- AROMATIC-SUBSTITUTED XANTHENE DYE
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PROBLEM TO BE SOLVED: To provide a useful compound used for independent detection of multiple spatially overlapping analytes in a mixture, for example, single-tube multiplex DNA probe assays, immunoassays, multicolor DNA sequencing methods and the like. SOLUTION: There is provided an aromatic-substituted xanthene dye represented by the following formula. (Y1 and Y2 each independently represents hydroxyl, oxygen, iminium, a linking group or an amine; Y1 forms a cyclic amine together with R2 or Y2 forms a cyclic amine together with R3; R2, R3, R5 and R7 each independently represents H, F, Cl, a lower alkyl, a lower alkene, sulfonate, sulfone, iminium, amide, nitrile, a lower alkoxy, phenyl or a linking group; R1 represents a single ring or a polycyclic aromatic or the like; R4 represents H, F, alkyl, amino or the like; and R6 represents acetylene, a lower alkyl or the like.) COPYRIGHT: (C)2015,JPO&INPIT
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Paragraph 0195; 0197
(2016/12/22)
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- ANTICANCER AGENT
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An anticancer agent comprising a compound represented by the formula (I) [R1 represents hydrogen atom, hydroxyl group, a C1-6alkoxy group and the like; R2 and R3 represents hydrogen atom, a halogen atom, a C1-6alkyl group and the like; R4 represents hydrogen atom, a C1-6alkyl group, a C1-6alkylsulfonyl group and the like; R5 represents hydrogen atom or a substituent; .... represents a single bond or a double bond; R6 and R7 represents hydrogen atom, a C1-6alkyl group and the like; R8 represents hydrogen atom, a C1-6alkyl group and the like; A represents -O-, -S-, or - CH2-; D represents -C= or -N=; X represents methylene group, -O-, or -CO-; Q represents -N= or -C(R8)=; and Y represents a heterocyclic group or amino group], which shows a superior inhibitory activity against pim-1 kinase.
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Paragraph 0180
(2013/03/26)
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- Synthesis, activity and molecular modeling of a new series of chromones as low molecular weight protein tyrosine phosphatase inhibitors
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Protein tyrosine phosphatases (PTP) are crucial elements in eukaryotic signal transduction. Several reports suggested that the LMW-PTP family has oncogenic relevance. Moreover, LMW-PTP has been recognized as a negative regulator of insulin-mediated mitotic and metabolic signaling. Thus, inhibition of the LMW-PTP can be considered an attractive approach for the design of new therapeutic agents for the treatment of type II diabetes and for new antitumoral drugs. To date very few (and weak) inhibitors of LMW-PTP have been identified. On the basis of the reported weak activity of some flavonoids on phosphatases, we discovered a lead that originated a new class of highly active LMW-PTP inhibitors; these compounds inhibit also PTP-1B and are active in cellular assays. Docking experiments and SAR highlighted the possible binding mode of these compounds to the enzyme, putting the background for the future optimization of their inhibitory activity and selectivity towards the closely related enzyme PTP-1B.
- Forghieri, Marco,Laggner, Christian,Paoli, Paolo,Langer, Thierry,Manao, Giampaolo,Camici, Guido,Bondioli, Lucia,Prati, Fabio,Costantino, Luca
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experimental part
p. 2658 - 2672
(2009/09/08)
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