Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Jean-Yves Le Brazidec"'
Autor:
Lin Zhang, Annie Raditsis, Istvan J. Enyedy, Jianhua Chao, Ishchenko Alexey, Brian Elenbaas, Laura Silvian, Jer Hong Chong, Victor Sukbong Hong, Douglas Marcotte, Junhua Fan, Aparna Hingway, Jean-Yves Le Brazidec, Latika Singh
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:474-480
PIM kinases are implicated in variety of cancers by promoting cell survival and proliferation and are targets of interest for therapeutic intervention. We have identified a low-nanomolar pan-PIM inhibitor (PIM1/2/3 potency 5:14:2nM) using structure b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f957718a29c892d89d0d2f01a1c02c95
https://doi.org/10.1016/j.bmcl.2014.12.041
https://doi.org/10.1016/j.bmcl.2014.12.041
Autor:
Lin Zhang, Art Taveras, Jer-Hong Chong, Jianhua Chao, Min Teng, Nuzhat Pathan, Angela Pasis, Betty Tam, Jean-Yves Le Brazidec, Michael J. Choi, Junhua Fan, Leona E. Ling, Deping Wang, Christina Boykin, Cheryl Black, Tony Li, Khanh Nguyen, Shuo Zhao, Laura Silvian, Gisela Claassen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2070-2074
Since the early 2000s, the Aurora kinases have become major targets of oncology drug discovery particularly Aurora-A and Aurora-B kinases (AKA/AKB) for which the selective inhibition in cells lead to different phenotypes. In addition to targeting the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::305d6a2f7a009fcf16ad3cbdfedcb372
https://doi.org/10.1016/j.bmcl.2012.01.019
https://doi.org/10.1016/j.bmcl.2012.01.019
Autor:
Kevin Hong, Adeela Kamal, Yingqing Ran, Jiandong Shi, Marcus F. Boehm, Karen Lundgren, Gregg Timony, Khang Vu, Edgar H. Ulm, Francis Burrows, Roy Grecko, Rachel Lough, Srinivas Rao Kasibhatla, John Sensintaffar, David J. Busch, Jean-Yves Le Brazidec, Marco A. Biamonte, Robert K. Mansfield, Junhua Fan, Lin Zhang
Publikováno v:
Journal of Medicinal Chemistry. 49:5352-5362
We report on the discovery of benzo- and pyridino- thiazolothiopurines as potent heat shock protein 90 inhibitors. The benzothiazole moiety is exceptionally sensitive to substitutions on the aromatic ring with a 7'-substituent essential for activity.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a30163f614c02b6f0a966897c679719
https://doi.org/10.1021/jm051146h
https://doi.org/10.1021/jm051146h
Autor:
Lin Zhang, Rachel Lough, Samina Khan, Lia Thao, Roy Grecko, Gregg Timony, Adeela Kamal, Francis Burrows, Tim Salazar, David J. Busch, Marcus F. Boehm, Jean-Yves Le Brazidec, Katy Trent
Publikováno v:
Journal of Medicinal Chemistry. 47:3865-3873
The heat shock protein Hsp90 has increasingly become an important therapeutic target especially for treatment of cancers. Inhibition of the ATPase activity of Hsp90 by natural products (e.g., 17-allylaminogeldanamycin or radicicol) leads to the ubiqu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e59bf4fbe8d00d50bccf2e8cf3571a4
https://doi.org/10.1021/jm0306125
https://doi.org/10.1021/jm0306125
Autor:
Yoko Nagumo, Masahiro Hirama, Masashi Kosaka, Tohru Oishi, Masayuki Inoue, Mitsuru Shoji, Jean Yves Le Brazidec, Hisatoshi Uehara
Publikováno v:
Tetrahedron. 58:6493-6512
