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Dive into the research topics where Susumu Komiyama is active.

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Featured researches published by Susumu Komiyama.


Bioorganic & Medicinal Chemistry Letters | 2012

Design and synthesis of novel macrocyclic 2-amino-6-arylpyrimidine Hsp90 inhibitors

Atsushi Suda; Hiroshi Koyano; Tadakatsu Hayase; Kihito Hada; Kenichi Kawasaki; Susumu Komiyama; Kiyoshi Hasegawa; Takaaki A. Fukami; Shigeo Sato; Takaaki Miura; Naomi Ono; Toshikazu Yamazaki; Ryoichi Saitoh; Nobuo Shimma; Yasuhiko Shiratori; Takuo Tsukuda

Macrocyclic compounds bearing a 2-amino-6-arylpyrimidine moiety were identified as potent heat shock protein 90 (Hsp90) inhibitors by modification of 2-amino-6-aryltriazine derivative (CH5015765). We employed a macrocyclic structure as a skeleton of new inhibitors to mimic the geldanamycin-Hsp90 interactions. Among the identified inhibitors, CH5164840 showed high binding affinity for N-terminal Hsp90α (K(d)=0.52nM) and strong anti-proliferative activity against human cancer cell lines (HCT116 IC(50)=0.15μM, NCI-N87 IC(50)=0.066μM). CH5164840 displayed high oral bioavailability in mice (F=70.8%) and potent antitumor efficacy in a HCT116 human colorectal cancer xenograft model (tumor growth inhibition=83%).


Bioorganic & Medicinal Chemistry | 2014

Design and synthesis of 2-amino-6-(1H,3H-benzo[de]isochromen-6-yl)-1,3,5-triazines as novel Hsp90 inhibitors.

Atsushi Suda; Kenichi Kawasaki; Susumu Komiyama; Yoshiaki Isshiki; D.H. Yoon; Sung-Jin Kim; Young-Jun Na; Kiyoshi Hasegawa; Takaaki A. Fukami; Shigeo Sato; Takaaki Miura; Naomi Ono; Toshikazu Yamazaki; Ryoichi Saitoh; Nobuo Shimma; Yasuhiko Shiratori; Takuo Tsukuda

A novel series of 2-amino-1,3,5-triazines bearing a tricyclic moiety as heat shock protein 90 (Hsp90) inhibitors is described. Molecular design was performed using X-ray cocrystal structures of the lead compound CH5015765 and natural Hsp90 inhibitor geldanamycin with Hsp90. We optimized affinity to Hsp90, in vitro cell growth inhibitory activity, water solubility, and liver microsomal stability of inhibitors and identified CH5138303. This compound showed high binding affinity for N-terminal Hsp90α (Kd=0.52nM) and strong in vitro cell growth inhibition against human cancer cell lines (HCT116 IC50=0.098μM, NCI-N87 IC50=0.066μM) and also displayed high oral bioavailability in mice (F=44.0%) and potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model (tumor growth inhibition=136%).


Bioorganic & Medicinal Chemistry Letters | 2013

Enantioselective synthesis of derivatives and structure-activity relationship study in the development of NA255 as a novel host-targeting anti-HCV agent.

Kenichi Kawasaki; Miyako Masubuchi; Tadakatsu Hayase; Susumu Komiyama; Fumio Watanabe; Hiroshi Fukuda; Takeshi Murata; Yasuaki Matsubara; Kouhei Koyama; Hidetoshi Shindoh; Hiroshi Sakamoto; Kohichi Okamato; Atsunori Ohta; Asao Katsume; Masahiro Aoki; Yuko Aoki; Nobuo Shimma; Masayuki Sudoh; Takuo Tsukuda

Hepatitis C virus (HCV) infection represents a serious health-care problem. Previously we reported the identification of NA255 from our natural products library using a HCV sub-genomic replicon cell culture system. Herein, we report how the absolute stereochemistry of NA255 was determined and an enantioselective synthetic method for NA255 derivatives was developed. The structure-activity relationship of the NA255 derivatives and rat pharmacokinetic profiles of the representative compounds are disclosed.


Archive | 2004

Compound having anti-hcv activity and process for producing the same

Masayuki Sudoh; Takuo Tsukuda; Miyako Masubuchi; Kenichi Kawasaki; Takeshi Murata; Fumio Watanabe; Hiroshi Fukuda; Susumu Komiyama; Tadakatsu Hayase


Archive | 2006

Process for producing compound with anti-hcv potency and intermediate for use therein

Tatsuya Kato; Susumu Komiyama; Akemi Mizutani; Toshihiko Makino; Kenichi Kawasaki; Takuo Tsukuda; Hiroshi Fukuda; Nobuaki Kimura


Archive | 2001

1-(h-1,2,4-triazol-1-yl)butan-2-ol derivatives

Susumu Komiyama; Nobuo Shimma; Takuo Tsukuda


Archive | 2010

Intermediate compound for synthesis of viridiofungin a derivative

Tatsuya Kato; Nobuaki Kimura; Akemi Mizutani; Toshihiko Makino; Kenichi Kawasaki; Hiroshi Fukuda; Susumu Komiyama; Takuo Tsukuda


Archive | 2013

Orally available viridiofungin derivative possessing anti-HCV activity

Yasunori Kohchi; Kimitaka Nakama; Susumu Komiyama; Fumio Watanabe


Archive | 2013

Orally administrable viridiofungin derivative having anti-hcv activity

Yasunori Kohchi; Kimitaka Nakama; Susumu Komiyama; Fumio Watanabe


Archive | 2013

Dérivé de viridiofungine administrable oralement ayant une activité anti-vhc

Yasunori Kohchi; 靖典 河内; Kimitaka Nakama; 公崇 仲間; Susumu Komiyama; 享 小宮山; Fumio Watanabe; 渡辺 史郎

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Takuo Tsukuda

Chugai Pharmaceutical Co.

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Fumio Watanabe

Chugai Pharmaceutical Co.

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Nobuo Shimma

Chugai Pharmaceutical Co.

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Masayuki Sudoh

Chugai Pharmaceutical Co.

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Takaaki Miura

Chugai Pharmaceutical Co.

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