25888-01-1Relevant academic research and scientific papers
Synthesis and biological evaluation of indole-3-carboxamide derivatives as antioxidant agents
Huang, Erfang,Zhang, Lan,Xiao, Chuying,Meng, Guangpeng,Zhang, Bingqi,Hu, Jianshu,Wan, David Chi-Cheong,Meng, Qingguo,Jin, Zhe,Hu, Chun
, p. 2157 - 2159 (2019/05/07)
Oxidative stress results in various pathologies and as consequence antioxidant agents have attracted uninterrupted attention. In this paper, a novel series of indole-3-carboxamide derivatives (6a–6l) were designed and synthesized based on the melatonin structure as novel antioxidants. All of them were evaluated for the antioxidant activities in vitro against human neuroblastoma SH-SY5Y cell line using H2O2 radical scavenging assay. The target compounds 6a, 6f and 6i indicated better activities than the positive control, ascorbic acid, and 6a exhibited the best antioxidant activity. In addition, the structure-activity relationships of the target compounds were also preliminarily summarized based on the obtained experimental data.
Benzpyrole-3-formamide compound and application thereof
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Paragraph 0028; 0029, (2019/07/04)
The invention belongs to the technical field of medicine, and relates to a benzpyrole-3-formamide compound and application thereof. The structural formula of the benzpyrole-3-formamide compound is shown in the description, wherein R1, R2, R3 and R are described in the claim and the description. The benzpyrole-3-formamide compound and acid addition salt applicable to the compound in pharmacy can betaken as an antioxidant to prepare medicines used for treating or preventing related diseases caused by oxidative damage of protein, wherein the related diseases caused by oxidative damage of proteinare Alzheimer's disease, Parkinson's disease, diabetes, chronic renal failure and the like.
Design, synthesis and biological evaluation of a novel series of indole-3-carboxamide derivatives for cancer treatment as EGFR inhibitors
Zhang, Lan,Deng, Xin-Shan,Meng, Guang-Peng,Zhang, Chao,Liu, Cong-Chong,Chen, Gu-Zhou,Jiang, Xu-Liang,Zhao, Qing-Chun,Hu, Chun
, p. 70 - 83 (2018/02/15)
Background: As reported EGFR is a sialoglycoprotein with tyrosine kinase activity involved in control of cellular survival, multiplication, differentiation and metastasis. Dysregulation or aberrant expression of EGFR has been implicated in cell transformation and having oncogenic roles in a number of human cancers. Therefore EGFR has become a significant target for developing targeted therapy for cancer. Methods: A novel series of indole-3-carboxamide derivatives as EGFR inhibitors were designed, synthesized and evaluated for the anticancer activity in vitro against three EGFR high-expressed cancer cell lines (A549, HeLa, and SW480), one EGFR low-expressed cell line (HepG2) and one human liver normal cell line (HL7702) by MTT assay. Results: The target compounds 6c, 6f, 6i, 6j, 6l, 6r, 6u and 6x exhibited potent anticancer activities against the three tested cancer cell lines and weak cytotoxic effects on HepG2, which imply that the target compounds are probably effective in inhibiting EGFR. And they also did not show measurable activities in HL7702, which imply the target compounds are likely to overcome the nonspecific toxicity against normal cells. Particularly, the target compound 6x indicated equal to the positive control erlotinib. In addition, molecular docking studies demonstrated the target compound 6x may be the potential inhibitor to EGFR. Conclusion: A new EGFR inhibitor scaffold and a preliminary discussion on their SARs provide promising opportunities to guide further research on indole-3-carboxamide derivatives as novel anticancer agents.
Indole carboxamide compounds and use thereof
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Paragraph 0053-0056, (2017/08/31)
The invention belongs to the technical field of medicine and relates to indole carboxamide compounds and a use thereof. The indole carboxamide compounds comprise derivatives of indole carboxamide and pharmaceutically acceptable salts thereof. The indole carboxamide compounds have a general formula shown in the description. R1, R2 and R3 are defined in the claims and the specification. The indole carboxamide compounds and pharmaceutically acceptable acid salts can be used as epidermal growth factor tyrosine kinase inhibitors for treatment on epidermal growth factor receptor transfer disorder associated diseases such as small cells lung cancer, squamous cell carcinoma, adenocarcinoma, large cell carcinoma, colorectal cancer, breast cancer, ovarian cancer and renal cell carcinoma.
N-H insertion reactions of rhodium carbenoids. Part 3. The development of a modified Bischler indole synthesis and a new protecting-group strategy for indoles
Bashford, Katherine E.,Cooper, Anthony L.,Kane, Peter D.,Moody, Christopher J.,Muthusamy, Sendogagounder,Swanna, Elizabeth
, p. 1672 - 1687 (2007/10/03)
A modified version of the Bischler indole synthesis has been developed in which the key step is the N-H insertion reaction of rhodium carbene intermediates derived from α-diazo-β-ketoesters with anilines. Thus N-methylanilines 1 react with diazoketoesters 2 in the presence of dirhodium(II) acetate to give (N-arylamino)ketones 3, cyclisation of which using boron trifluoride-ethyl acetate or acidic ion exchange resin gives the indoles 4. In order to extend this method to the synthesis of N-unsubstituted indoles, a new protecting group strategy for indoles was developed. In this, anilines are reacted with α,β-unsaturated-esters or -sulfones to give the conjugate addition products 6 and 9, cyclisation of which gives indoles 8 and 11. The N-(2-ethoxycarbonylethyl)- and -(2-sulfonylethyl)- protecting groups are readily removed from indoles 8 and 11 by treatment with base.
