsuyoshi Nishitoba

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:2935-2940

A novel series of 4-phenoxyquinolines, some of which showed potent and highly selective inhibitory activities for PDGF receptor autophosphorylation, was discovered. Interestingly, their structures were very similar to those of the selective inhibitor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2015881c3d4bd4e4ebe63154524edb92
https://doi.org/10.1016/s0960-894x(97)10117-2

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Selective Inhibition of Platelet-Derived Growth Factor (PDGF) Receptor Autophosphorylation and PDGF-Mediated Cellular Events by a Quinoline Derivative

Autor: Shinichi Oyama, Noriko Iinuma, Kazuo Kubo, Kazuhide Nakamura, Mikio Yagi, Hideya Ohashi, Tatsushi Osawa, Tsuyoshi Nishitoba, Nami Kobayashi, Shinichiro Kato, Toshiyuki Shimizu, Toshiyuki Isoe, Rie Onose, Hiroyuki Osada, Yoshiko Kobayashi

Publikováno v: Experimental Cell Research. 234:285-292

This report describes the biological effects of our original compound, Ki6783 ((3,4-dimethoxy)-4-phenoxy-6,7-dimethoxyquinoline), a potent and selective inhibitor of platelet-derived growth factor (PDGF) receptor autophosphorylation. This compound st

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::499b3e337c3562643995a1a0bc46df47
https://doi.org/10.1006/excr.1997.3616

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Syntheses of α-, β-monoglycosylceramides and four diastereomers of an α-galactosylceramide

Autor: Tatsushi Osawa, Takenori Natori, Yasuhiko Koezuka, Kohji Akimoto, Hideaki Fukushima, Masahiro Morita

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:699-704

To examine antitumor activities of monoglycosylceramide, we synthesized α-, β-galactosylceramides and α-, β-glucosylceramides which have the same ceramide portion, and four kinds of diastereomers of the ceramide portion in an α-galactosylceramid

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0c2cc485d88cf90b55612f17c93f66f8
https://doi.org/10.1016/0960-894x(95)00097-d

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A novel anti-cancer substance, MK615, from ume, a variety of Japanese apricot, inhibits growth of hepatocellular carcinoma cells by suppressing Aurora A kinase activity

Autor: Toshie, Okada, Tokihiko, Sawada, Tatsushi, Osawa, Masakazu, Adachi, Keiichi, Kubota

Publikováno v: Hepato-gastroenterology. 54(78)

MK615 is an anti-cancer substance extracted from the Japanese apricot. In the present study, the anti-neoplastic effect of MK615 against hepatocellular carcinoma (HCC) was evaluated in vitro, and its mechanism was elucidated.Two HCC lines, HuH7 and H

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::ab53722b05c865e31716b625f08fc1e0
https://pubmed.ncbi.nlm.nih.gov/18019715

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Identification of potent and selective inhibitors of PDGF receptor autophosphorylation

Autor: Megumi Endo, Teruyuki Sakai, Atsushi Miwa, Rika Suzuki, Toshiyuki Shimizu, Takayuki Furuta, Tetsuya Yoshino, Tatsushi Osawa, Kazuo Kubo, Terufumi Senga

Publikováno v: Journal of medicinal chemistry. 49(7)

We report the structure-activity relationship of quinoline and quinazoline derivatives, which include urea, thiourea, urethane, and acylthiourea groups, as inhibitors of the platelet-derived growth factor (PDGF) receptor autophosphorylation. Our prev

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::68cb4436707a63e099cd3c67209440a4
https://pubmed.ncbi.nlm.nih.gov/16570914

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Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors

Autor: Kaname Kimura, Kayoko Fukushima, Akemi Iwai, Tetsuya Yoshino, Tatsushi Osawa, Tsuyoshi Nishitoba, Teruyuki Sakai, Atsushi Miwa, Kazuo Kubo, Yasunari Fujiwara, Kinya Kubo, Toshiyuki Shimizu, Terufumi Senga, Hideko Murooka

Publikováno v: Bioorganicmedicinal chemistry letters. 14(4)

(6,7-Disubstituted-quinolin-4-yloxy-phenyl)(4-substituted-phenyl)amine derivatives were synthesized and evaluated by a cellular autophosphorylation assay for FGF-R2 in the human scirrhous gastric carcinoma cell line, OCUM-2MD3. We also performed meta

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40b340e0ee4e942071125347bcb666e5
https://pubmed.ncbi.nlm.nih.gov/15012985

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Beneficial effects of a novel inhibitor of platelet-derived growth factor receptor autophosphorylation in the rat with mesangial proliferative glomerulonephritis

Autor: Nami Kobayashi, Shinichiro Kato, Kazuo Kubo, Nobuo Nagano, Mikio Yagi, Toshiyuki Shimizu, Tsuyoshi Nishitoba, Kazuhide Nakamura, Noriko Iinuma, Hideko Murooka, Tatsushi Osawa, Shinichi Ohyama, Yoshiko Kobayashi

Publikováno v: General pharmacology. 31(5)

1. Our original compound, Ki6896 ((4- t -butylphenyl){4-[(6,7-dimethoxy-4-quinolyl) oxy]phenyl} methanone) strongly inhibited the autophosphorylation of platelet-derived growth factor (PDGF) β-receptor (IC 50 =0.31 μM) and that of basic fibroblast

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5d3bace55ce66f2d7b6e30f4555cb66
https://pubmed.ncbi.nlm.nih.gov/9809476

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