578703-90-9Relevant academic research and scientific papers
Synthesis and Anticancer Activity of (E)-5-[(1-Aryl-1H-1,2,3-triazol-4-yl)methylene]thiazolidine-2,4-diones
Manikala, V. K.,Rao, V. M.
, p. 863 - 868 (2020/07/03)
Abstract: A novel series of 1,2,3-triazolylthiazolidinedione analogs have been synthesized by the condensation of the corresponding 1-aryl-1H-1,2,3-triazole-4-carbaldehydes with thiazolidine-2,4-dione in the presence of KOH. The title compounds were evaluated for their in vitro anticancer activity using MTT assay against four cancer cell lines: A549 (lung), HT-29 (colon), MCF-7 (breast), and A375 (melanoma). Most compounds displayed good anticancer activity, but hydroxy- and nitro-substituted derivatives showed higher activity than the others.
Synthesis and Antimicrobial Activity of (E)-2-[(1-Substituted Phenyl-1H-1,2,3-triazol-4-yl)methylene]-2,3-dihydro-1H-inden-1-ones
Swamy,Swapna,Sandeep,Venkateswar Rao
, p. 1884 - 1886 (2019/11/02)
A series of novel (E)-2-[(1-phenyl-1H-1,2,3-triazol-4-yl)methylene]-2,3-dihydro-1H-inden-1-one derivatives has been synthesized by condensation of 1-phenyl-1H-1,2,3-triazole-4-carbaldehydes with 2,3-dihydro-1H-inden-1-one. The synthesized compounds are ch
Design, synthesis and biological evaluation of new steroidal β-triazoly enones as potent antiproliferative agents
Zhao, Jian-Wei,Guo, Jia-Wen,Huang, Ming-Jie,You, Ya-Zhen,Wu, Zeng-Hui,Liu, Hong-Min,Huang, Li-Hua
supporting information, (2019/07/12)
β-Triazoly enones are biologically interesting scaffolds, incorporation of such scaffolds into the steroid nucleus may generate new bioactive steroids and further enrich structural types of steroids. In this work, a series of new steroidal β-triazoly enon
16-(1'-aryl-1',2',3'-triazole)methylene-androst-17-ketone derivative
-
Paragraph 0035; 0040; 0041, (2019/02/04)
The invention belongs to the technical field of drug chemistry, and relates to a 16-(1'-aryl-1',2',3'-triazole)methylene-androst-17-ketone derivative as well as a preparation method and application thereof. The compound has the following general formula:
Synthesis and biological evaluation of ursolic acid derivatives bearing triazole moieties as potential anti-Toxoplasma gondii agents
Luan, Tian,Jin, Chunmei,Jin, Chun-Mei,Quan, Zhe-Shan,Gong, Guo-Hua
, p. 761 - 772 (2019/03/23)
Ursolic acid (UA), a plant-derived compound, has many properties beneficial to health. In the present study, we synthesised three series of novel UA derivatives and evaluated their anti-Toxoplasma gondii activity both in vitro and in vivo. Most derivative
Design, synthesis, and biological evaluation of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia
Xu, Qiaoling,Dai, Baozhu,Li, Zhiwei,Xu, Le,Yang, Di,Gong, Ping,Hou, Yunlei,Liu, Yajing
, (2019/08/27)
FMS-like tyrosine kinase 3 (FLT3) was an important therapeutic target in acute myeloid leukemia (AML). We synthesized two series of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives possessing the semicarbazide moiety and 2,2,2-trifluoro-N,N′-dimeth
Design and synthesis of novel dehydroepiandrosterone analogues as potent antiproliferative agents
Huang, Xing,Shen, Qing-Kun,Zhang, Hong-Jian,Li, Jia-Li,Tian, Yu-Shun,Quan, Zhe-Shan
, (2018/09/12)
The aim of the present study was to determine the cytotoxic effects of a series of novel dehydroepiandrosterone derivatives containing triazole at the C16 position on human cancer cells. The cancer cells used in the present study were A549, Hel
Revisiting ring-degenerate rearrangements of 1-substituted-4-imino-1,2,3-triazoles
Fletcher, James T.,Hanson, Matthew D.,Christensen, Joseph A.,Villa, Eric M.
supporting information, p. 2098 - 2105 (2018/09/04)
The 1-substituted-4-imino-1,2,3-triazole motif is an established component of coordination compounds and bioactive molecules, but depending on the substituent identity, it can be inherently unstable due to Dimroth rearrangements. This study examined parameters governing the ring-degenerate rearrangement reactions of 1-substituted-4-imino-1,2,3-triazoles, expanding on trends first observed by L’abbé et al. The efficiency of condensation between 4-formyltriazole and amine reactants as well as the propensity of imine products towards rearrangement was each strongly influenced by the substituent identity. It was observed that unsymmetrical condensation reactions conducted at 70 °C produced up to four imine products via a dynamic equilibrium of condensation, rearrangement and hydrolysis steps. Kinetic studies utilizing 1-(4-nitrophenyl)-1H-1,2,3-triazole-4-carbaldehyde with varying amines showed rearrangement rates sensitive to both steric and electronic factors. Such measurements were facilitated by a high throughput colorimetric assay to directly monitor the generation of a 4-nitroaniline byproduct.
Synthesis and antifungal activity of 1,2,3-triazole phenylhydrazone derivatives
Dai, Zhi-Cheng,Chen, Yong-Fei,Zhang, Mao,Li, Sheng-Kun,Yang, Ting-Ting,Shen, Li,Wang, Jian-Xin,Qian, Shao-Song,Zhu, Hai-Liang,Ye, Yong-Hao
, p. 477 - 486 (2015/02/02)
A series of 1,2,3-triazole phenylhydrazone derivatives were designed and synthesized as antifungal agents. Their structures were determined based on 1H-NMR spectroscopy, MS, elemental analysis and X-ray single-crystal diffraction. The antifunga
Synthesis of novel 1-substituted triazole linked 1,2-benzothiazine 1,1-dioxido propenone derivatives as potent anti-inflammatory agents and inhibitors of monocyte-to-macrophage differentiation
Gannarapu, Malla Reddy,Vasamsetti, Sathish Babu,Punna, Nagender,Kotamraju, Srigiridhar,Banda, Narsaiah
, p. 1494 - 1500 (2015/08/18)
A series of novel 1-substituted-triazole linked 1,2-benzothiazine 1,1-dioxido propenone derivatives 8a-s & 12a-l were prepared from 1-substituted 1,2,3-triazol-4-aldehydes 6 & 11 with N-methyl-3-acetyl-4-hydroxybenzothiazine-1,1-dioxide 7 by condensation.
