- A straightforward expeditious synthesis of 5-nitrobenzo[b]thiophene-2- carbaldehyde
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A high yielding one-pot synthesis of 5-nitrobenzo[b]thiophene-2- carbaldehyde is reported using the readily available,cheap starting material 2,5-dihydroxy-1,4-dithiane and 2-chloro-5-nitrobenzaldehyde.
- Wei, Hongtao,Sun, Min,Ji, Min
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- Synthesis and pharmacological evaluation of 2-substituted benzo[b]thiophenes as anti-inflammatory and analgesic agents
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An efficient method for trapping isocyanate 4, generated from the Curtius rearrangement, with ethyl alcohol to afford the carbamate 5 is reported. 5-Nitrobenzo[b]thiophene-2-carboxylic acid 1 is converted to the corresponding hydrazide 2 by the reaction with hydrazine hydrate and then to the azide 3 with nitrous acid, followed by thermal rearrangement, cooling, and trapping in one pot reaction. The carbamate 5 is treated with hydrazine hydrate to afford the desired, Zileuton analogue, 4-(5-nitrobenzo[b]thiophene-2-yl)semicarbazide 6. Also the reactivity of hydrazide 2 towards some carboxyaldehydes and phenylisothiocyanate afforded the corresponding carbohydrazides 7, 8 and phenylthiosemicarbazide 9, respectively. Compounds 9, 2 and 6, respectively, were more potent as anti-inflammatory and anti-nociceptive agents.
- Fakhr, Issa M.I.,Radwan, Mohamed A.A.,El-Batran, Seham,Abd El-Salam, Omar M.E.,El-Shenawy, Siham M.
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- Design, synthesis, and biological evaluation of novel benzo[b]thiophene-diaryl urea derivatives as potential anticancer agents
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A hybrid pharmacophore approach was applied to design and synthesize a series of benzo[b]thiophene-diaryl urea derivatives 17a–g with potential anticancer effect. In vitro antiproliferative activities of all target compounds were evaluated against HT-29 a
- Zarei, Omid,Azimian, Fereshteh,Hamzeh-Mivehroud, Maryam,Shahbazi Mojarrad, Javid,Hemmati, Salar,Dastmalchi, Siavoush
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p. 1438 - 1448
(2020/05/28)
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- Synthesis and biological evaluation of diaryl urea derivatives designed as potential anticarcinoma agents using de novo structure-based lead optimization approach
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To develop inhibitors blocking VEGFR2 and the Raf/MEK/ERK mitogen-activated protein kinase signaling pathway new compounds based on sorafenib were designed, synthesized and biologically evaluated. Using de novo design method, a library of new ligands was
- Azimian, Fereshteh,Dastmalchi, Siavoush,Hamzeh-Mivehroud, Maryam,Hemmati, Salar,Shahbazi Mojarrad, Javid
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- Design, synthesis, and in vitro antiproliferative activity of novel Dasatinib derivatives
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Two series of novel Dasatinib derivatives have been designed and synthesized, with their in vitro cytostatic effect screened on human chronic myeloid leukemia cell line K562 and human myeloid leukemia cell line U937. Some target compounds demonstrated sig
- Cai, Jin,Zhang, Shaoning,Zheng, Ming,Wu, Xiaoqing,Chen, Junqing,Ji, Min
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scheme or table
p. 806 - 810
(2012/03/26)
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- BENZOTHIOPHENE HYDROXAMIC ACID DERIVATIVES
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The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing t
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Page/Page column 54
(2008/06/13)
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- BENZOTHIOPHENE HYDROXAMIC ACID DERIVATIVES WITH CARBAMATE, UREA, AMIDE AND SULFONAMIDE SUBSTITUTIONS
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The present invention relates to a novel class of hydroxamic acid derivatives carbamate, urea, amide and sulfonamide substitutions. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetyla
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(2008/06/13)
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- BENZOTHIOPHENE DERIVATIVES
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The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.
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Page/Page column 73
(2008/06/13)
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- THIOPHENE AND BENZOTHIOPHENE HYDROXAMIC ACID DERIVATIVES
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The present invention relates to a novel class of hydroxamic acid derivatives having a benzothiophene or thiophene backbone. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit historic deacetylase and
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Page/Page column 94
(2008/06/13)
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- EP2 RECEPTOR AGONISTS
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A compound of Formula (I) or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of Formulae (Ai), (Aii), (Aiii) D is selected from Formulae (Di), (Dii), (Diii), (Div), (Dv) B is selected from the group consisting of Formulae (Bi), (Bii), (Biii), (Biv) (Bv).
