139768-71-1Relevant articles and documents
Structural optimization and structure–activity relationship of 4-thiazolidinone derivatives as novel inhibitors of human dihydroorotate dehydrogenase
Zeng, Fanxun,Quan, Lina,Yang, Guantian,Qi, Tiantian,Zhang, Letian,Li, Shiliang,Li, Honglin,Zhu, Lili,Xu, Xiaoyong
, (2019/08/07)
Human dihydroorotate dehydrogenase (hDHODH), one of the attractive targets for the development of immunosuppressive drugs, is also a potential target of anticancer drugs and anti-leukemic drugs. The development of promising hDHODH inhibitors is in high demand. Based on the unique binding mode of our previous reported 4-thiazolidinone derivatives, via molecular docking method, three new series 4-thiazolidinone derivatives were designed and synthesized as hDHODH inhibitors. The preliminary structure–activity relationship was investigated. Compound 9 of biphenyl series and compound 37 of amide series displayed IC50 values of 1.32 μM and 1.45 μM, respectively. This research will provide valuable reference for the research of new structures of hDHODH inhibitors.
New prodrugs derived from 6-aminodopamine and 4-aminophenol as candidates for melanocyte-directed enzyme prodrug therapy (MDEPT)
Knaggs, Sarah,Malkin, Hugh,Osborn, Helen M.I.,Williams, Nana Aba O.,Yaqoob, Parveen
, p. 4002 - 4010 (2007/10/03)
Two novel tyrosinase mediated drug delivery pathways have been investigated for the selective delivery of cytotoxic units to melanocytes from urea and thiourea prodrugs. The synthesis of these prodrugs is reported, as well as oximetry data that illustrate that the targets are substrates for tyrosinase. The stability of each of the prodrugs in (i) phosphate buffer and (ii) bovine serum is discussed, and the urea prodrugs are identified as lead candidates for further studies. Finally, HPLC studies and preliminary cytotoxicity studies in a melanotic and an amelanotic cell line, that illustrate the feasibility of the approach, are presented. The Royal Society of Chemistry 2005.
Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors
Wilson, Kenneth J.,Illig, Carl R.,Subasinghe, Nalin,Hoffman, James B.,Jonathan Rudolph,Soll, Richard,Molloy, Christopher J.,Bone, Roger,Green, David,Randall, Troy,Zhang, Marie,Lewandowski, Frank A.,Zhou, Zhao,Sharp, Celia,Maguire, Diane,Grasberger, Bruce,DesJarlais, Renee L.,Spurlino, John
, p. 915 - 918 (2007/10/03)
The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis of a series of substituted 4-[2-amino-1,3-thiazolyl]-thiophene-2-carboxamidines is described. Further optimization of this series by substitution of the terminal amine yielded urokinase inhibitors with excellent activities.
Biphenyl-substituted guanidine derivatives useful as hypoglycaemic agents
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, (2008/06/13)
Compounds of formula I STR1 and their salts in which R1 is optionally substituted phenyl, R2 is alkyl, cycloalkyl or optionally substituted amino, or R2 and R3 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R3 and R4 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring and R5 is H, halo, alkyl, alkoxy, trifluoromethyl or a group of formula S(O)m R8 in which m is 0, 1 or 2 and R8 is alkyl have utility in the treatment of diabetes particularly in the treatment of hyperglycaemia.
Anthelmintic 1-(substituted phenyl)-3-alkanimidoyl ureas
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, (2008/06/13)
The compounds of this invention are novel imidoylureas having anthelmintic activity and imidoylthioureas having antifertility activity. They are prepared by the reaction of appropriate amidines with appropriate isocyanates or isothiocyanates.
