- Smo inhibitor as well as synthesis method and application thereof
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The invention discloses an Smo inhibitor as well as a synthesis method and application thereof. A structural formula of the Smo inhibitor is shown by a formula (I) as shown in the specification. The invention also discloses the synthesis method and the application of the Smo inhibitor. According to the invention, nilotinib is optimized into the dual-targeted inhibitor being active against Smo andBcr-Abl, and the inhibitor can overcome the tolerance problem caused by single-targeted drugs, has the advantages of improving anti-tumor efficacy and reducing toxic or side effects, and provides a reference for future research on dual-targeted anti-hematologic malignant drugs.
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Paragraph 0044; 0045; 0048-0051
(2019/09/17)
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- A bodipy based hydroxylamine sensor
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With this research, we have developed a bodipy based system as the first "turn-on" fluorescence system for the detection hydroxylamine.
- Sedgwick, Adam C.,Chapman, Robert S. L.,Gardiner, Jordan E.,Peacock, Lucy R.,Kim, Gyoungmi,Yoon, Juyoung,Bull, Steven D.,James, Tony D.
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supporting information
p. 10441 - 10443
(2017/09/25)
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- Design, synthesis and in vivo anti-hyperglycemic activity of gem-dimethyl-bearing C-glucosides as SGLT2 inhibitors
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A series of gem-dimethyl-bearing C-glucosides were designed and synthesized as SGLT2 inhibitors, with anhydrous aluminum chloride-mediated Friedel-Crafts alkylation to construct the gem-dimethyl functionality being the key step. The in vivo anti-hyperglycemic activity was evaluated with mice oral glucose tolerance test (OGTT), and all the synthesized compounds showed significant but less potent anti-hyperglycemic activity than the positive control dapagliflozin.
- Zhao, Wen Jing,Shi, Yong Heng,Zhao, Gui Long,Wang, Yu Li,Shao, Hua,Da Tang, Li,Wang, Jian Wu
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scheme or table
p. 1215 - 1218
(2012/02/02)
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- Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines
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A series of tricyclic carboxylic acids having 6-amino-pyrimidine-2,4(1H,3H) -dione with piperazino or homopiperazino moiety linked by propylene, were synthesized and evaluated for their affinity toward human histamine H 1 receptor and Caco-2 cell permeability. Selected compounds were further evaluated for their oral anti-histaminic activity in mice, bioavailability in rats, and their anti-inflammatory activity in mice OVA-induced biphasic cutaneous reaction model. Among the compounds tested, dibenzoxazepine carboxylic acid 13b showed both histamine H1 receptor antagonistic activity and anti-inflammatory activity in vivo. In addition, 13b exhibited low affinity toward α1 receptor and low occupancy of H1 receptor in the brain. It is therefore, believed that 13b is a potential candidate for development as 3rd generation anti-histamine.
- Kubota, Katsumi,Kurebayashi, Hirotaka,Miyachi, Hirotaka,Tobe, Masanori,Onishi, Masako,Isobe, Yoshiaki
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experimental part
p. 3005 - 3021
(2011/06/19)
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- Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury
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A novel series of benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines were designed and synthesized as Na+/H+exchanger inhibitors. Most of them were found to inhibit NHE1-mediated platelet swelling in a concentration-dependent manner, and to have significant cardioprotective effect against myocardial ischemic-reperfusion injury, among which compounds 10a and 34 were more potent than cariporide in both in vivo and in vitro tests.
- Zhang, Rui,Lei, Lin,Xu, Yun-Gen,Hua, Wei-Yi,Gong, Guo-Qing
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p. 2430 - 2433
(2008/04/18)
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- Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors
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A series of 3-substituted benzamide derivatives structurally related to STI-571 (imatinib mesylate), a Bcr-Abl tyrosine kinase inhibitor used to treat chronic myeloid leukemia (CML), was prepared and evaluated for antiproliferative activity against the Bc
- Asaki, Tetsuo,Sugiyama, Yukiteru,Hamamoto, Taisuke,Higashioka, Masaya,Umehara, Masato,Naito, Haruna,Niwa, Tomoko
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p. 1421 - 1425
(2007/10/03)
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- AMIDE DERIVATIVE
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The present invention provides an amide derivative represented by the following general formula (1): wherein R1 represents a saturated cyclic amino group, R2 represents alkyl, halogen or haloalkyl, R3 represents hydrogen or halogen, Het 2 represents pyridyl or pyrimidinyl, and Het 1 represents a group of the formula [6], or a salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention is useful as a BCR-ABL tyrosine kinase inhibitor.
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Page/Page column 13
(2008/06/13)
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- Synthesis and properties of an optically active helical bis-cobaltocenium ion
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The optically active helical bis-cobaltocenium salt 6 is synthesized, as are two related monocobaltocenium salts, 29 and 30. The structure of 6 is analyzed by X-ray diffraction, which shows that the metals are separated by 8.49 ?. Reducing 6 either electrochemically or with K(Hg) produces species that absorb near 920 nm, but the absorption is not an intervalence transition. It originates instead from isolated Co(II) centers. This is demonstrated by the reduction product of 29, which has only one cobalt, also absorbing at a similar wavelength (λmax, = 957 nm). The optical and ESR spectra imply that the unpaired electron in monoreduced 6 is largely localized on cobalt and that direduced 6 is essentially a Co(II)Co(II) diradical. The difference between two Co(III)/Co(II) reduction potentials of 6, 130 mV, is shown to be appropriate for a conjugated dimetallocene with metals so distant. Crystal data for 6: M = 1275.02; orthorhombic, space group P212121; Z = 4; a = 11.560(4), b = 12.244(3), and c = 41.349(17) ?; V = 5852.5 ?3; R = 0.1137 for 4653 reflections having Fo ≥ nσ(Fo) (n = 7.5).
- Gilbert, Adam M.,Katz, Thomas J.,Geiger, William E.,Robben, Matthew P.,Rheingold, Arnold L.
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p. 3199 - 3211
(2007/10/02)
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