- Synthesis and structure-activity relationship studies of 2,4-thiazolidinediones and analogous heterocycles as inhibitors of dihydrodipicolinate synthase
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Dihydrodipicolinate synthase (DHDPS), responsible for the first committed step of the diaminopimelate pathway for lysine biosynthesis, has become an attractive target for the development of new antibacterial and herbicidal agents. Herein, we report the di
- Christoff, Rebecca M.,Soares da Costa, Tatiana P.,Bayat, Saadi,Holien, Jessica K.,Perugini, Matthew A.,Abbott, Belinda M.
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supporting information
(2021/11/27)
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- Novel Furochromone Derivatives: Synthesis and Anticancer Activity Studies
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Medicinal plant extracts have been used for medical purposes throughout human history. In this study, khellin, having furochromone structure, which is obtained from a well-known traditional medicinal plant, was selected. A series of furochromonyl compounds (K1–K14) were synthesized for their anticancer activities. Furochromonyl compounds (K1–K14) were synthesized by Knoevenagel reaction of substituted 2,4-thiazolidinediones (Ia–j)/rhodanines (Ik–n) with khellin-2-carboxaldehyde (V), and their cytotoxicity was investigated in 22 cancer cell lines, which were originated from tissues such as the liver, breast, colon, and cervix. As the first step, two hepatocellular carcinoma cell lines Huh7 and PLC/PRF/5 (Alexander cells) were treated with 10?μM of each compound for 72?h, and then sulforhodamine B assay was performed to analyze their anti-growth activities. Ethyl 2-(5-((4,9-dimethoxy-5-oxo-5H-furo[3,2-g]chromen-7-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)acetate (K11) was found as the most cytotoxic compound of primary screening. Afterwards, 12 hepatocellular carcinoma, seven breast cancer, two colon cancer, and a cervical cancer cell lines were selected to test K11 for 72?h at multiple concentrations to determine 50% effective doses. Results showed that the 14 cell lines were affected by K11 quantities lower than 10?μM. The structure of K11, which is particularly effective on breast cancers, can be used to slow down the progression of tumors. Furthermore, the discovery of more effective compounds can be carried out on the basis of this structure.
- Demir, Senem,?zen, Cigdem,Ceylan-ünlüsoy, Meltem,?ztürk, Mehmet,Bozda?-Dündar, Oya
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p. 1341 - 1351
(2019/03/07)
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- HETEROCYCLIC INHIBITORS OF LYSINE BIOSYNTHESIS VIA THE DIAMINOPIMELATE PATHWAY
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The present invention relates to certain heterocyclic compounds of formula (1) that have the ability to inhibit lysine biosynthesis via the diaminopimelate biosynthesis pathway in certain organisms. As a result of this activity these compounds can be used
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Paragraph 0195
(2018/11/10)
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- Development of Phenothiazine-Based Theranostic Compounds That Act Both as Inhibitors of β-Amyloid Aggregation and as Imaging Probes for Amyloid Plaques in Alzheimer's Disease
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Early detection of Alzheimer's disease (AD) is imperative in enabling the understanding and clinical treatment of this disorder, as well as in preventing its progression. Imaging agents specifically targeting Aβ plaques in the brain and the retina may lead to the early diagnosis of AD. Among them, near-infrared fluorescent (NIRF) imaging has emerged as an attractive tool to noninvasively identify and monitor diseases during the preclinical and early stages. In the present study, we report the design, synthesis, and evaluation of a series of new near-infrared fluorescent probes. Most of these probes displayed maximum emission in PBS (>650 nm), which falls in the good range for NIRF probes. Among them, 4a1 showed the highest affinity toward Aβ aggregates (Kd = 7.5 nM) and an excellent targeting ability for Aβ plaques in slices of brain and retina tissue from double transgenic mice. These compounds are also found to effectively prevent Aβ fibril formation and disaggregate preformed Aβ fibrils, showing a promising potential as theranostic agents for the diagnosis and therapy of AD.
- Dao, Pascal,Ye, Feifei,Liu, Yan,Du, Zhi Yun,Zhang, Kun,Dong, Chang Zhi,Meunier, Bernard,Chen, Huixiong
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p. 798 - 806
(2017/04/26)
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- Novel phenothiazine derivative and preparation method and application thereof
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The invention discloses a novel phenothiazine derivative and a preparation method and application thereof, and belongs to the technical field of biological medicines. The invention particularly discloses a compound of a structural general formula I and salts, applicable in pharmacy, of the compound, and the compound and the salts can be used as near-infrared fluorescent molecular probes. The invention further provides a preparation method of the molecular probes and application of the molecular probes. Fluorescent molecules are novel in structure, good in sensitivity and selectivity and good in light stability. The molecules and Abeta(1-42) aggregates have good affinity, and meanwhile auto-polymerization of beta-amyloid protein can be well inhibited. Therefore, the probes can be applied to imaging of Abeta amyloid plaque and can be used for treating the Alzheimer's disease.
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Paragraph 0063; 0064; 0065
(2017/01/02)
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- RADIOACTIVE IODINE LABELED ORGANIC COMPOUND OR SALT THEREOF
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The present invention is a compound represented by the following formula (1) or a salt thereof. Furthermore, the present invention is an imaging agent used for imaging a tau protein, the imaging agent containing a compound represented by the formula (1) b
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Page/Page column 5
(2013/02/28)
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- Rhodanine-based tau aggregation inhibitors in cell models of tauopathy
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Breaking up the crowd: The pathological aggregation of tau protein correlates closely with the progression of Alzheimer's disease. Rhodanine-based inhibitors of tau aggregation (e.g. 1) have been identified, and it has been shown that tau aggregation in a
- Bulic, Bruno,Pickhardt, Marcus,Khlistunova, Inna,Biernat, Jacek,Mandelkow, Eva-Maria,Mandelkow, Eckhard,Waldmann, Herbert
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p. 9215 - 9219
(2008/12/22)
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- Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCV NS3 protease inhibitor
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Arylalkylidene rhodanines 2(a-d) inhibit HCV NS3 protease at moderate concentrations. They are better inhibitors of other serine proteases such as chymotrypsin and plasmin. However, the selectivity of arylmethylidene rhodanines (8a, 9a) with bulkier and more hydrophobic functional groups increases by 13- and 25-fold towards HCV NS3 protease respectively.
- Sing, Wan Theng,Lee, Cheng Leng,Yeo, Su Ling,Lim, Siew Pheng,Sim, Mui Mui
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