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Page/Page column 146
(2008/06/13)
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- Novel benzothienyl or indole derivatives, preparation and use thereof as inhibitors of prenyl transferase proteins
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The invention concerns compounds of general formula (1), wherein, in particular; W represents H, SO2R5. CO(CH2)nR5, (CH2)nR6, CS(CH2)nR5; X represents S or NH; Y represents (CH2)p, CO, (CH2)pCO, CH═CH—CO; Z represents a hetcrocycle, imidazole, benzimidazole, isoxazole, tetrazole, oxadiazole, thiadazole, pyridine, quinazoline, quinoxaline, quinoline, thiophene; R1 represents COOR6, CONR6R7, CO—NH—CH(R6)—COOR7, CH2NR6R7, CH2OR6, (CH2)pR6, CH═CHR6; R2 represents in particular hydrogen, C1-C10 alkyl, a substituted or unsubstituted phenyl; R5 and R6 represents hydrogen, C1—C6 alkyl; R5 represents a substituted or unsubstituted phenyl or naphthyl; R6 and R7, identical or different, represent hydrogen, C1—C15 alkyl, a hetcrocycle. an aryl; n represents 0 to 10; p represents 1 to 6.
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- HISTONE DEACETYLASE INHIBITORS
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The present invention provides histone deacetylase inhibitors of general formula (I), process for the preparation of such compounds and uses of the compounds in medicine.
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- Benzoxazepinones and their use as squalene synthase inhibitors
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There is disclosed a compound represented by the formula [I]: wherein R1 is optionally substituted 1-carboxyethyl group, optionally substituted alkyl-sulfonyl group, optionally substituted (carboxy-cycloalkyl)-alkyl group, -X1-X2-Ar-X3-X4-COOH (wherein X1 and X4 are a bond or alkylene group, X2 and X3 are a bond, -O-, -S-, Ar is divalent aromatic group etc.), R2 is alkyl group optionally substituted with alkanoyloxy group and/or hydroxy group, R3 is alkyl group, and W is halogen atom, etc., or a salt thereof. The compound has the cholesterol lowering activity and the triglyceride lowering activity and is useful for preventing and/or treating hyperlipidemia.
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- Synthesis of new 5-substitutedbenzo[b]thiophene derivatives
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Previous works of our group have dealt with the synthesis of 1-(aryl)-3-[4-(aryl)piperazin-1-yl]propane derivatives in the search for new and efficient antidepressants with a dual mode of action: serotonin reuptake inhibition and 5-HT1A receptor afinity [1-4]. From these studies we concluded that the 3-[4-(aryl)piperazin-1-yl]-l-(benzo[b]thiophen-3-yl)propane derivatives led to the best results. The continuation of this research project required the preparation of some new 3-acyl-5-substituted benzo[b]thiophenes with a wide variety of substituents at the 5 position, ranging from nitro to hydroxyl derivatives. To obtain these derivatives we acylated the corresponding 5-substituted benzo[b]thiophenes when it was possible.
- Perez-Silanes,Martinez-Esparza,Oficialdegui,Villanueva,Orus,Monge
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p. 1025 - 1030
(2007/10/03)
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- Benzothiophene derivatives and corresponding use and composition
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Benzothiophene derivative compounds and corresponding use and composition; the compounds respond to formula (I): where Z is: —CO—, —CH(OR6)—, —C(NOR7)—; R1is: H, C1-C6alkyl, halogen, or —OR8/sub
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- Practical Synthesis of Optically Pure Bifunctionalized Heterohelicenes
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Optically active 2-(hydroxymethyl)- and 2-(ethylthiocarbonyl)[1]benzothieno[5′,4′ :2.3][1]benzothieno [4′.5 :4,5]-thieno[3,2-f]quinolines containing π-excessive thiophene and π-deficient pyridine units were prepared by the use of exo-3-amino-2-hydroxybornane as a chiral auxiliary. This procedure consists of separation of the helical diastereomers prepared by photocyclization of 1,2-diarylethylenes and removal of the chiral auxiliary by a thiolate ion. Large scale preparation of the helicenes can be accomplished by a modified procedure of the photocyclization reaction. Optical purities of both enantiomers of 2-(hydroxymethyl)- and 2-(ethylthiocarbonyl)[1] benzothieno[5′ ,4′ : 2,3][I]benzothieno[4′.5′ : 4,5]-thieno[3,2-f lquinolines were >99.5%. Their absolute configurations were determined by comparison of CD spectra.
- Osuga, Hideji,Suzuki, Hitomi,Tanaka, Kazuhiko
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p. 891 - 897
(2007/10/03)
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