30369-88-1Relevant academic research and scientific papers
Synthesis of series of triazine derivatives and their evaluation against root knot nematode meloidogyne incognita
Kaur, Jagdish,Utreja, Divya,Dhillon,Sharma, Shivali
, p. 870 - 877 (2018/11/06)
Nine triazine derivatives were synthesized by reacting triazine with different aromatic amines. The synthesized derivatives were characterized by IR, NMR spectral studies and micro analytical data. The resulted compounds had also been evaluated for their in vitro antinemic studies against root knot nematode, Meloidogyne incognita. All compounds showed considerable nematicidal activity as compared to the control when screened for their hatching inhibition and mortality potential.
Identification of novel vacuolin-1 analogues as autophagy inhibitors by virtual drug screening and chemical synthesis
Chen, Chang,Lu, Yingying,Siu, Ho Ming,Guan, Jintao,Zhu, Longchao,Zhang, Shuang,Yue, Jianbo,Zhang, Liangren
, (2017/06/19)
Autophagy is a fundamental cellular degradation process which is essential for cell homeostasis, and dysfunctional autophagy has been associated with a variety of human diseases, such as cancer. Several autophagy chemical modulators have been applied in a number of preclinical or clinical trials against these autophagy related diseases, especially cancer. Small molecule vacuolin-1 potently and reversibly inhibits both endosomal-lysosomal trafficking and autophagosome-lysosome fusion, yet the molecular mechanisms underlying vacuolin-1 mediated autophagy inhibition remain unknown. Here, we first performed the virtual drug screening and identified 14 vacuolin-1 analogues as autophagy inhibitors. Based on these virtual screening results, we further designed and synthesized 17 vacuolin-1 analogues, and found that 13 of them are autophagy inhibitors and a couple of them are as potent as vacuolin-1. In summary, these studies expanded the pool of useful autophagy inhibitors and reveal the structural-activity relationship of vacuolin-1 analogues, which is useful for future development of vacuolin-1 analogues with high potency and for identification of the molecular targets of vacuolin-1.
Synthesis and structure-activity relationship study of triazine-based inhibitors of the DNA binding of NF-κB
Fujii, Shinya,Kobayashi, Takanobu,Nakatsu, Aki,Miyazawa, Hiroshi,Kagechika, Hiroyuki
, p. 700 - 708 (2014/08/05)
Nuclear transcription factor nuclear factor-kappa B (NF-κB) has diverse pathophysiological functions, and NF-κ B inhibitors are considered to be candidates for multiple therapeutic applications. We previously reported a novel triazine-based NF-κB inhibitor, 2-anilino-4,6-dichloro-1,3,5- triazine (NI241), that directly inhibits DNA binding of NF-κB. Here, we report synthesis of a series of triazine derivatives and evaluation of their structure-activity relationships for NF-κB inhibition. We found that 2-amino-4,6-dichloro-1,3,5-triazine substructure is essential for the inhibitory activity of the lead compound NI241, and modification of NI241 by introduction of an m-methoxy substituent on the phenyl ring afforded the more potent derivative 28. The structure-activity relationships identified in this study suggested a possible mechanism of irreversible NF-κB inhibition by NI241, and should be helpful in the design of other NF-κB inhibitors.
Synthesis and in vitro antibacterial screening of some new 2,4,6-trisubstituted-1,3,5-triazine derivatives
Singh, Ravi Bhushan,Das, Nirupam,Jana, Srabanti,Das, Aparoop
experimental part, p. 316 - 321 (2012/06/18)
With an objective to evaluate the antibacterial activity of triazine derivatives, a series of 2,4,6-trisubstituted-1,3,5-triazine were synthesized and characterized by FTIR, 1H-NMR, 13C-NMR, mass spectroscopy and elemental analysis. The minimum inhibitory concentration (MIC) of the compounds that displayed favourable zone of inhibition was determined by broth microdilution method. Derivatives with morpholinyl substituent (4a and 4i) demonstrated good in vitro activities against Gram-positive organisms, whereas two of the compound bearing a diethylamino side chain exhibited moderate (4e) to broad spectrum (4j) activity comparable to streptomycin. The promising activity of the latter maybe attributed to the substitution of electron releasing group at para position of phenyl rings.
