361541-87-9Relevant academic research and scientific papers
Discovery of β-carboline-(phenylsulfonyl)furoxan hybrids as potential anti-breast cancer agents
Hu, Xu,Gao, Xiang,Gao, Gang,Wang, Yanbing,Cao, Hao,Li, Dahong,Hua, Huiming
, (2021/04/02)
The cytotoxicity properties of the β-carboline alkaloids have been broadly investigated. However, the potential application of β-carbolines was hindered due to the moderate activity in cancer. In the present study, thirty β-carboline-(phenylsulfonyl)furoxan hybrids (11a–j, 12a–j and 13a–j) were designed and synthesized through esterification and amidation reaction strategy, and their inhibitory activities against the human breast cancer cell lines MCF-7 and MDA-MB-231 were evaluated by CCK-8 assay. Biological evaluation presented that the most promising amide derivative 13h, substituted with p-methoxyphenyl group at position 1, generated high concentration of NO and evidently depressed the MCF-7 (IC50 = 0.89 μM) and MDA-MB-231 (IC50 = 0.62 μM) cells proliferation. Particularly, the wound healing and transwell assays demonstrated that 13h significantly inhibited the migration and invasion of MDA-MB-231cells. Furthermore, the preliminary mechanisms studies indicated that 13h induced G2/M phase arrest and apoptosis possibly causing by ROS accumulation and ROS-mediated DNA damage. Based on these considerations, 13h may be a promising antimetastatic agent for breast cancer, which is noteworthy for further exploration.
Compound based on zaltoprofen parent structure and anti-inflammatory application of compound
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Paragraph 0030; 0033; 0038-0041, (2021/08/06)
The invention discloses a novel compound formed by splicing zaltoprofen or a derivative thereof and a compound with a structure as shown in a formula (1) or a formula (2). The compound has anti-inflammatory activity aiming at dual targets of COX-2 and PPAR-gamma, the water content of lung tissue can be reduced, inflammatory response caused by acute lung injury can be relieved, the expression levels of COX-2 and PPAR-gamma in the lung tissue are detected in an immunohistochemical mode, and results show that the compound can remarkably reduce LPS-induced COX-2 level high expression and can remarkably improve LPS-induced PPAR-gamma low expression, and therefore, the compound can be used for preparing anti-inflammatory drugs.
Evaluation of novel paclitaxel-loaded NO-donating polymeric micelles for an improved therapy for gastroenteric tumor
Fang, Yuanying,Jin, Yi,Li, Huilan,Li, Xiang,Liu, Ronghua,Tu, Liangxing,Xu, Guoliang,Yang, Zunhua
, p. 13763 - 13774 (2021/08/16)
This study reports the design and synthesis of NO-donating polymer to generate biodegradable polymeric micelle containing paclitaxel (NO/PTX) as a nanomedicine delivery system aimed to enhance the solubility and anti-cancer activity of paclitaxel (PTX). NO/PTX showed greater NO-releasing performance than nitroglycerin, displaying excellent tolerance in KM mice, and exhibited a two-fold stronger antiproliferative activity than PTXin vitroagainst HCT116, SW480, and SGC-7901 cell lines.In vivotumor growth inhibition assay results indicated that NO/PTX displayed lightly stronger activities against tumor growth than PTX at a dose of 10 mg kg?1, while the anti-tumor effect of NO/PTX was significantly improved than that of PTX and Genexol-PM groups at a dose of 15 mg kg?1(the inhibition rate: 67%vs.53% and 41%). In addition, NO/PTX showed an improved area under the plasma concentration-time curve and drug deposition in tumors in comparison to PTX. Wound healing assay and western blot analysis of EMT-related markers suggested that NO/PTX could inhibit the potential of HCT116 migration. Western blot analysis also demonstrated that NO/PTX dampened efflux activity of P-gp and up-regulated apoptosis-related proteins. Overall, these promising results suggested that the synergism between PTX and NO-donating micelles could contribute to the potent anti-cancer activity of NO/PTX.
Novel nitric oxide-releasing derivatives of triptolide as antitumor and anti-inflammatory agents: Design, synthesis, biological evaluation, and nitric oxide release studies
Zang, Yingda,Lai, Fangfang,Fu, Junmin,Li, Chuangjun,Ma, Jie,Chen, Chengjuan,Liu, Ke,Zhang, Tiantai,Chen, Xiaoguang,Zhang, Dongming
, (2020/02/04)
A series of novel triptolide/furoxans hybrids were designed and synthesized as analogues of triptolide, which is a naturally derived compound isolated from the thunder god vine (Tripterygium wilfordii Hook. F). Some of these synthesized compounds exhibite
A class of chelidonine nitric oxide donor derivatives, preparation method and applications
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Paragraph 0020-0022, (2020/05/01)
The invention relates to the field of natural medicines and medicinal chemistry, and relates to a chelidonine nitric oxide donor derivative, a preparation method and applications, particularly to a preparation method of a series of chelidonine nitric oxide donor derivatives with antitumor activity, and new applications of the chelidonine nitric oxide donor derivatives in preparation of antitumor drugs. The chelerythrine nitric oxide donor derivative and the pharmaceutically acceptable salt thereof disclosed by the invention are represented by a general formula, wherein n1, n2, n3 and X are defined in the claims and the specification.
