935758-93-3Relevant academic research and scientific papers
Novel gambogic acid class derivative and preparation method and application thereof
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Paragraph 0016; 0017; 0027; 0028, (2018/02/04)
The invention belongs to the technical field of antitumor drug preparation and discloses a novel gambogic acid class derivative and a preparation method and application thereof. The derivative of the structure mainly modifies gambogic acid C-30, and a plu
Discovery of novel, highly potent, and selective matrix metalloproteinase (MMP)-13 inhibitors with a 1,2,4-triazol-3-yl moiety as a zinc binding group using a structure-based design approach
Nara, Hiroshi,Kaieda, Akira,Sato, Kenjiro,Naito, Takako,Mototani, Hideyuki,Oki, Hideyuki,Yamamoto, Yoshio,Kuno, Haruhiko,Santou, Takashi,Kanzaki, Naoyuki,Terauchi, Jun,Uchikawa, Osamu,Kori, Masakuni
, p. 608 - 626 (2017/02/05)
On the basis of a superposition study of X-ray crystal structures of complexes of quinazoline derivative 1 and triazole derivative 2 with matrix metalloproteinase (MMP)-13 catalytic domain, a novel series of fused pyrimidine compounds which possess a 1,2,4-triazol-3-yl group as a zinc binding group (ZBG) was designed. Among the herein described and evaluated compounds, 31f exhibited excellent potency for MMP-13 (IC50 = 0.036 nM) and selectivities (greater than 1,500-fold) over other MMPs (MMP-1, -2, -3, -7, -8, -9, -10, and -14) and tumor necrosis factor-α converting enzyme (TACE). Furthermore, the inhibitor was shown to protect bovine nasal cartilage explants against degradation induced by interleukin-1 and oncostatin M. In this article, we report the discovery of extremely potent, highly selective, and orally bioavailable fused pyrimidine derivatives that possess a 1,2,4-triazol-3-yl group as a novel ZBG for selective MMP-13 inhibition.
Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors
Su, Ting,Wu, Yanhong,Doughan, Brandon,Kane-Maguire, Kim,Marlowe, Charles K,Kanter, James P,Woolfrey, John,Huang, Brian,Wong, Paul,Sinha, Uma,Park, Gary,Malinowski, John,Hollenbach, Stan,Scarborough, Robert M,Zhu, Bing-Yan
, p. 2279 - 2282 (2007/10/03)
A series of glycolic and mandelic acid derivatives was synthesized and investigated for their factor Xa inhibitory activity. These analogues are highly potent and selective inhibitors against fXa. In a rabbit deep vein thrombosis model, compound 26 showed
