- Synthesis, structure and antitumor activity of a new water-soluble platinum complex, (1R,2R-cyclohexanediamine-N,N')[2-hydroxy-4-oxo-2-pentenoato(2-)-O2]p latinum(II)
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The reaction of dihydroxo(1R,2R-cyclohexanediamine)platinum(II) with 2,4-dioxopentanoic acid gave a water-soluble complex, (1R,2R-cyclohexanediamine-N,N')[2-hydroxy-4-oxo-2-pentenoato(2-)-O2]p latinum(II). The structure of the complex was determined by X-ray crystal analysis. The data indicated a chelation of the acetylacetonato part of 2,4-dioxo-pentanoic acid to platinum(II). The complex showed moderate antitumor activity against murine leukemia L1210 in mice (T/C = 195% at a dose of 200 mg/kg) and high activity against cisplatin-resistant L1210 leukemia (T/C = 275% at a dose of 25 mg/kg).
- Kawai,Kitano,Mutoh,Hata
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Read Online
- Benzoxadiazepine tetradecene derivative and application thereof
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The invention discloses a benzoxadiazepine tetradecene derivative and application thereof, belonging to the field of medicines. The benzoxadiazepine tetradecene derivative with a structure as shown ina general formula (I) has excellent anaplastic lymphoma enzyme (ALK) inhibition activity and excellent pharmacodynamic performance, and can obviously prolong the large metabolic half-life period of adrug; the derivative can be safely and effectively used for treating anaplastic lymphoma kinase positive (ALK+) metastatic (advanced) non-small cell lung cancer (NSCLC) and the like, thereby providing a new means for treating cancers, metabolic and immune diseases, cardiovascular diseases, neurological diseases and the like.
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Paragraph 0075-0079
(2020/07/15)
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- With anti-tumor activity of the 3-substituted pyrazole-5-amide compound and use thereof (by machine translation)
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The invention belongs to the field of medical technology, relates to a sulfenyl class with anti-tumor activity of the compounds, in particular to a thio-containing the 3-substituted pyrazole-5-amide compounds, and its pharmaceutically acceptable salt, hydrate, and the compound is a pharmaceutical composition of the active ingredient, the preparation and and its histone deacetylase inhibitor for the treatment and/or use in the prevention of cancer. The compounds of general formula I to shows, and its pharmaceutically acceptable salt, hydrate structure is as follows :? wherein R 1, R 2 such as the claim and the specification. (by machine translation)
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Paragraph 0077; 0078; 0079
(2016/10/09)
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- Synthesis, Acaricidal Activity, and Structure-Activity Relationships of Pyrazolyl Acrylonitrile Derivatives
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A series of novel pyrazolyl acrylonitrile derivatives was designed, targeting Tetranychus cinnabarinus, and synthesized. Their structures were identified by combination of1H NMR,13C NMR, and MS spectra. The structures of compounds 18 and 19 were further confirmed by X-ray diffraction. Extensive greenhouse bioassays indicated that compound 19 exhibits excellent acaricidal activity against all developmental stages of T. cinnabarinus, which is better than the commercialized compounds cyenopyrafen and spirodiclofen. It was shown that the acute toxicity of compounds 19 to mammals is quite low. The structure-activity relationships are also discussed.
- Yu, Haibo,Cheng, Yan,Xu, Man,Song, Yuquan,Luo, Yanmei,Li, Bin
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p. 9586 - 9591
(2017/01/12)
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- SMALL MOLECULE INHIBITORS OF MCL-1 AND USES THEREOF
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This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having pyrazolopyridine structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
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Paragraph 0138
(2015/10/28)
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- Pyrazole derivatives as inhibitors of arachidonic acid-induced platelet aggregation
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Antiplatelet drugs are promising therapeutics to intervene with platelet aggregation in arterial thrombosis, most prominently in myocardial infarction and ischemic stroke. Here, we describe the synthesis and structure-activity relationships of potent inhibitors of platelet aggregation based on the 1,5-diarylpyrazol-3-carboxamide scaffold. Analogs from this series demonstrated potent anti-aggregatory activities against arachidonic acid-induced platelet aggregation, as measured by turbidimetric method of Born. 1,5-Diarylpyrazole-3- carboxamides obtained with small-basic amines (7, 8, 50, 51, 61, 62) displayed the strongest activity with IC50 values in low nanomolar range (5.7-83 nM). On the basis of their high potency in cellular environment, these straightforward pyrazole derivatives may possess potential in the design of more potent compounds for intervention with cardiovascular diseases.
- Levent, Serkan,?ali?kan, Burcu,?ift?i, Murat,?zkan, Ye?im,Yenicesu, Idil,ünver, Hüseyin,Banoglu, Erden
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- Practical and scalable synthesis of S1P1 receptor agonist ACT-209905
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A practical and scalable route for the fast delivery of 12 kg of S1P 1 agonist (ACT-209905) has been developed. ACT-209905 is composed of an amino pyridine group, an oxadiazole spacer, a 2-ethyl-5-methylphenol moiety and a chiral 1-amino-2-propanol side chain. The convergent synthesis consists of 16 steps with 9 isolated intermediates and is chromatography-free. Key building blocks are accessed from low-cost starting materials, such as acetone, diethyl oxalate, cyanoacetamide, and 2-ethyl-5-methyl aniline. A Negishi coupling that was troubled by the use of metal reagents and concomitant metal waste streams has been replaced by a less expensive Guareschi-Thorpe reaction to build up an amino isonicotinic acid. The chiral 1-amino-2-propanol moiety was secured by selective ring-opening of an epoxide with lithium hexamethyldisilazide as an ammonia surrogate, thus omitting the notorious double alkylated byproduct.
- Schmidt, Gunther,Reber, Stefan,Bolli, Martin H.,Abele, Stefan
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experimental part
p. 595 - 604
(2012/07/13)
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- 1-Substituted Pyridyl-Pyrazolyl Amide Compounds and Uses Thereof
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The present invention discoses a kind of 1-substituted pyridyl-pyrazolyl amide compounds and uses thereof. The compounds have structures as represented by the general formula I, wherein the definitions of each substituent showed in the specification. The compounds of formula I are novel and have excellent insecticidal and fungicidal activities and can be used for controlling insect pest and diseases.
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Page/Page column 7
(2011/04/14)
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- Synthesis and fluorescence properties of lanthanide(III) complexes of a novel bis(pyrazolyl-carboxyl)pyridine-based ligand
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A novel bis-pyrazolyl-carboxyl ligand, 2,6-bis(5-methyl-3-carboxypyrazol-1-ylmethyl)pyridine (L), was designed and synthesized and its several lanthanide(III) complexes Eu(III), Tb(III), Sm(III) and Gd(III) were successfully prepared and characterized in detail based on elemental analysis, infrared, mass, proton nuclear magnetic resonance spectroscopy and TG-DTA studies. Analysis of the IR spectra suggested that each of the lanthanide metal ions coordinated to the ligand via the carbonyl oxygen atoms and the nitrogen atom of the pyridine ring and pyrazole rings. The fluorescence spectra exhibits that the Tb(III) complex and the Eu(III) complex display characteristic metal-centered fluorescence in solid state while ligand fluorescence is completely quenched. However, the Tb(III) complex displays more effective fluorescence than the other complexes, which is attributed to especial effectivity in transferring energy from the lowest triplet energy level of the ligand (L) onto the excited state (5D4) of Tb(III).
- Shi, Xiao-Ming,Tang, Rui-Ren,Gu, Guo-Liang,Huang, Ke-long
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scheme or table
p. 198 - 203
(2009/03/12)
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