92654-79-0Relevant academic research and scientific papers
Benzocarbazoles dioxane derivatives, its preparation process and its use in medicine
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Paragraph 0352; 0355; 0362-0364, (2016/10/10)
The invention relates to a benzodioxane derivative, a preparation method thereof and application of the derivative in medicines. Specifically, the invention relates to a novel benzodioxane derivative shown as a formula (I), medial salt thereof or a medicine composition containing the derivative, and a preparation method of the derivative. The invention further relates to a use of the benzodioxane derivative and the medial salt thereof or the medicine composition containing the derivative in preparing therapeutic agent, especially GPR 40 agonist, and a drug for treating the diseases such as diabetes, metabolic disorders and the like, wherein each substituent group in the formula (I) is as defined in the description.
Six-coordinated ruthenium complex
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Page/Page column 16; 17, (2014/07/22)
A six-coordinated ruthenium complex is represented by the following formula (I): [in-line-formulae]RuL1L2L3??(I)[/in-line-formulae]wherein L1 represents a 2,2′-bipyridine-based bidentate ligand having at least t
Cucurbituril slippage: Cations as supramolecular lubricants
Ling, Xiaoxi,Masson, Eric
supporting information, p. 4866 - 4869 (2013/01/15)
The dethreading rate of a polyaminated axle flanked by two benzo-15-crown-5 stoppers from the cavity of Cucurbit[7]uril (CB[7]) was enhanced by up to 500 times in the presence of aqueous metallic and organic cations. Cations likely stabilize the highest energy transition state of the dethreading process by interacting with both crown ether and CB[7] units.
INHIBITORS OF SPHINGOSINE KINASE
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Page/Page column 76, (2012/10/08)
The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12,
THERAPEUTIC DRUG FOR ADULT T-CELL LEUKEMIA
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Page/Page column 9, (2011/08/02)
An object is to provide a novel therapeutic drug for adult T-cell leukemia having an ATL cell specific antitumor effect. The therapeutic drug for adult T-cell leukemia according to the invention is characterized by containing a compound represented by the formula I or a prodrug thereof, wherein R1 is H, OH, an alkoxy group, an acyl group, or a thioacyl group, R2 is an acyl group, a thioacyl group, CONR7R8, or CSNR7R8 (R7 and R8 being each independently H, an alkyl group containing 1 to 3 carbon atoms, or a phenyl group), or R1 and R2 together may form a ring, X1 and X2 may be the same or different and are each —CR3R4—, —SiR3R4— or oxygen, and R3 and R4 may be the same or different and are each an alkyl group containing 1 to 6 carbon atoms.
Discovery of tetrahydrotetramethylnaphthalene analogs as adult T-cell leukemia cell-selective proliferation inhibitors in a small chemical library constructed based on multi-template hypothesis
Nakamura, Masahiko,Hamasaki, Takayuki,Tokitou, Maiko,Baba, Masanori,Hashimoto, Yuichi,Aoyama, Hiroshi
experimental part, p. 4740 - 4746 (2009/10/10)
Adult T cell leukemia (ATL), caused by infection of human T-lymphotropic virus type 1 (HTLV-1), has a poor prognosis and curative therapy is unavailable, so it is important to find or design superior lead compounds for the drug treatment of ATL. We used our micro-reversed fragment-based drug design hypothesis and multi-template hypothesis to extract the tetrahydrotetramethylnaphthalene (TMN) skeleton from tamibarotene, a useful medicament for the treatment of acute promyelocytic leukemia (APL). Structural development of TMN yielded highly ATL cell-selective growth inhibitors, including 2-acetyl-3-hydroxy-5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalene (6). Structure-activity relationship analysis suggests the existence of a specific target molecule for ATL cell-selective inhibition of proliferation through G2 arrest.
