- Design, synthesis, and anti-proliferative evaluation of 1: H -1,2,3-triazole grafted tetrahydro-β-carboline-chalcone/ferrocenylchalcone conjugates in estrogen responsive and triple negative breast cancer cells
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A series of 1H-1,2,3 triazole grafted tetrahydro-β-carboline-chalcone/ferrocenylchalcone conjugates were synthesized and in vitro evaluated against estrogen responsive (MCF-7) and triple negative (MDA-MB-231) breast cancer cells. Comparative analysis reve
- Awolade, Paul,Cele, Nosipho,Gu, Liang,Kaur, Mandeep,Kumar, Vipan,Pillay, Ruvesh Pascal,Sharma, Bharvi,Singh, Parvesh
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p. 11137 - 11147
(2020/07/15)
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- Beta-carbolines V-type phosphodiesterase inhibitor and preparation method and usage thereof
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The invention provides a Beta-carbolines V-type phosphodiesterase inhibitor and a preparation method and a usage thereof. The Beta-carbolines V-type phosphodiesterase inhibitor has a structure as shown in a formula (X): the formula is as shown in the desc
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Paragraph 0192; 0194; 0197; 0198
(2019/01/23)
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- Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect
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Based on our previous studies and predictive docking results, furans and thiophenes were introduced to the privileged tetrahydro-β-carboline scaffold to generate more potent and selective PDE5 inhibitors. A total of 66 novel furyl/thienyl tetrahydro-β-carboline derivatives were designed, synthesized and evaluated for PDE5 inhibition. Tetrahydro-β-carboline-piperazinedione 19f and tetrahydro-β-carboline-hydantoin 26b with optimized pendant 5-ethylfuran/5-ethylthiophene were identified as the most potent PDE5 inhibitors, and showed high selectivity towards PDE5 versus other PDE isozymes, especially PDE6 and PDE11. Further vasorelaxant activity assessments revealed that these PDE5 inhibitors also exhibited significant angiectasis on the norepinephrine-precontracted 3rd-order mesenteric arteries (110–150 μm) via NO–sGC–cGMP pathway, implying their further application for the treatment of vascular diseases.
- Zheng, Hongbo,Wu, Yifeng,Sun, Bin,Cheng, Chuanle,Qiao, Yanan,Jiang, Yuehua,Zhao, Shengtian,Xie, Zhiyu,Tan, Jing,Lou, Hongxiang
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p. 767 - 780
(2018/09/25)
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- Histone demethylating agents as potential S-adenosyl-l-methionine-competitors
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Histone H3 methylation on K9 and/or K27 depends on histone lysine methyltransferases (KMTs). EZH2, one of the components of the PRC2 complex, catalyzes the trimethylation of histone H3K27, which is associated with transcriptional repression and tumor development. H3K9me3 mediated gene silencing may result from other KDMs such as G9a/GLP, SUV39H1-2, SETDB1, CCLD8 and RIZ1. Their disturbance leads to defective cell mitosis. It is therefore desirable to find small molecules that are able to decrease H3K9 and K27 tagging to reinitiate gene transcription. Most KDM inhibitors are still based on SAM co-factor competition/modulation. Herein, functional screening of a diversity library proved to be a useful tool for finding new specific KDM inhibitors; the use of SAM-based pharmacophoric models facilitated the understanding of their possible mechanism of action.
- Navakauskiene,Mori,Christodoulou,Zentelyte,Botta,Via, L. Dalla,Ricci,Damia,Passarella,Zilio,Martinet
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p. 1245 - 1255
(2016/07/06)
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- (R/S)-BINOL-α-phosphoryloxy enecarbamate-mediated and (R/S)-Titanium(IV) BINOLates-catalyzed enantioselective intramolecular heck/aza-diels-alder cycloaddition (IHADA): An expedient methodology
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An (R/S)-titanium(IV) BINOLate-catalyzed highly enantioselective intramolecular Heck/aza-Diels-Alder cycloaddition (IHADA) cascade was developed to prepare tetrahydropyridoindoles (tHPs) and octahydropyrazinopyridoindoles (oHPPs) from in situ generated (R/S)-BINOL α-phosphoryloxy carbamate (αPPC2) in one pot. Chiral cooperativity between (R/S)-αPPC2 and (R/S)-titanium(IV) BINOLate was observed and successfully utilized for the construction of various tHPs (7 examples) and oHPPs (17 examples). Copyright
- Khan, Imran A.,Saxena, Anil K.
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p. 2617 - 2626
(2013/10/21)
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- Some 3-carboxamides of β-carboline and tetrahydro-β-carboline
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A series of tetrahydro-β-carboline-3-carboxamides (L- and D-series) was made by the interaction of the respective amine with the appriopriate methyl tetrahydro-β-carboline-3-carboxylate.The β-carboline-3-carboxamides were prepared by a similar route from methyl β-carboline-3-carboxylate or by aromatization of the respective tetrahydro-β-carboline-3-carboxamide.The diastereomers of N-sec-butyl tetrahydro-β-carboline-3-carboxamide (L- and D-series) were separated by chromatography.
- Couts, Ronald T.,Micetich, Ronald G.,Baker, Glen B,Benderly, Abraham,Dewhurst, Tim,et al.
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p. 131 - 142
(2007/10/02)
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