Chelidonine furazan nitric oxide donor derivatives as well as preparation method and application thereof
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Paragraph 0020-0022, (2020/05/08)
The invention relates to the field of natural medicines and medicinal chemistry, and relates to chelidonine furazan nitric oxide donor derivatives as well as a preparation method and application thereof. The invention particularly relates to a preparation method of the series of chelidonine furazan nitric oxide donor derivatives with antitumor activity and new application of the chelidonine furazan nitric oxide donor derivatives in preparation of antitumor drugs. The chelidonine furazan nitric oxide donor derivatives and the pharmaceutically acceptable salt of the chelidonine furazan nitric oxide donor derivatives are shown as a general formula I in the specification, wherein m, n and X are as described in the claims and the specification.
[...] derivative and its inflammation and immune dysfunction disease in the use of the
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Paragraph 0089; 0093; 0094; 0095, (2019/01/22)
The present invention discloses uses of a class of brusatol derivatives and uses of the brusatol derivatives in inflammations and immune function disorder diseases, particularly to a class of nitric oxide donor brusatol derivatives or medically acceptable salts thereof, a pharmaceutical composition containing the derivative, and applications of the derivatives or the salts thereof in preparation of anti-inflammatory and immunosuppressive drugs. In addition, the applications of the derivatives are provided in preparation of drugs for inflammations and/or immune disorder related diseases. The formula I is defined in the instruction.
Design, synthesis and apoptosis-related antiproliferative activities of chelidonine derivatives
Cheng, Keguang,Gao, Xiang,Hu, Xu,Hua, Huiming,Huang, Xueyan,Li, Dahong,Li, Haonan,Li, Zhanlin,Liu, Lilin,Xu, Fanxing
, (2020/01/03)
To get chelidonine derivatives with enhanced antiproliferative activity and selectivity, a series of nitric oxide donating derivatives (10a-f and 11a-j) were designed, synthesized and biologically evaluated. Compared with chelidonine, these compounds exhibited lower IC50 values against human hepatoma cells HepG2, breast cancer cells MCF-7, colon cancer cells HCT-116, as well as leukemia cells K562. Compound 11j displayed the strongest antiproliferative activity with IC50 values of 3.91, 6.90, 4.36 and 1.12 μM against the above four cells, respectively. Nevertheless, it showed an IC50 value >40 μM against human peripheral blood mononuclear cells (PBMCs), which demonstrated high selectivity between normal and cancer blood cells. In further mechanism studies, 11j showed the capability to induce K562 cells apoptosis, S phase cell cycle arrest and mitochondrial membrane potential disorder. Besides, 11j was found to be effective in promoting the expression of proapoptotic protein Bad and suppressing the expression of anti-apoptotic proteins Bcl-xL, catalase, survivin, claspin and clusterin.
Design and synthesis of novel senkyunolide analogues as neuroprotective agents
Fang, Yuanying,Wang, Rikang,Wang, Qi,Sun, Yongbing,Xie, Saisai,Yang, Zunhua,Li, Min,Jin, Yi,Yang, Shilin
, p. 668 - 672 (2018/01/27)
A class of senkyunolide analogues bearing benzofuranone fragment were designed, synthesized and evaluated for their neuroprotective effect in models of oxygen glucose deprivation (OGD) and oxidative stress. All tested compounds showed neuroprotection profile based on the cell viability assay. In particular, derivatives 1f–1i possessing furoxan-based nitric oxide releasing functionality exhibited significant biological activities in OGD models. More importantly, compound 1g containing short linker with furoxan displayed the most potent neuroprotection at the concentration of 100 μM (cell survival up to 145.2%). Besides, 1g also showed the middle level neuroprotective effect in model of oxidative stress.
Design, synthesis and biological evaluation of novel furoxan-based coumarin derivatives as antitumor agents
Zhang, Zhuo,Bai, Zhi-Wei,Ling, Yong,He, Li-Qin,Huang, Peng,Gu, Hong-Xia,Hu, Rong-Feng
, p. 1198 - 1205 (2018/03/26)
In order to find new anticancer drugs, a series of novel furoxan-based coumarin derivatives (10a–k) were synthesized and evaluated for their antiproliferative activities in vitro. All compounds displayed more potent inhibition on human cervical cancer HeLa cell proliferation than coumarin-3-carboxylic acid, and compounds 10b, 10c, 10f, 10h, and 10i with IC50 values ranging from 0.88 to 5.95 μM were even stronger than doxorubicin (IC50 = 10.21 μM). The further study showed that compound 10i exerted the highest antiproliferative activity (IC50 = 0.60 μM) against human breast cancer MCF-7 cells, and compound 10f had broader spectrum antiproliferative activity against five cancer cells with IC50 values in the low micromolar range of 1.86–9.85 μM. More interestingly, compound 10f had little effect on normal intestinal epithelial CCD841 cells. Our findings suggest that these novel furoxan-based coumarin derivatives may provide a new framework for the discovery of novel antitumor agents for the intervention of human carcinoma cells.