Synthesis of some novel tetrahydronaphthalene benzimidazole derivatives
Ates-Alagoz, Zeynep,Buyukbingol, Erdem
, p. 455 - 460 (2007/10/03)
Retinoids, synthetic and natural analogues of all-trans-retinoic acid (RA), exert their biological effects with responsive elements of DNA to promote on cell differentiation and proliferation and behave as potent adipogenic hormones. Herein, we describe the synthesis of a number of novel tetrahydrotetramethylnaphthalene benzimidazole derivatives as retinoids. Analogs were prepared as depicted in Scheme 1 and 2. As is evident from both shemes, a variety of tetrahydrotetramethylnaphthalene benzimidazole derivatives have been synthesized by using an appropiate NaHSO3 addiction product.
Polyenylidene thiazolidine derivatives with retinoidal activities
Tashima, Toshihiko,Kagechika, Hiroyuki,Tsuji, Motonori,Fukasawa, Hiroshi,Kawachi, Emiko,Hashimoto, Yuichi,Shudo, Koichi
, p. 1805 - 1813 (2007/10/03)
Several polyenylidene thiazolidinedione or 2-thioxo-4-thiazolidinone derivatives were synthesized and their retinoidal activities were examined in terms of the differentiation-inducing ability towards human promyelocytic leukemia HL-60 cells and inhibitory effect on interleukin (IL)-1α-induced IL-6 production in MC3T3-E1 cells. Compounds containing a trimethylcyclohexenyl ring induced HL-60 cell differentiation with weaker activity than retinoic acid (1a) by one or two orders of magnitude. The thiazolidinedione derivatives (2, 5, 7) showed stronger activity than the corresponding 2-thioxo-4-thiazolidinone derivatives (3, 6, 8). The effects of a retinoid antagonist (LE540) and synergists (retinoid X receptor (RXR) agonists, HX600 or HX630) on the activities of thiazolidine derivatives indicate that these compounds elicit their activities through the nuclear retinoic acid receptors (RARs). All the thiazolidines examined also inhibited IL-1α-induced IL-6 production with IC50 values of 10nM order. The retinoidal activities of the thiazolidines are significant, considering that replacement of the carboxylic acid in retinoid structures with bioisosteric functional groups is generally ineffective, as seen in the structure-activity relationships of retinoidal benzoic acids.
Effects of a benzimidazole compound on monooxygenase activities
Ates,Suzen,Buyukbingol
, p. 703 - 706 (2007/10/03)
A retinoid-type benzimidazole compound (benzimidazole-tetranaphthalene, BITN) was synthesized and its effects on hepatic cytochrome P450 (CYP) dependent ethoxyresorufin O-deethylase (EROD) and pentoxyresorufin O- depentylase (PROD) enzyme activities were determined in rats in vitro. In vitro addition of BITN in 10-3 M concentration to the reaction medium caused inhibitions in EROD (94%) and PROD (82%) activities. With the same concentration (10-3 M) all-trans-retinoic acid (RA) was able to inhibit EROD activity 65% and PROD activity 59% whereas buthylated hydroxytoluen (BHT) inhibited EROD and PROD activities 73% and 62%, respectively. The specific inhibitors of EROD activity (caffeine) and PROD activity (SKF 525A) at 10-3 M concentration inhibited the corresponding enzymes 33% and 77%, respectively. Thus, these results reveal that the BITN has stronger inhibitory effect than RA, BHT, caffeine and SKF 525 A on the enzyme activities. Since these enzymes (EROD, CYP 1A1/2 and PROD, CYP2B1) activate polycyclic hydrocarbons, aromatic amines and aliphatic halogenated hydrocarbons to their ultimate mutagenic or carcinogenic forms, and are effective in producing reactive oxygen species such as superoxide, hydroxyl radical and hydrogen peroxide, the new compound, BITN, appears to have a greater anticarcinogenic and antioxidant potential than RA and BHT.
Synthesis of nitrone analogues of RAR α selective retinoid Am 580
Yu,Ostrowski,Chen,Reczek,Mansuri,Starrett Jr.
, p. 2819 - 2827 (2007/10/02)
Synthesis of nitrone analogues of RAR α-selective retinoid Am 580 in which the amide linker is replaced with a nitrone moiety is described. The nitrone segment was constructed by oxidizing the corresponding amine using MCPBA or dimethyldioxirane. The resu
