60639-20-5Relevant academic research and scientific papers
Preparation method of halogenated benzothiazepine oxide, product prepared by preparation method and application of product
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, (2020/09/09)
The invention discloses a preparation method of halogenated benzothiazepine oxide as well as a product prepared by the preparation method and application of the halogenated benzothiazepine oxide, andrelates to the technical field of chemical synthesis. Th
Synthesis and anticancer activities of thiosemicarbazones derivatives of thiochromanones and related scaffolds
Li, Guobi,Li, Jincheng,Liu, Shenggui,Pan, Rongkai,Song, Jiangli,Song, Xiumei,Su, Wenyi
, (2020/02/13)
A series of novel thiosemicarbazone analogs (4a–t, 6a–j) were synthesized and evaluated for their cytotoxic activities. The obtained results showed that thiochromanone-based thiosemicarbazones substituted primarily at the C-8 position exhibited higher cytotoxicity than the corresponding 1,1-dioxo-thiochromanone-, benzothiazepine-, and 1,1-dioxo-benzothiazepine-based analogs. Significantly, compound 4c (8-fluoro thiochromanone thiosemicarbazone) was found to be the most active and exhibited potent cytotoxicity against the MCF-7, SK-mel-2, and DU145 cancer cell lines, with IC50 values of 0.42, 0.58, and 0.43 μM, respectively. In addition, the mechanism of compound 4c induced MCF-7 cell apoptosis was preliminarily investigated through cell cycle, Annexin V-FITC/PI staining, and ROS assays, indicating that compound 4c may exert its anticancer property through ROS-mediated apoptosis.
Synthesis of Novel Pterocarpen Analogues via [3?+?2] Coupling-Elimination Cascade of α,α-Dicyanoolefins with Quinone Monoimines
Chen, Hui,Zhao, Sihan,Cheng, Shaobing,Dai, Xingjie,Xu, Xiaoying,Yuan, Weicheng,Zhang, Xiaomei
, p. 1672 - 1683 (2019/04/08)
By employing triethylamine as a catalyst, [3?+?2] coupling-elimination cascade of α,α-dicyanoolefins with quinone monoimines was realized. The reactions afforded various novel pterocarpen analogues with generally moderate yields (up to 75%). In addition, a plausible reaction mechanism was proposed.
Thiochroman-4-one thiosemicarbazide compound as well as preparation method and application thereof
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, (2018/11/22)
The invention relates to a thiochroman-4-one thiosemicarbazide compound, as well as a preparation method and an application thereof. The structural formula of the thiochroman-4-one thiosemicarbazide compound is shown as Formula (I), wherein n is 1 or 2, R
Ionic liquid catalyzed synthesis of 2-(indole-3-yl)-thiochroman-4-ones and their novel antifungal activities
Song, Ya-Li,Wu, Fan,Zhang, Chao-Chao,Liang, Guo-Chao,Zhou, Guan,Yu, Jiao-Jiao
, p. 259 - 261 (2015/04/13)
2-(Indole-3-yl)-thiochroman-4-ones were synthesized via ionic liquid and tested for in vitro antifungal activity. The contribution of ionic liquid to Michael addition reaction is significant. Structures of all compounds are elucidated by 1H NMR, 13C NMR and HRMS. Most of these compounds showed better antifungal activity than fluconazole. The results suggest that 2-(indole-3-yl)-thiochroman-4-ones would be efficient antifungal agents.
Facile one-pot synthesis of some novel thiazolylpyrazole derivatives with antifungal activity
Song, Ya-Li,Yang, Tao,Dong, Yun-Fang,Wu, Fan,Yang, Geng-Liang
, p. 134 - 136 (2014/01/23)
A series of novel 1-(4-phenylthiazol-2-yl)-1,4-dihydrothiochroman[ 4,3-c]pyrazole have been prepared by a three-component reaction of thiochromanone-3-carbaldehyde, phenacyl bromide, and thiosemicarbazide. The reaction was in one-pot and did not require any additional catalyst with moderate yields. This method provided several advantages such as environment friendliness and simple work-up procedure. The compounds were assayed for antifungal activity and some of the new compounds can be further utilized as lead compounds.
