193808-69-4Relevant academic research and scientific papers
Novel 1-hydroxypiperazine-2,6-diones as new leads in the inhibition of metalloproteinases
Marques, Sérgio M.,Tuccinardi, Tiziano,Nuti, Elisa,Santamaria, Salvatore,André, Vania,Rossello, Armando,Martinelli, Adriano,Santos, M. Amélia
experimental part, p. 8289 - 8298 (2012/02/05)
New compounds containing a novel zinc-binding group (1-hydroxypiperazine-2, 6-dione, HPD) have been identified as effective inhibitors of matrix metalloproteinases (MMPs), with activities in the nanomolar concentration range. That moiety seemed to bind th
Dual inhibitors of matrix metalloproteinases and carbonic anhydrases: Iminodiacetyl-based hydroxamate-benzenesulfonamide conjugates
Marques, Sérgio M.,Nuti, Elisa,Rossello, Armando,Supuran, Claudiu T.,Tuccinardi, Tiziano,Martinelli, Adriano,Santos, M. Amélia
supporting information; experimental part, p. 7968 - 7979 (2009/12/07)
Matrix metalloproteinases (MMPs) and carbonic anhydrases (CAs) are two classes of zinc enzymes with different roles and catalytic targets, such as the degradation of most of the extracellular matrix (ECM) proteins and the regulation of the CO2/
Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives
Tamura, Yoshinori,Watanabe, Fumihiko,Nakatani, Takuji,Yasui, Ken,Fuji, Masahiro,Komurasaki, Tadafumi,Tsuzuki, Hiroshige,Maekawa, Ryuji,Yoshioka, Takayuki,Kawada, Kenji,Sugita, Kenji,Ohtani, Mitsuaki
, p. 640 - 649 (2007/10/03)
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.
