Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Toshihiro Hamajima"'
Autor:
Hidehiko Fukahori, Kaoru Yamagami, Satoshi Kubo, Yukihito Sugano, Fumie Takahashi, Ayako Moritomo, Koji Kato, Susumu Yamaki, Koji Nakamura, Koji Yokoo, Toshihiro Hamajima, Suzuki Daisuke
Publikováno v:
Bioorganic & Medicinal Chemistry. 27:1056-1064
Chemical optimization of the 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine (THPP) scaffold was conducted with a focus on cellular potency while maintaining high selectivity against PI3K isoforms. Compound 11f was identified as a potent, highly selective
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::45f4885a30545480350b0f2b6589425c
https://doi.org/10.1016/j.bmc.2019.02.001
https://doi.org/10.1016/j.bmc.2019.02.001
Autor:
Koichiro Mukoyoshi, Kaoru Yamagami, Kousei Yoshihara, Koji Yokoo, Susumu Yamaki, Fumie Takahashi, Toshihiro Hamajima, Yukihito Sugano, Koji Kato, Hidehiko Fukahori, Ayako Moritomo
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:2410-2419
Phosphatidylinositol-3-kinase (PI3K)δ inhibition is one of the most attractive approaches to the treatment of autoimmune diseases and leukocyte malignancies. Through the exploration of pyrazolopyridine derivatives as potential PI3Kδ inhibitors, com
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::85ec92c15654c1c5276396c3ef1540be
https://doi.org/10.1016/j.bmc.2018.03.042
https://doi.org/10.1016/j.bmc.2018.03.042
Autor:
Toshihiro Hamajima, Fumie Takahashi, Yukihito Sugano, Susumu Yamaki, Satoshi Kubo, Kaoru Yamagami, Koji Kato, Koji Nakamura, Nozomu Hamakawa, Koji Yokoo, Hidehiko Fukahori, Ayako Moritomo
Publikováno v:
Bioorganicmedicinal chemistry. 26(14)
Chemical optimization of pyrazolopyridine 1, focused on cellular potency, isoform selectivity and microsomal stability, led to the discovery of the potent, selective and orally available PI3Kδ inhibitor 5d. On the basis of its desirable potency, sel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7780e6b0ae77807416e7f21ce49912f2
https://pubmed.ncbi.nlm.nih.gov/29907471
https://pubmed.ncbi.nlm.nih.gov/29907471
Autor:
Octerloney B. McDonald, Carla A. Donatelli, William F. Huffman, Toshihiro Hamajima, Christine Thompson, Kelly E. Fisher, Martha A. Sarpong, Jamin C Wang, David Sutton, Dashyant Dhanak, Peter J. Tummino, Jun Tang, Ken A. Newlander, Zhihong V Lai, Hong Xiang, Kosuke Sasaki, Domingos J. Silva, Mary Ann Hardwicke, Jerry L. Adams, Cynthia A. Parrish, Schmidt Stanley J, Denis R. Patrick, Hiroko Nakamura, Jingsong Yang, Catherine A. Oleykowski, Robert A. Copeland, Amita M. Chaudhari, Ramona Plant, David H. Drewry, Kristin K Koretke-Brown, Nicholas D. Adams, Joelle Lorraine Burgess
Publikováno v:
Journal of Medicinal Chemistry. 53:3973-4001
The Aurora kinases play critical roles in the regulation of mitosis and are frequently overexpressed or amplified in human tumors. Selective inhibitors may provide a new therapy for the treatment of tumors with Aurora kinase amplification. Herein we
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e9b7d71b0eb4521a715c9504ca08490
https://doi.org/10.1021/jm901870q
https://doi.org/10.1021/jm901870q
Publikováno v:
Tetrahedron Letters. 47:1261-1265
A catalytic amount of ytterbium triflate (Yb(OTf) 3 ) promotes the cyclization of an N -silylenamine with in situ generated 2-methylene-1,3-cyclohexanedione and 2-methylenecyclohexanone to produce the corresponding 2,3-disubstituted 7,8-dihydroquinol
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ab091ce8973d576fe244376035c7c0e3
https://doi.org/10.1016/j.tetlet.2005.12.080
https://doi.org/10.1016/j.tetlet.2005.12.080
Autor:
Harada Katsuya, Hitoshi Sakashita, Yuzo Matsumoto, Tatsuya Niimi, Tomohiko Yamaguchi, Takeshi Hondo, Keita Nakanishi, Makoto Takeuchi, Masaichi Warizaya, Masaya Orita, Toshihiro Hamajima, Ichiji Namatame
Publikováno v:
Journal of medicinal chemistry. 56(9)
D-Amino acid oxidase (DAAO) catalyzes the oxidation of d-amino acids including d-serine, a coagonist of the N-methyl-d-aspartate receptor. We identified a series of 4-hydroxypyridazin-3(2H)-one derivatives as novel DAAO inhibitors with high potency a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79cb0716f906c33a015e43b9152f87c6
https://pubmed.ncbi.nlm.nih.gov/23566269
https://pubmed.ncbi.nlm.nih.gov/23566269
Publikováno v:
Tetrahedron Letters. 43:4821-4823
A catalytic amount of copper(II) trifluoromethanesulfonate (Cu(OTf)2) in the presence of trimethylchlorosilane (TMSCl) effectively promoted the aminomethylation of indoles bearing a variety of functional groups with a N-silyl-N,O-acetal in good to ex
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::263a4b275aae2a5b213b353522146551
https://doi.org/10.1016/s0040-4039(02)00921-8
https://doi.org/10.1016/s0040-4039(02)00921-8
Publikováno v:
ChemInform. 33
A catalytic amount of copper(II) trifluoromethanesulfonate (Cu(OTf)2) in the presence of trimethylchlorosilane (TMSCl) effectively promoted the aminomethylation of indoles bearing a variety of functional groups with a N-silyl-N,O-acetal in good to ex
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0c9814960370ed0e45060deee9cf1383
https://doi.org/10.1002/chin.200241115
https://doi.org/10.1002/chin.200241115
Autor:
Huangshu Lei, Anne M. Hassell, Rakesh Kumar, M. Anthony Leesnitzer, Toshihiro Hamajima, Felix Deanda, Hiroko Nakamura, Stanley D. Chamberlain, J. Brad Shotwell, Jun Tang, Roseanne Gerding, Samarjit Patnaik, Lisa M. Shewchuck, Kirk L. Stevens
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(11)
Exploration of the SAR around a series of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines led to the discovery of novel pyrrolopyridine inhibitors of the IGF-1R tyrosine kinase. Several compounds demonstrated nanomolar potency in enzyme and cellular mec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::701863fa69f3d183d14561c2ba78ff87
https://pubmed.ncbi.nlm.nih.gov/19394223
https://pubmed.ncbi.nlm.nih.gov/19394223
Autor:
Karen Lackey, Toshihiro Hamajima, Masato Nakano, Hideyuki Sato, Jun Tang, Scott Howard Dickerson
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(16)
The synthesis of a 7-azaindole series of novel, potent B-Raf kinase inhibitors using knowledge-based design was carried out. Compound 6h exhibits not only excellent potency in both the enzyme assay (IC50 = 2.5 nM) and the cellular assay (IC50 = 63 nM
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d5da163721e9fcff84caad31045d7f68
https://pubmed.ncbi.nlm.nih.gov/18662874
https://pubmed.ncbi.nlm.nih.gov/18662874