- Anti-tumor compound of targeting Neddylation path
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The invention discloses an anti-tumor compound of a targeting Neddylation path. The compound can be represented by a structural formula shown as a general formula I, a general formula II, a general formula III, a general formula IV, a general formula V, a general formula VI or a general formula VII. The compound provided by the invention has good anti-tumor activity; a plurality of compounds are close to a positive control drug MLN4924 and can be used as the good anti-tumor compound. The compound and a composition, provided by the invention, can be used with other drugs to provide combined therapy, and the other drugs can form a part of the same composition or can be used as different components for drug administration at the same time or at different time.
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Paragraph 0038; 0042; 0043; 0044
(2019/01/07)
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- Universal peptidomimetics
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This paper concerns peptidomimetic scaffolds that can present side chains in conformations resembling those of amino acids in secondary structures without incurring excessive entropic or enthalpic penalties. Compounds of this type are referred to here as minimalist mimics. The core hypothesis of this paper is that small sets of such scaffolds can be designed to analogue local pairs of amino acids (including noncontiguous ones) in any secondary structure; i.e., they are universal peptidomimetics. To illustrate this concept, we designed a set of four peptidomimetic scaffolds. Libraries based on them were made bearing side chains corresponding to many of the protein-derived amino acids. Modeling experiments were performed to give an indication of kinetic and thermodynamic accessibilities of conformations that can mimic secondary structures. Together, peptidomimetics based on these four scaffolds can adopt conformations that resemble almost any combination of local amino acid side chains in any secondary structure. Universal peptidomimetics of this kind are likely to be most useful in the design of libraries for high-throughput screening against diverse targets. Consequently, data arising from submission of these molecules to the NIH Molecular Libraries Small Molecule Repository (MLSMR) are outlined.
- Ko, Eunhwa,Liu, Jing,Perez, Lisa M.,Lu, Genliang,Schaefer, Amber,Burgess, Kevin
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supporting information; experimental part
p. 462 - 477
(2011/04/16)
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- Synthesis and antiviral evaluation of C-4-hydrazide derivatives of 2′,3′-dideoxycytidine
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Syntheses of three hitherto unknown derivatives of 2′,3′-dideoxycytidine, namely C-4-(salicylic hydrazide)-ddC, C-4-(N-butyloxycarbonyl-isoleucine hydrazide)-ddC and its N-unprotected chlorhydrate salt have been carried out. These compounds do not induce inhibition of HIV-1 replication in cell culture experiments. Nevertheless, the modifications on the base moiety increased in all cases the lipophilicity of the parent molecule with an acceptable water solubility compared to ddC.
- Boudou-Vivet,Mathe,Gosselin
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p. 1029 - 1032
(2007/10/03)
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