- TRICYCLIC COMPOUNDS ACTING ON CRBN PROTEINS
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The present invention discloses a series of tricyclic compounds and use thereof in preparing a medicament for treating a disease related to CRBN protein. Specifically, the present invention discloses a derivative compound of formula (1) or a pharmaceutically acceptable salt thereof.
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- A functional and self-assembling octyl-phosphonium-tagged esculetin as an effective siRNA delivery agent
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Herein, we document a self-assembling octyl-TPP tagged esculetin (Mito-Esc) as functionally active and as a novel small molecule siRNA delivery vector. While Mito-Esc itself induces selective breast cancer cell death, the amphiphilic nature of Mito-Esc delivers therapeutic siRNAs intracellularly without the need for any excipient to exacerbate the anti-proliferative effects.
- Shaikh, Altab,Neeli, Praveen Kumar,Singuru, Gajalakshmi,Panangipalli, Sravya,Banerjee, Rajkumar,Maddi, Sridhar Reddy,Thennati, Rajamannar,Bathula, Surendar Reddy,Kotamraju, Srigiridhar
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supporting information
p. 12329 - 12332
(2021/12/07)
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- Effect of the Chromone Core Substitution of Dirchromone on the Resultant Biological Activities
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Dirchromone is a bioactive vinyl sulfoxide-bearing chromone first isolated from the shrub Dirca palustris. Altogether, 32 of its derivatives were prepared to assess the effect of substitution of its chromone core upon activities against cancer cell lines, Gram-positive bacteria, and fungi (such as Candida albicans). All compounds were synthesized following a synthetic strategy involving Pummerer and soft-enolization Baker-Venkataraman rearrangements. Substituent position changes induced little variability on the activities tested. There was no correlation between cytotoxic and antibacterial effects, suggesting different underlying mechanisms of action. In particular, hydroxy group and cyanide substituents diminished cytotoxicity, with the latter featuring enhanced antibacterial activity. Higher homologues of 6-alkoxydirchromones also exhibited progressively emerging antifungal activity. Other modifications had moderate effects on cytotoxicity with some derivatives leading to increased potency. This behavior highlights the robustness of the natural dirchromone pharmacophore toward decoration, thus paving the way for more elaborate future drug design.
- St-Gelais, Alexis,Alsarraf, Jér?me,Legault, Jean,Plourde, Joanne,Pichette, André
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p. 2786 - 2794
(2021/12/02)
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- Compound with HMG-CoA reductase inhibitory activity, pharmaceutical composition and application thereof
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The invention belongs to the field of biological medicines, and particularly discloses a compound shown as a formula I and used for treating and/or preventing HMG-CoA reductase related diseases or pharmaceutically acceptable salt or ester of the compound. The invention also discloses a pharmaceutical composition containing the compound. In addition, the invention also provides an application of the compound as an HMG-CoA reductase inhibitor and in preparation of drugs for treating and/or preventing HMG-CoA reductase related diseases. The compound provided by the invention has relatively strong activity of inhibiting HMG-CoA reductase, the prepared medicine is expected to have a relatively good effect on treating and/or preventing dyslipidemia and atherosclerosis, and the compound is relatively simple in structure and relatively low in expected price. In addition, the structure of the compound provided by the invention is completely different from that of the existing statins, and the phenomenon of drug resistance to the existing statins can be overcome.
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Paragraph 0032; 0040-0042
(2021/05/05)
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- In the mists of a fungal metabolite: An unexpected reaction of 2,4,5-trimethoxyphenylglyoxylic acid
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The reactions of phenylglyoxylic acids during the synthesis and biological evaluation of fungal metabolites led to the discovery of hitherto unknown compounds with a p-quinone methide (p-QM) structure. The formation of these p-QMs using 13C-lab
- Csuk, René,Liebing, Phil,Loesche, Anne,Serbian, Immo,Sommerwerk, Sven,Str?hl, Dieter
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- A 2, 4, 5 - trihydroxy - 3 - bromophenylmethyl synthetic method (by machine translation)
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The invention discloses a 2, 4, 5 - trihydroxy - 3 - bromophenylmethyl synthetic method, steps are as follows: the raw material is dissolved in tetrahydrofuran, then adding N - bromosuccinimide, add sulfuric acid reaction 48 hours to obtain the target com
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Paragraph 0021; 0022
(2018/06/15)
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- A facile total synthesis of neurotrophic metabolite (+/-)-neuchromenin
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The synthesis of (+/-)-neuchromenin, a known natural product that induces neurite outgrowth of PC12 cells, is described. The total synthesis involved constructing a chromone ring from sesamol and coupling this intermediate to an aldehyde by a Morita-Baylis-Hillman reaction (MBH). The MBH adduct was cyclized under acidic conditions followed by removal of a methylene group to afford (+/-)-neuchromenin in 9 steps from sesamol.
