15317-58-5Relevant articles and documents
Microwave irradiation synthesis of novel indole triazole Schiff base fluorescent probe for Al3+ ion
Shi, Zhichuan,Zhao, Zhigang
, (2019)
An efficient triazole Schiff base fluorescent Al3+-probe 4-((2-hydroxybenzylidene) amino)-5-(1H-indol-3-yl)-4H-1,2,4-triazole-3-thiol (H2L) was designed and synthesized under microwave irradiation. The structure of fluorescent probe H2L was characterized by spectral data and elemental analysis. The probe H2L displays excellent chemo-selectivity towards Al3+ over other metal ions, which can directly inspect with the naked eye under UV lamp. The limit of detection of the probe H2L for Al3+ could reach 29.9 nM. The binding stoichiometry between H2L and Al3+ was determined from the Job's plot to be 1:1, the association constant (Ka) of 9.31 × 104 M?1, and further verified with fluorescence titration, ESI-MS and 1H NMR study.
Development of 2-oindolin-3-ylidene-indole-3-carbohydrazide derivatives as novel apoptotic and anti-proliferative agents towards colorectal cancer cells
Abdel-Aziz, Hatem A.,Abdulla, maha,Abo-Ashour, mahmoud f.,Ahmad, Rehan,Al-Khayal, Khayal,Al-Rashood, Sara T.,Al-Warhi, Tarfah,Alharbi, Amal,Ayyad, Rezk R.,El-Haggar, Radwan,Eldehna, Wagdy m.
, p. 319 - 328 (2021)
Mitochondrial anti-apoptotic Bcl2 and BclxL proteins, are overexpressed in multiple tumour types, and has been involved in the progression and survival of malignant cells. Therefore, inhibition of such proteins has become a validated and attractive target for anticancer drug discovery. In this manner, the present studies developed a series of novel isatin–indole conjugates (7a-j and 9a-e) as potential anticancer Bcl2 and BclxL inhibitors. The progression of the two examined colorectal cancer cell lines was significantly inhibited by all of the prepared compounds with IC50 ranges132–611 nM compared to IC50 = 4.6 μM for 5FU, against HT-29 and IC50 ranges 37–468 nM compared to IC50 = 1.5 μM for 5FU, against SW-620. Thereafter, compounds 7c and 7g were selected for further investigations. Interestingly, both compounds exhibited selective cytotoxicity against both cell lines with high safety to normal fibroblast (HFF-1). In addition, both compounds 7c and 7g induced apoptosis and inhibited Bcl2 and BclxL expression in a dose-dependent manner. Collectively, the high potency and selective cytotoxicity suggested that conjugates 7c and 7g could be a starting point for further optimisation to develop novel pro-apoptotic and antitumor agents towards colon cancer.
Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites
Ju, Zhiran,Su, Mingzhi,Hong, Jongki,La Kim, Eun,Moon, Hyung Ryong,Chung, Hae Young,Kim, Suhkmann,Jung, Jee H.
, p. 86 - 98 (2019)
The aim of this study was to design and synthesize COX-1/COX-2 balanced inhibitors incorporating the structural motifs of anti-inflammatory ascidian metabolites. We designed a series of substituted indole analogs that incorporate the key structures of the ascidian metabolites, herdmanines C and D. The synthesized analogs were tested for their inhibitory activity against COX-1 and COX-2, and compound 5m, which displayed balanced inhibition, was further evaluated for in vitro anti-inflammatory activity. Compound 5m suppressed the expression of pro-inflammatory factors, including iNOS, COX-2, TNF-α, and IL-6 in LPS-stimulated murine RAW264.7 macrophages. The reduction of PGE2, NO, and ROS was also observed, together with the suppression of NF-κB, IKK, and IκBα phosphorylation. Our results characterized 5m as a COX-1/COX-2 balanced inhibitor that subsequently caused ROS inhibition and NF-κB suppression, and culminated in the suppression of iNOS, COX-2, TNF-α, and IL-6 expression.
NOVEL INDOLE DERIVATIVES AND COMPOSITION FOR PREVENTING OR TREATING INFLAMMATORY DISEASES COMPRISING THE SAME
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Paragraph 0124; 0125; 0133; 0134, (2021/02/16)
The present invention relates to a novel indole derivative and a composition for preventing or treating inflammatory diseases comprising the same. More specifically, since a series of substituted indole derivative compounds combining a core structure of an anti-inflammatory seaweed metabolite are designed and synthesized, and inhibitory activity and anti-inflammatory activity on COX-1 and COX-2 in the compound are confirmed, the compound can be used as an effective pharmaceutical composition or health functional food composition for preventing, alleviating or treating inflammatory diseases.
Design, Synthesis, and Pharmacological Evaluation of First-in-Class Multitarget N-Acylhydrazone Derivatives as Selective HDAC6/8 and PI3Kα Inhibitors
Alves, Marina A.,Chaves, Lorrane S.,Fernandes, Patrícia D.,Fraga, Carlos A. M.,Guerra, Fabiana S.,Rodrigues, Daniel A.,Sagrillo, Fernanda S.,Sant'Anna, Carlos M. R.,Thota, Sreekanth,de Sena M. Pinheiro, Pedro
supporting information, (2020/02/25)
Targeting histone deacetylases (HDACs) and phosphatidylinositol 3-kinases (PI3Ks) is a very promising approach for cancer treatment. This manuscript describes the design, synthesis, in vitro pharmacological profile, and molecular modeling of a novel class of N-acylhydrazone (NAH) derivatives that act as HDAC6/8 and PI3Kα dual inhibitors. The surprising selectivity for PI3Kα may be related to differences in the conformation in the active site. Cellular studies showed that these compounds act in HDAC6 inhibition and the PI3/K/AKT/mTOR pathway. The compounds that are selective for inhibition of HDAC6/8 and inhibit PI3Kα show potential for the treatment of cancer.
