- Exploring hydrogen peroxide responsive thiazolidinone-based prodrugs
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A novel approach for developing prodrugs based on masked carboxylic acids is described. Rather than using conventional esterase-based activation, thiazolidinone protecting groups have been identified that can reveal carboxylic acid groups upon activation by hydrogen peroxide. This may prove valuable in the continuing development of prodrug strategies that rely on reactive oxygen species (ROS) as a trigger. This journal is
- Perez, Christian,Monserrat, Jean-Philippe,Chen, Yao,Cohen, Seth M.
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supporting information
p. 7116 - 7119
(2015/04/27)
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- Specific detection and imaging of enzyme activity by signal-amplifiable self-assembling 19Fa MRI probes
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Specific turn-on detection of enzyme activities is of fundamental importance in drug discovery research, as well as medical diagnostics. Although magnetic resonance imaging (MRI) is one of the most powerful techniques for noninvasive visualization of enzy
- Matsuo, Kazuya,Kamada, Rui,Mizusawa, Keigo,Imai, Hirohiko,Takayama, Yuki,Narazaki, Michiko,Matsuda, Tetsuya,Takaoka, Yousuke,Hamachi, Itaru
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p. 12875 - 12883
(2013/10/01)
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- Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors
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Aggrecanases are recently discovered enzymes that cleave aggrecan, a key component of cartilage. Aggrecanase inhibitors may provide a unique means to halt the progression of cartilage destruction in osteoarthritis. The synthesis and evaluation of biphenyl
- Xiang, Jason S.,Hu, Yonghan,Rush, Thomas S.,Thomason, Jennifer R.,Ipek, Manus,Sum, Phaik-Eng,Abrous, Leila,Sabatini, Joshua J.,Georgiadis, Katy,Reifenberg, Erica,Majumdar, Manas,Morris, Elisabeth A.,Tam, Steve
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p. 311 - 316
(2007/10/03)
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- Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives
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Various N-sulfonylamino acid derivatives were synthesized and evaluated for their in vitro and in vivo activities to inhibit type IV collagenase (MMP-9 and MMP-2). When the amino acid residue and the sulfonamide moiety were modified, their inhibitory activities were greatly affected by the structure of the sulfonamide moiety. A series of aryl sulfonamide derivatives containing biaryl, tetrazole, amide, and triple bond were found to be potent and highly selective inhibitors of MMP-9 and MMP-2. In addition, these compounds were orally active in animal models of tumor growth and metastasis. These results revealed the potential of the N-sulfonylamino acid derivatives as a new type of candidate drug for the treatment of cancer.
- Tamura, Yoshinori,Watanabe, Fumihiko,Nakatani, Takuji,Yasui, Ken,Fuji, Masahiro,Komurasaki, Tadafumi,Tsuzuki, Hiroshige,Maekawa, Ryuji,Yoshioka, Takayuki,Kawada, Kenji,Sugita, Kenji,Ohtani, Mitsuaki
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p. 640 - 649
(2007/10/03)
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