- Synthesis and in vitro antitumour activity of carboplatin analogues containing functional handles compatible for conjugation to drug delivery systems
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We describe herein the synthesis of a series of carboplatin derivatives with different functional groups at position 3 of the cyclobutane ring. This pharmacomodulation approach aims at facilitating the vectorisation of these analogues, via their subsequen
- Re?nik, Lisa-Maria,Cantelli, Christophe,Fersing, Cyril,Gongora, Céline,Pouget, Jean-Pierre,Lisowski, Vincent
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supporting information
(2020/09/11)
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- Synthesis and anticancer activity of diam(m)ine platinum(II) complexes with 3-oxo-cyclobutane-1,1-dicarboxylate as the leaving group
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Four water-soluble dia(m)mine platinum complexes with 3-oxo-cyclobutane- 1,1-dicarboxylate as the leaving group have been synthesized. These compounds were evaluated for their in vitro anticancer activity against three human A549, SK-OV-3, and HT-29 cance
- Tian, Wen,He, Ling
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p. 8725 - 8733
(2015/02/19)
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- Potent anticancer activity and possible low toxicity of platinum(II) complexes with functionalized 1,1-cyclobutanedicarboxylate as a leaving ligand
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Two platinum(II) complexes, DN603 and DN604, were designed and prepared by using 3-oxocyclobutane-1,1-dicarboxylate as a ligand. The compounds were prepared according to the concept that incorporation of a functionalized moiety in the leaving ligand that
- Zhao, Jian,Gou, Shaohua,Liu, Fengfan
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p. 15216 - 15225
(2015/01/09)
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- COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
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The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases.
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Paragraph 0543-0551
(2013/03/26)
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- Synthesis of spiro[26]nonadienones and spiro[3.6]decadienones by the reaction of cyclopropyl- and cyclobutylmagnesium carbenoids with lithium phenolates and naphtholates
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Treatment of 1-chlorocyclopropyl p-tolyl sulfoxides and 1-chlorocyclobutyl p-tolyl sulfoxides with a Grignard reagent at low temperature afforded cyclopropylmagnesium carbenoids and cyclobutylmagnesium carbenoids, respectively, via a sulfoxide-magnesium e
- Satoh, Tsuyoshi,Kimura, Tsutomu,Sasaki, Yuki,Nagamoto, Shinobu
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supporting information; experimental part
p. 2091 - 2101
(2012/08/27)
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- CYSTEINE PROTEASE INHIBITORS
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Compounds of the formula (I) wherein One of A1 and A2 is N-CH3 and the other is CH; R1 is C1-C6alkyl, C1-C6haloalkyl, C3-C6cycloalkyl or oxetan-3-yl, wherein C3-C6cycloalkyl is optionally substituted with one, two or three fluoro or with CF3; R2a and R2b are independently selected from H, halo, C1-C4alkyl, C1-C4haloalkyl and C1- C4alkoxy; R3 is CH3 or F; n is 1, 2, 3 or 4; or a pharmaceutically acceptable salt, hydrate or N-oxide thereof for the use in the prophylaxis and/or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
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Page/Page column 21
(2013/02/28)
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- Antitumor platinum(II) complexes containing platinum-based moieties of present platinum drugs and furoxan groups as nitric oxide donors: Synthesis, DNA interaction, and cytotoxicity
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Six novel platinum(II) complexes 1-6 bearing different furoxan moieties as nitric oxide (NO) donors have been designed, synthesized, and characterized by elemental analysis and 1H NMR, IR, and ESI-MS spectroscopy. The furoxan groups were introduced to the platinum complexes to release NO, which may take synergic action with the platinum-based moieties on the tumor cells. It was found that all compounds exhibited considerable cytotoxicity against human HCT-116 and SGC-7901 cell lines via DNA binding together with NO-releasing features, especially for compound 3. This finding is in accordance with the previous reports that NO hybrids show higher cytotoxicity against colon cancer cell lines compared with their parent compounds.
- Zhao, Jian,Gou, Shaohua,Sun, Yanyan,Fang, Lei,Wang, Zhimei
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p. 10317 - 10324
(2013/01/15)
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- Nitric oxide donor-based platinum complexes as potential anticancer agents
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Joining forces: Platinum complexes containing organic nitrate ligands were investigated as anticancer agents. The complexes, which were stable in aqueous solution, showed cytotoxicity that was superior to that of the corresponding parent compound (carbopl
- Zhao, Jian,Gou, Shaohua,Sun, Yanyan,Yin, Runting,Wang, Zhimei
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p. 14276 - 14281
(2013/01/15)
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- NEW CATHEPSIN S PROTEASE INHIBITORS, USEFUL IN THE TREATMENT OF E.G. AUTOIMMUNE DISORDERS, ALLERGY AND CHRONIC PAIN CONDITIONS
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Compounds of the formula (I) wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together wi
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- CYSTEINE PROTEASE INHIBITORS
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Compounds of Formula (II) wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R
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Page/Page column 24-25
(2011/06/26)
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- CYSTEINE PROTEASE INHIBITORS
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Compounds of the formula (I) wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and Rs
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Page/Page column 24
(2011/06/26)
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- Potent ketoamide inhibitors of HCV NS3 protease derived from quaternized P1 groups
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Blood borne hepatitis C infections are the primary cause for liver cirrhosis and hepatocellular carcinoma. HCV NS3 protease, a pivotal enzyme in the replication cycle of HCV virus has been the primary target for development of new drug candidates. Boceprevir and telaprevir are two novel ketoamide derived inhibitors that are currently undergoing phase-III clinical trials. These inhibitors include ketoamide functionality as serine trap and have an acidic alpha-ketoamide center that undergoes epimerization under physiological conditions. Our initial attempts to arrest this epimerization by introducing quaternary amino acids at P1 had resulted in significantly diminished activity. In this manuscript we describe alpha quaternized P1 group that result in potent inhibitors in the enzyme assay and demonstrate cellular activity comparable to boceprevir.
- Venkatraman, Srikanth,Velazquez, Francisco,Wu, Wanli,Blackman, Melissa,Madison, Vincent,Njoroge, F. George
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scheme or table
p. 2151 - 2155
(2010/06/19)
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- CYSTEINE PROTEASE INHIBITORS
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Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and Rsu
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Page/Page column 28; 29
(2010/08/05)
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- P1-NONEPIMERIZABLE KETOAMIDE INHIBITORS OF HCV NS3 PROTEASE
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The present invention discloses novel compounds, which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
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Page/Page column 60
(2009/03/07)
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- CARBOPLATIN-TYPE PLATINUM (II) COMPLEXES
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The invention relates to carboplatinum derivatives, medicaments containing said derivatives and to the use of the carboplatinum derivatives in the production of medicaments for tumour therapy.
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Page/Page column 12-14
(2008/06/13)
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- Synthesis and Activity of a Potent N-Methyl-D-aspartic Acid Agonist, trans-1-Aminocyclobutane-1,3-dicarboxylic Acid, and Related Phosphonic and Carboxylic Acids
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We report the synthesis of a series of 3-carboxy-, 3-(carboxymethyl)-, 3-(1o-phosphoalkenyl)-, and 3-(1o-phosphonoalkyl)-1-aminocyclobutane-1-carboxylic acids for evaluation as agonists or antagonists of neurotransmission at excitatory amino acid receptor
- Allan, Robin D.,Hanrahan, Jane R.,Hambley, Trevor W.,Johnston, Graham A. R.,Mewett, Kenneth N.,Mitrovic, Ann D.
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p. 2905 - 2915
(2007/10/02)
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