Ciguatoxin CTX3C is a representative congener of the ciguatoxins, which are known to be the principal causative agents of ciguatera food poisoning. The structure of CTX3C spans more than 3 nm and is characterized by 13 ether rings. To attain a practi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bb9d5bb1efce2769f79b325dfc93e419
https://doi.org/10.1016/s0040-4020(02)00660-9
https://doi.org/10.1016/s0040-4020(02)00660-9
Autor:
Jer-Hong Chong, Michael J. Choi, Douglas Marcotte, Tony Li, Junhua Fan, Deping Wang, Leona E. Ling, Lin Zhang, Art Taveras, Nuzhat Pathan, Khanh Nguyen, Min Teng, Gisela Claassen, Jean-Yves Le Brazidec, Shuo Zhao, Christina Boykin, Betty Tam, Laura Silvian, Angela Pasis, Jianhua Chao
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(12)
This Letter reports the optimization of a pyrrolopyrimidine series as dual inhibitors of Aurora A/B kinases. This series derived from a pyrazolopyrimidine series previously reported as inhibitors of aurora kinases and CDKs. In an effort to improve th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d04c16b379ccb805ccedbd00429b130f
https://pubmed.ncbi.nlm.nih.gov/22607669
https://pubmed.ncbi.nlm.nih.gov/22607669
Autor:
Liang-Shang Gan, Betty Tam, Khang Vu, Jinhua Piao, Douglas Marcotte, Shuo Zhao, Min Teng, Jianhua Chao, Charles A. Iii Gilson, Dikran Aivazian, Qin Wang, Guangqing Xiao, Arthur G. Taveras, Samina Khan, Tony Li, Junhua Fan, Jean-Yves Le Brazidec, Wen-Cherng Lee, Noel Timple, Khanh Nguyen, Lin Zhang, Jer-Hong Chong, Kevin Hong, Laura Silvian, Nicole Takeda, Mitchell Reff, Angela Cesena, Ron A. Morena, Deping Wang, Karen Lundgren, Leona E. Ling, Christina Boykin
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(18)
A novel class of pyrazolopyrimidine-sulfonamides was discovered as selective dual inhibitors of aurora kinase A (AKA) and cyclin-dependent kinase 1 (CDK1). These inhibitors were originally designed based on an early lead (compound I). SAR development
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c36dadf5f7bf00efcdb5a0ac2fe8944
https://pubmed.ncbi.nlm.nih.gov/21798738
https://pubmed.ncbi.nlm.nih.gov/21798738
Autor:
Yoko Nagumo, Tohru Oishi, Mitsuru Shoji, Hisatoshi Uehara, Jean-Yves Le Brazidec, Masahiro Hirama
Publikováno v:
ChemInform. 31
The IJKLM ring fragment of CTX3C, an important member of the ciguatoxin family, was synthesized via ring-closing metathesis using the Tebbe reagent and an improved method of reductive hydroxy ketone cyclization.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f7efb1dbf2951c06161aef20cde76811
https://doi.org/10.1002/chin.200006237
https://doi.org/10.1002/chin.200006237
Autor:
Yoko Nagumo, Hisatoshi Uehara, Masashi Kosaka, Tohru Oishi, Mitsuru Shoji, Masahiro Hirama, Jean-Yves Le Brazidec
Publikováno v:
ChemInform. 32
The HIJKLM ring segment (27) of the right half portion of ciguatoxin CTX3C (1) has been synthesized using a ring-closing reaction mediated by a low-valent titanium reagent.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2b620c029a59f0dd9658fcc38f20afba
https://doi.org/10.1002/chin.200123208
https://doi.org/10.1002/chin.200123208
Autor:
Hisatoshi Uehara, Tohru Oishi, Masayuki Inoue, Mitsuru Shoji, Yoko Nagumo, Masashi Kosaka, Jean-Yves Le Brazidec, Masahiro Hirama
Publikováno v:
ChemInform. 33
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::00f5ed833df211790f4efd28de11c6e6
https://doi.org/10.1002/chin.200250209
https://doi.org/10.1002/chin.200250209