- Design, synthesis and biological evaluation of benz-fused five-membered heterocyclic compounds as tubulin polymerization inhibitors with anticancer activities
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A series of benz-fused five-membered heterocyclic compounds were designed and synthesized as novel tubulin inhibitors targeting the colchicine binding site. Among them, compound 4d displayed the highest antiproliferative activity against four cancer cell lines with an IC50 value of 4.9?μM in B16-F10 cells. Compound 4d effectively inhibited tubulin polymerization in vitro (IC50 of 13.1?μM). Further, 4d induced cell cycle arrest in G2/M phase. Finally, 4d inhibited the migration of cancer cells in a dose-dependent manner. In summary, these results suggest that compound 4d represents a new class of tubulin inhibitors deserving further investigation.
- Komuraiah, Buduma,Ren, Yichang,Xue, Mingming,Cheng, Binbin,Liu, Jin,Liu, Yao,Chen, Jianjun
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p. 1109 - 1116
(2021/03/16)
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- Catalytic enantioselective one-pot approach to cis- and trans-2,3-diaryl substituted 1,5-benzothiazepines
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The first enantioselective catalytic approach to cis- and trans-2,3-diaryl substituted 1,5-benzothiazepines has been conveniently developed in a one-pot fashion, starting from α,β-unsaturated acyl pyrazoles and 2-aminothiophenol. The organocatalytic two-s
- Meninno, Sara,Quaratesi, Ilaria,Volpe, Chiara,Mazzanti, Andrea,Lattanzi, Alessandra
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supporting information
p. 6923 - 6934
(2018/10/17)
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- Catalytic Enantioselective Synthesis of Protecting-Group-Free 1,5-Benzothiazepines
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A one-pot enantioselective route to N-unprotected 2,3-dihydro-1,5-benzothiazepinones, by an organocatalyzed sulfa-Michael reaction of readily available α,β-unsaturated N-acyl pyrazoles with 2-aminothiophenols followed by silica-gel-catalyzed lactamization
- Meninno, Sara,Volpe, Chiara,Lattanzi, Alessandra
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supporting information
p. 4547 - 4550
(2017/04/13)
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- Indoline dyes with benzothiazole unit for dye-sensitized solar cells
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We report a new series of indoline dyes with a donoraromatic-acceptor (D-π-A) structure. D-π-A metal-free organic dyes with indoline-benzothiazole-rhodanine units were synthesized and their photovoltaic performances were evaluated. The photoelectric conversion efficiency (η) of the indoline-benzothiazole-rhodanine dye is 3.7%, while that of the indolinethiophene-rhodanine dye is 0.9% under the same conditions. The incident photon-to-current conversion efficiencies (IPCEs) of these dyes are 60% and 25%, respectively, at 500 nm. To understand their electronic structures, the geometries of the dyes were optimized by density functional theory (DFT) calculations at the 6-31G(d) level using a B3LYP exchange-correlation functional. As a result, the localized highest occupied molecular orbital (HOMO) and the lowest unoccupied molecular orbital (LUMO) of the indoline?benzothiazole?rhodanine dye were obtained and were compared with those of the indoline-thiophene-rhodanine dye.
- Horiuchi, Tamotsu,Yashiro, Tohru,Kawamura, Ryo,Uchida, Satoshi,Segawa, Hiroshi
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supporting information
p. 517 - 519
(2016/06/09)
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- COMPOUNDS FOR THE MODULATION OF MYC ACTIVITY
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The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angio genesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.
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Paragraph 395; 396-397; 565; 566-567; 935-936; 950-951; 1010
(2017/01/31)
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- INHIBITORS OF HIF PROLYL HYDROXYLASE
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The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
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Page/Page column 187
(2016/04/20)
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- Facile net cycloaddition approach to optically active 1,5-benzothiazepines
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The 1,5-benzothiazepine moiety is well-known as a versatile pharmacophore, and its derivatives are expected to have antagonism against numerous diseases. Thus, it is desirable to develop a synthetic route that enables facile enantioselective preparation of a wide range of such derivatives. Although the cycloaddition approach could be considered a possible route to these compounds, to date, there has been no precedent of such a protocol. We therefore present the first example of a highly enantioselective net [4 + 3] cycloaddition to afford 1,5-benzothiazepines by utilizing α,β-unsaturated acylammonium intermediates generated by chiral isothiourea catalysts, which undergo two sequential chemoselective nucleophilic attacks by 2-aminothiophenols. This protocol provided cycloadducts in extremely high regioselectivity, with a good-to-excellent stereoselectivity being achieved regardless of the steric and electronic properties of the substrates. This method therefore offers promising synthetic routes for the construction of a library of optically active 1,5-benzothiazepines for assay evaluation.
- Fukata, Yukihiro,Asano, Keisuke,Matsubara, Seijiro
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supporting information
p. 5320 - 5323
(2015/05/13)
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- COMPOUNDS FOR TREATMENT OF DRUG RESISTANT AND PERSISTENT TUBERCULOSIS
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Described herein are compounds and compositions for treating drug resistant and persistent tuberculosis. Also described herein is a method of screening for identifiying biofilm formation inhibitors.
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- Fused bicyclic-substituted amines as histamine-3 receptor ligands
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Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.
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- Fused bicyclic-substituted amines as histamine-3 receptor ligands
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Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.
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