179003-85-1Relevant academic research and scientific papers
Facile syntheses of 3',4'-methylenedioxy-2,2-dimethylpyrano- [5'',6'': 7,8] -flavone and (±)-ponganone III, two pyranoflavanoids
Tan, Wenfei,Li, Wei-Dong Z.,Huang, Chusheng,Li, Yulin,Xing, Yacheng
, p. 3369 - 3377 (1999)
Facile syntheses of two naturally occurring pyranoflavanoids, 3',4'- methylenedioxy-2,2-dimethylpyrano-[5,6'':7,8]-flavone (1) and (±)- ponganone III (2), have been achieved through the key intermediate chromene 6 by a DDQ
Identification of small molecule inhibitors of the STAT3 signaling pathway: Insights into their structural features and mode of action
Kim, Kyeojin,Kim, Su-Jung,Han, Young Taek,Hong, Sung-Jun,An, Hongchan,Chang, Dong-Jo,Kim, Taewoo,Lim, Bumhee,Lee, Jeeyeon,Surh, Young-Joon,Suh, Young-Ger
, p. 5444 - 5448 (2015)
A series of novel STAT3 inhibitors consisting of Michael acceptor has been identified through assays of the focused in-house library. In addition, their mode of action and structural feature responsible for the STAT3 inhibition were investigated. In parti
Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors
Yao, Hong,Xu, Feijie,Wang, Guangyu,Xie, Shaowen,Li, Wenlong,Yao, Hequan,Ma, Cong,Zhu, Zheying,Xu, Jinyi,Xu, Shengtao
, p. 485 - 498 (2019/02/24)
A series of novel B[sbnd] and C-rings truncated deguelin derivatives have been designed and synthesized in the present study as heat shock protein 90 (Hsp90) inhibitors. The synthesized compounds exhibited micromolar antiproliferative potency toward a pan
NOVEL COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
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Paragraph 0419-0422, (2015/05/26)
The present invention relates to a novel compound inhibiting Hsp 90 and to a pharmaceutical composition including same as an active ingredient. Compounds of formula 1 and formula 2 according to the present invention inhibit the accumulation of HIF-1α protein, which is an Hsp90 client protein, by suppressing Hsp90 expression, and effectively inhibit the activity of vascular endothelial growth factor (VEGF). Furthermore, said compounds have low cytotoxicity and can thus be used as an active ingredient for the treatment of diabetic retinopathy and arthritis.
NOVEL COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
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Paragraph 0519-0522, (2015/07/15)
The present invention relates to a compound inhibiting Hsp90 and a pharmaceutical composition comprising the same as an active ingredient. The compounds represented by formula 1 and formula 2 of the present invention suppress the expression of Hsp90 so that they can inhibit the accumulation of HIF-1α, the Hsp90 client protein, and also efficiently inhibit the activation of VEGF. In addition, these compounds display low cytotoxicity, so that they can be effectively used as an active ingredient of an anti-cancer agent, a diabetic retinopathy treating agent, and an anti-arthritic agent.
Synthesis and biological evaluation of pyranoisoflavone derivatives as anti-inflammatory agents
Wei, Zhe,Yang, Youzhe,Xie, Caifeng,Li, Chunyan,Wang, Guangcheng,Ma, Liang,Xiang, Mingli,Sun, Jian,Wei, Yuquan,Chen, Lijuan
, p. 172 - 183 (2014/07/21)
In this paper, barbigerone (1a) and its twenty-seven related structural analogues were synthesized via complementary synthetic routes and their anti-inflammatory effects on the expression of TNF-α in LPS-stimulated splenocytes were evaluated. Among these compounds, 1a, 1d, 1f and 1g were found to remarkably inhibit TNF-α production. Furthermore, 1g showed the most potent and dose-dependent manner inhibitory effect on TNF-α release, with better IC50 value (3.58 μM) than barbigerone (8.46 μM). Oral administration of 1g at 20 mg/kg/day for two weeks obviously demonstrated protective effect in adjuvant-induced arthritis models as evaluated by clinical score of paws, and histological examination of joint tissues from rats. Mechanism studies on mRNA and protein level suggested that 1g inhibited the TNF-α production via depressing TNF-α converting enzyme (TACE) mRNA expression. In conclusion, these data show 1g with potential therapeutic effects as an anti-inflammatory agent.
Rational design, synthesis, and pharmacological properties of pyranochalcone derivatives as potent anti-inflammatory agents
Peng, Fei,Wang, Guangcheng,Li, Xiuxia,Cao, Dong,Yang, Zhuang,Ma, Liang,Ye, Haoyu,Liang, Xiaolin,Ran, Yan,Chen, Jinying,Qiu, Jingxiang,Xie, Caifeng,Deng, Chongyang,Xiang, Mingli,Peng, Aihua,Wei, Yuquan,Chen, Lijuan
, p. 272 - 280 (2012/09/07)
24 derivatives (5a-x) derived from natural pyranochalcones (I and II) were designed and evaluated for their inhibitory potency on the production of nitric oxide (NO) in LPS-stimulated RAW264.7 cells. Among them, four compounds (5b, 5d, 5f, and 5h) exhibit
Natural product-like combinatorial libraries based on privileged structures. 1. General principles and solid-phase synthesis of benzopyrans
Nicolaou,Pfefferkorn,Roecker,Cao,Barluenga,Mitchell
, p. 9939 - 9953 (2007/10/03)
Herein we report a novel strategy for the design and construction of natural and natural product-like libraries based on the principle of privileged structures, a term originally introduced to describe structural motifs capable of interacting with a variety of unrelated molecular targets. The identification of such privileged structures in natural products is discussed, and subsequently the 2,2-dimethylbenzopyran moiety is selected as an inaugural template for the construction of natural product-like libraries via this strategy. Initially, a novel solid-phase synthesis of the benzopyran motif is developed employing a unique cycloloading strategy that relies on the use of a new, polystyrene-based selenenyl bromide resin. Once the loading, elaboration, and cleavage of these benzopyrans was established, this new solid-phase method was then thoroughly validated through the construction of six focused combinatorial libraries designed around natural and designed molecules of recent biological interest.