Synthesis and antifungal activity of some novel (E)-2, 3-dihydro-3- [(phenylamino) methylene]-4H-1-benzothiopyran-4-ones
Liu, Xiao-Ming,Yang, Geng-Liang,Song, Ya-Li,Liu, Jie-Jie,Yang, Wang,Zhang, Dong-Nuan
, p. 228 - 234 (2013/07/26)
A series of novel (E)-2,3-dihydro-3-[(phenylamino)methylene]-4H-1- benzothiopyran-4-ones has been synthesized by using 2,3-dihydro-4H-1- benzothiopyran-4-ones as the starting material. The structures of the new compounds are characterized by UV-vis, IR, HRMS, 1H NMR, and 13C NMR. 2D NMR spectroscopic studies revealed that at room temperature, these compounds rather exist in the keto-enamine than in the Schiff base form. The synthesized compounds were evaluated against two species of fungi in vitro by agar double dilution method. The results of antifungal screening revealed that the MIC value of (E)-8-chloro-2,3-dihydro-3-[(4- nitrophenylamino)methylene]-4H-1-benzothiopyran-4-one (4j) against Candida albicans is 32 μg·ml-1 while the control Fluconazole is 64 μg?ml-1.
Synthesis and pharmacological evaluation of novel bisindolylalkanes analogues
Song, Ya-Li,Dong, Yun-Fang,Yang, Tao,Zhang, Chao-Chao,Su, Li-Min,Huang, Xin,Zhang, Dong-Nuan,Yang, Geng-Liang,Liu, Yu-Xin
, p. 7624 - 7627 (2014/01/06)
In an effort to develop potent anti-cancer chemopreventive agents that act on topoisomerase II, a novel series of bisindolylalkanes analogues such as 3,3′-(thiochroman-4,4-diyl)bis(1H-indole) are synthesized. Structures of all compounds are elucidated by 1H NMR, 13C NMR and HRMS. Anti-proliferative activities for all of these compounds are investigated by the method of MTT assay on 7 human cancer lines. Most of them showed antitumor activities in vitro, the half maximal inhibitory concentration (IC50) value is 7.798 μg/mL of 3a against MCF7. Compound 3a showed comparable topoisomerase II inhibitory activity to etoposide (VP-16) at 100 μM concentration. The rest of the compounds also showed varying degree topoisomerase II inhibitory activity.
Copper-free asymmetric allylic alkylation of trisubstituted cyclic allyl bromides using grignard reagents
Grassi, David,Alexakis, Alexandre
, p. 13642 - 13646 (2014/01/06)
AAA: The asymmetric allylic alkylation (AAA) of trisubstituted cyclic allyl bromides with Grignard reagents is catalytic (2 mol % of ligand) and regioselective (SN2'/SN2=91:9→100:0). The quaternary carbon centers are formed with good to high enantioselectivity (e.r.=81.5:19.5→96:4). Copyright
Design and synthesis of α,β-epoxyketones as new anticancer agents
Ma, Zhengyue,Zhang, Xinghua,Wang, Shikui,He, Yang,Yang, Gengliang,Li, Beilei,Yang, Junjie,Lu, Yuejuan,Sun, Jiewei
, p. 757 - 764 (2011/11/12)
As epoxy functional group has high anticancer activity, α,β-epoxyketones were designed and synthesized as new anticancer agents, and their structures were confirmed by UV, 1H NMR, IR, MS technigeces and elemental analysis. Their in vitro anticancer activities were evaluated by MTT method and the results showed that the compound 4c exhibited good activity with IC50 of 17.8, 22.0 and 24.1 μg/mL against A-549, Hela and HepG2 cells, respectively. The dose of LD50 of the mice by intragastric administration was 1864.4 mg/kg. Therefore, the α,β-epoxyketones could potentially provide as new anticancer agents. A series of α,β-epoxyketones were synthesized in a four steps reaction and tested for their anticancer activities.