- Ramos, Josierika A. Ferreira,Nagem, Tanus J.,Taylor, Jason G.
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p. 194 - 196
(2014/05/20)
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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 0470
(2013/03/26)
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- Inhibitors for expression of IgE receptor on human mast cell from Puerariae Flos
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Bioassay-guided separation of the extract of the medicinal plant, Puerariae Flos, disclosed the two isoflavones tectorigenin (1) and genistein (2) as the inhibitors for expression of IgE receptor (FcRI), the key molecule triggering the allergic reactions, on human mast cells. As a result of analysis of structure-activity relationship of the naturally occurring and synthesized isoflavones, 7-O-methyl glycitein (11) was disclosed as the more potent inhibitor than tectorigenin (1). These isoflavone ingredients suppressed expression of FcRI more potently than the active flavonoids found previously. In addition, tectorigenin (1) was clarified to particularly reduce generation of γ-chain subunit to suppress expression of FcRI among the three subunits.
- Tamura, Satoru,Yoshihira, Kunichika,Tokumaru, Mariko,Zisheng, Xu,Murakami, Nobutoshi
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scheme or table
p. 3872 - 3875
(2010/08/19)
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- Structure-activity relationship studies of flavonoids as potent inhibitors of human platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2
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Human lipoxygenase (hLO) isozymes have been implicated in a number of disease states and have attracted much attention with respect to their inhibition. One class of inhibitors, the flavonoids, have been shown to be potent lipoxygenase inhibitors but their study has been restricted to those compounds found in nature, which have limited structural variability. We have therefore carried out a comprehensive study to determine the structural requirements for flavonoid potency and selectivity against platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2. We conclude from this study that catechols are essential for high potency, that isoflavones and isoflavanones tend to select against 12-hLO, that isoflavans tend to select against 15-hLO-1, but few flavonoids target 15-hLO-2.
- Vasquez-Martinez, Yesseny,Ohri, Rachana V.,Kenyon, Victor,Holman, Theodore R.,Sepulveda-Boza, Silvia
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p. 7408 - 7425
(2008/09/18)
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- A synthesis of ayapin
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Ayapin (6) has been synthesised from 4-hydroxy-6,7-methylenedioxybenzopyran-2(H)-one (4) by the method of tosylation and reductive detosyloxylation. 4-Chloroayapin (7) has also been synthesised from 4 by the reaction with phosphorus oxychloride.
- Soman, Shubhangi S.,Trivedi, K. N.
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p. 372 - 373
(2007/10/02)
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- Synthetic aci-Reductones: 3,4-Dihydroxy-2H-1-benzopyran-2-ones and Their cis- and trans-4a,5,6,7,8,8a-Hexahydro Diastereomers. Antiaggregatory, Antilipidemic, and Redox Properties Compared to Those of the 4-Substituted 2-Hydroxytetronic Acids
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Synthetic procedures for the elaboration of aci-reductones belonging to the 6- or 7-mono- or bis-substituted-3,4-dihydroxy-2H-1-benzopyran-2-ones (6 - 10) and their cis- and trans-4a,5,6,7,8,8a-hexahydro diastereomers (11, 12) are described.Hexahydrobenzo
- Witiak, Donald T.,Kim, Sung K.,Tehim, Ashok K.,Sternitzke, Kent D.,McCreery, Richard L.,et al.
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p. 1437 - 1445
(2007/10/02)
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