452095-50-0Relevant academic research and scientific papers
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)
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.
Aurovertin B derivative as well as preparation method and application thereof
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Paragraph 0048; 0050, (2020/12/30)
The invention provides an aurovertin B derivative, a preparation method of the aurovertin B derivative, and an application of the aurovertin B derivative in the preparation of a medicine for treatingtriple negative breast cancer. The polarity of the aurov
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
Synthesis and biological study of class I selective HDAC inhibitors with NO releasing activity
Ding, Qin'ge,Liu, Chunxi,Zhao, Chunlong,Dong, Hang,Xu, Qifu,James Chou,Zhang, Yingjie
, (2020/09/07)
Based on the multi-mechanism antitumor strategy and the regulatory effect of nitric oxide (NO) on histone deacetylases (HDACs), a series of N-acyl-o-phenylenediamine-based HDAC inhibitors equipped with the phenylsulfonylfuroxan module as NO donor was desi
Synthesis of cucurbitacin B derivatives as potential anti-hepatocellular carcinoma agents
Ge, Weizhi,Chen, Xinyi,Han, Fangzhi,Liu, Zhongquan,Wang, Tianpeng,Wang, Mengmeng,Chen, Yue,Ding, Yahui,Zhang, Quan
, (2019/01/04)
Cucurbitacin B shows potent activity against tumor cells, but its high toxicity limits its application in the clinic. A series of cucurbitacin B derivatives was synthesized and evaluated for their anti-hepatocellular carcinoma (HCC) activities against the HepG-2 cell line. These compounds were also tested for their toxicity against the L-O2 normal cell line. The compound with the most potential, 10b, exhibited potent activity against the HepG-2 cell line with an IC50 value of 0.63 μM. Moreover, compound 10b showed the highest TI value (4.71), which is a 14.7-fold improvement compared to its parent compound cucurbitacin B. A preliminary molecular mechanism study of 10b indicated that 10b could inhibit P-STAT3 to induce the activation of mitochondrial apoptotic pathways. An in vivo acute toxicity study indicated that the compound 10b has preferable safety and tolerability compared with cucurbitacin B. These findings indicate that compound 10b might be considered as a lead compound for exploring effective anti-HCC drugs.
Design, synthesis, and antitumor evaluation of novel histone deacetylase inhibitors equipped with a phenylsulfonylfuroxan module as a nitric oxide donor
Duan, Wenwen,Li, Jin,Inks, Elizabeth S.,Chou, C. James,Jia, Yuping,Chu, Xiaojing,Li, Xiaoyang,Xu, Wenfang,Zhang, Yingjie
, p. 4325 - 4338 (2015/06/08)
On the basis of the strategy of creating multifunctional drugs, a novel series of phenylsulfonylfuroxan-based hydroxamates with histone deacetylase (HDAC) inhibitory and nitric oxide (NO) donating activities were designed, synthesized, and evaluated. The
Design, synthesis and evaluation of nitric oxide-releasing derivatives of N-(n-butyl)matrinic acid and N-(n-butyl)matrinol as anti-hepatocellular carcinoma agents
Wu, Ya-Xian,Huang, Jun-Kai,Gao, Lei-Lei,He, Li-Qin,Huang, Peng,Wan, Xiao-Shan
, p. 301 - 312 (2015/03/04)
A series of novel furoxan-based derivatives of N-n-butyl matrinic acid (9a-m) and N-n-butyl matrinol (10a-m) were synthesized and their anti-human hepatocellular carcinoma (HCC) activities were evaluated. All derivatives displayed potential inhibition of
Synthesis and biological evaluation of nitric oxide-releasing hybrids from gemcitabine and phenylsulfonyl furoxans as anti-tumor agents
Li, Xianghua,Wang, Xuemin,Xu, Chenjun,Huang, Junkai,Wang, Chengniu,Wang, Xinyang,He, Liqin,Ling, Yong
, p. 1130 - 1136 (2015/06/25)
A series of novel hybrids 10a-m were designed and synthesized by coupling phenylsulfonyl furoxans with gemcitabine through various diols or alcohol amine linkers, and their biological activities were evaluated in vitro. Most of the hybrids exhibited good to moderate anti-tumor activities, which are associated with NO release. In particular, hybrid 10e showed excellent anticancer activities which were more potent than or comparable to gemcitabine. However, inhibition of nucleoside transport only significantly decreased the inhibitory rates of gemcitabine against HepG2 cells but not 10e, and the inhibitory rates of 10e were partially reduced by pre-treatment with hemoglobin, demonstrating that the anti-tumor activity of 10e might result from the synergic effect of high levels of NO production and gemcitabine fragment. In addition, compound 10ecould apparently induce cell apoptosis by regulating apoptotic relative proteins. Therefore, our novel findings provide a proof of principle in the design of new furoxan/gemcitabine hybrids for the intervention of human cancers.
Synthesis and bioactivity of furoxan-based nitric oxide-releasing colchicine derivatives as anticancer agents
Shen, Li Hong,Wang, Sheng Li,Li, Hong Yu,Lai, Yi Sheng,Liu, Li Jie
, p. 3294 - 3296 (2013/04/24)
A series of novel nitric oxide-donating colchicine derivatives (9a-j) were synthesized by coupling furoxan with N-methyl colchiceinamide through an appropriate spacer arm and their cytotoxicity against four human cancer cell lines in vitro were evaluated by MTT method. It was found that many of the derivatives displayed significant activity, particularly, compound 9f showed more potent cytotoxic activities than colchicine.
Novel nitric oxide-releasing derivatives of farnesylthiosalicylic acid: Synthesis and evaluation of antihepatocellular carcinoma activity
Ling, Yong,Ye, Xiaolei,Zhang, Zhenzhen,Zhang, Yihua,Lai, Yisheng,Ji, Hui,Peng, Sixun,Tian, Jide
scheme or table, p. 3251 - 3259 (2011/06/24)
Figure Presented. Novel furoxan-based nitric oxide (NO) releasing derivatives (8a-p) of farnesylthiosalicylic acid (FTS) were synthesized. Compound 8l displayed the strongest inhibition on the proliferation of human hepatocellular carcinoma (HCC) cells in vitro, superior to FTS, sorafenib, and furoxan moiety, selectively induced high frequency of HCC cell apoptosis, and produced high levels of NO in HCC cells but not in nontumor liver cells. Furthermore, 8l exhibited low acute toxicity to mice and significantly inhibited the growth of HCC tumors in vivo and the Ras-related signaling in the tumors. Therefore, our novel findings may provide a new framework for the design of new NO-releasing furoxan/FTS hybrids for the intervention of human HCC.
