98165-65-2Relevant academic research and scientific papers
An HDAC8-selective fluorescent probe for imaging in living tumor cell lines and tissue slices
Huang, Chaoqun,Li, Wei,Liu, Jian,Shan, Chenxiao,Shu, Yi,Wang, Xinzhi,Wen, Hongmei,Yan, Yinyu
, p. 8352 - 8366 (2021/10/14)
Histone deacetylase 8 (HDAC8) has been used as a therapeutic target for many cancers as it is highly expressed in neuroblastoma cells and breast cancer cells. HDAC8-selective fluorescent probes need to be urgently developed. Herein, two novel fluorescent probes, namelyNP-C6-PCIandAM-C6-PCI, based on the conjugation of 1,8-naphthalimide with a highly selective inhibitor of HDAC8 (PCI-34051) were reported. Compared withPCI-34051(KD= 6.25 × 10?5M),NP-C6-PCI(KD= 8.05 × 10?6M) andAM-C6-PCI(KD= 7.42 × 10?6M) showed great selectivity toward HDAC8. Two fluorescent probes exhibited high fluorescence intensity underλex= 450 nm and a large Stokes shift (100 nm).NP-C6-PCIwas selected for cell and tissue imaging due to the similarity in the bioactivity ofNP-C6-PCIwithPCI-34051. The ability ofNP-C6-PCIto target imaging HDAC8 in SH-SY5Y and MDA-MB-231 tumor cells was demonstrated. Furthermore,NP-C6-PCIwas applied to imaging SH-SY5Y tumor tissue slices to indicate the relative expression level of HDAC8. Therefore, this HDAC8-selective fluorescent probe can be expected for applications in HDAC8-targeted drug screening as well as in pathologic diagnoses.
NOVEL ADENINE COMPOUND AND USE THEREOF
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Page/Page column 29, (2010/02/12)
A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene; etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents -COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.
Indazole compounds, pharmaceutical compositions and use
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, (2008/06/13)
The invention provides a series of novel heterocyclic amides of the formula I in which the group A CRa can be --CRb=CRa--, --CHRb--CHRa-- or --N=CRa--, the amidic group Re.L can be Re.X.CO.NH, Re.X.CS.NH or Re.NH.CO attached at position 4, 5 or 6 of the benzenoid moiety, Z is an acid group selected from the group consisting of carboxy, an acylsulphonamide residue of the formula CO.NH.SOn Rg and a tetrazolyl residue of the formula II, and the radicals Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh, n, X, G1, Q and G2 have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compounds, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.
