35816-87-6Relevant academic research and scientific papers
Identification of anticancer agents based on the thieno[2,3-b]pyridine and 1H-pyrazole molecular scaffolds
Eurtivong, Chatchakorn,Reynisdóttir, Inga,Kuczma, Stephanie,Furkert, Daniel P.,Brimble, Margaret A.,Reynisson, Jóhannes
supporting information, p. 3521 - 3526 (2016/07/20)
Structural similarity search of commercially available analogues of thieno[2,3-b]pyridine and 1H-pyrazole derivatives, known anticancer agents, resulted in 717 hits. These were docked into the phosphoinositide specific-phospholipase C (PLC) binding pocket, the putative target of the compounds, to further focus the selection. Thirteen derivatives of the thieno[2,3-b]pyridines were identified and tested against the NCI60 panel of human tumour cell lines. The most active derivative 1 was most potent against the MDA-MB-435 melanoma cell line with GI50at 30?nM. Also, it was found that a piperidine moiety is tolerated on the thieno[2,3-b]pyridine scaffold with GI50?=?296?nM (MDA-MB-435) for derivative 10 considerably expanding the structure activity relationship for the series. For the 1H-pyrazoles four derivatives were identified using the in silico approach and additionally ten were synthesised with various substituents on the phenyl moiety to extend the structural activity relationship but only modest anticancer activity was found.
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 (2015/11/09)
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
NOVEL COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
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Paragraph 0216-0217, (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 0314, (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.
First total synthesis of highly anti-inflammatory active licochalcone d through water-accelerated [3,3]-sigmatropic rearrangement
Kim, Si-Jun,Jun, Jong-Gab
, p. 54 - 58 (2013/08/24)
Licochalcones, derived from the dried roots of Glycyrrhiza inflata, have been reported to show various biological activities including antitumor, antiparasitic, antileishmanial, antioxidative, superoxide scavenging, antibacterial, and PTP1B activity. Lico
Copper(I) iodide: A catalyst for the improved synthesis of aryl propargyl ethers
Bell,Davies,Geen,Mann
, p. 707 - 712 (2007/10/02)
Copper(I) iodide catalyses the reaction between phenols and dialkylpropargyl chlorides to give aryl 1,1-dialkylpropargyl ethers 5 a-k and 7a-e in good yields and purity. These ethers are important as precursors to the 2H-1-benzopyrans 8a-l and 9a-e.
Improved Synthesis of Aryl 1,1-Dimethylpropargyl Ethers
Godfrey, Jollie D.,Mueller, Richard H.,Sedergran, Thomas C.,Soundarajan, Nachimuthu,Colandrea, Vincent J.
, p. 6405 - 6408 (2007/10/02)
An efficient, general, and practical synthesis of aryl 1,1-dimethylpropargyl ethers has been developed.
