21665-63-4Relevant academic research and scientific papers
Design and development of novel thiazolidin-4-one-1,3,5-triazine derivatives as neuro-protective agent against cerebral ischemia–reperfusion injury in mice via attenuation of NF-?B
Lu, Min,Qi, Yujun,Han, Yu,Yi, Qiong,Xu, Lei,Sun, Wenlin,Ni, Guihua,Ni, Xiaoyu,Xu, Changsong
, p. 1315 - 1327 (2020/07/13)
The present study enumerates the discovery and development of novel thiazolidin-4-one-1,3,5-triazine as neuro-protective agent against cerebral ischemia–reperfusion injury in mice. These compounds showed significant inhibition of NF-?B transcriptional activity in LPS-stimulated RAW264.7 cells, displaying compound 8k as most potent inhibitor among the tested derivative. The compound 8k was further studied in in vivo middle cerebral artery occlusion (MCAO) mice model for neuro-protective action. Results suggest that compound 8k causes attenuation of inflammation (TNF-α, IL-β, and IL-6), oxidative stress (SOD, GSH, and MDA), and apoptosis (Bcl-2, Bax, and cleaved caspase-3) in MCAO mice in concentration-dependent manner. Collectively, our results documented that compound 8k pre-treatment protects cerebral I/R. This novel lead scaffold may be helpful for investigation of new neuro-protective agent by inactivation of NF-?B.
Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs
Tber, Zahira,Wartenberg, Mylène,Jacques, Jean-Eddy,Roy, Vincent,Lecaille, Fabien,Warszycki, Dawid,Bojarski, Andrzej J.,Lalmanach, Gilles,Agrofoglio, Luigi A.
, p. 4310 - 4319 (2018/07/30)
We report herein the synthesis and biological evaluation of a new series of 2,4,6-trisubstituted 1,3,5-triazines as reversible inhibitors of human cysteine cathepsins. The desired products bearing morpholine and N-Boc piperidine, respectively, were obtained in three to four steps from commercially available trichlorotriazine. Seventeen hitherto unknown compounds were evaluated in vitro against various cathepsins for their inhibitory properties. Among them, compound 7c (4-(morpholin-4-yl)-6-[4-(trifluoromethoxy)anilino]-1,3,5-triazine-2-carbonitrile) was identified as the most potent and selective inhibitor of cathepsin S (Ki = 2 ± 0.3 nM). Also 7c impaired the autocatalytic maturation of procathepsin S. Molecular docking studies support that 7c bound within the active site of cathepsin S, by interacting with Gly23, Cys25 and Trp26 (S1 subsite), with Asn67, Gly69 and Phe70 (S2 subsite) and with Gln19 (S1′ pocket).
Design and Development of Novel 4-(4-(1H-Tetrazol-5-yl)-1H-pyrazol-1-yl)-6-morpholino-N-(4-nitrophenyl)-1,3,5-triazin-2-amine as Cardiotonic Agent via Inhibition of PDE3
Mao, Zhi-Wei,Li, Qiao-Ling,Wang, Ping,Sun, Yang-Li,Liu, Yu
, p. 268 - 276 (2016/04/26)
The classical phosphodiesterase 3A (PDE3A) inhibitors provide relaxation of the vasculature system via increasing the cellular level of cyclic adenosine monophosphate (cAMP) and proved to be useful in the management of congestive heart failure. Consequent
Design, synthesis, and cytotoxicity of novel 2,4,6-trisubstituted 1,3,5-triazines bearing aryl hydrazone moiety as potent antitumor agent
Wang, Limei,Zhao, Sijia,Bao, Guanglong,Zhang, Yu,Xi, Shuancheng,Zhou, Guolin,Zhai, Xin,Gong, Ping
, p. 621 - 630 (2016/10/18)
A novel series of 2,4,6-trisubstituted 1,3,5-triazine derivatives bearing aryl hydrazone moiety were designed and synthesized under the guidance of scaffold hopping and bioisosterism from the autophagy inhibitor VLX600. The target compounds were evaluated for cytotoxicity against HT-29 by MTT assay with VLX600 as positive control. Then, ten potent target compounds (5c-5f, 5i-5r, 5s, 5t) were further evaluated against two cancer cell lines H460 and A549 and one normal cell line WI-38. Most of them exhibited significant cytotoxicity against one or more cell lines. Particularly, a promising compound 5f was identified, which exhibited the most potent cytotoxicity against HT-29, H460 and A549 cancer cell lines with IC50 values of 0.047 μM, 0.071 μM and 0.071 μM, respectively, which was 10-to 62-folds more potent than VLX600 (IC50 = 0.47 μM, 4.1 μM, 4.4 μM). The preliminary structure-activity relationships (SARs) of the compounds were also discussed.
Anticancer activity of 4-aminoquinoline-triazine based molecular hybrids
Manohar, Sunny,Pepe, Antonella,Velez Gerena, Christian E.,Zayas, Beatriz,Malhotra, Sanjay V.,Rawat, Diwan S.
, p. 7062 - 7067 (2014/02/14)
In this study the potential for anticancer activity of 4-aminoquinoline- triazine based hybrids has been investigated on 60 human cancer cell lines (NCI 60). The representative compounds show activity on a range of cell lines and apoptosis as the mode of growth inhibition. The Royal Society of Chemistry 2014.
Synthesis, in vitro antiplasmodial activity and cytotoxicity of a series of artemisinin-triazine hybrids and hybrid-dimers
Cloete, Theunis T.,De Kock, Carmen,Smith, Peter J.,N'Da, David D.
, p. 470 - 481 (2014/03/21)
A series of artemisinin-triazine hybrids and hybrid-dimers were synthesized and their in vitro antimalarial activity against the chloroquine sensitive (CQS), the gametocytocidal (NF54) and the choroquine resistant (CQR) Dd2 strains of Plasmodium falciparu
4-aminoquinoline-triazine-based hybrids with improved in vitro antimalarial activity against CQ-sensitive and CQ-resistant strains of plasmodium falciparum
Manohar, Sunny,Khan, Shabana I.,Rawat, Diwan S.
, p. 625 - 630 (2013/06/27)
A systematic chemical modification in the triazine moiety covalently attached via suitable linkers to 4-amino-7-chloroquinolines yielded a series of new 7-chloro-4-aminoquinoline-triazine hybrids exhibiting high in vitro activity against W2 (chloroquine-resistant) and D6 (chloroquine-sensitive) strains of Plasmodium falciparum without any toxicity against mammalian cell lines (Vero, LLC-PK11, HepG2). Many of the compounds (6, 8, 10, 11, 13, 14, 16, 27, 29 and 33) showed excellent potency against chloroquine sensitive and resistant strains. In particular, compounds 6, 8, 14, 16 and 29 were found to be significantly more active than chloroquine against the chloroquine-resistant strains (W2 clone) of P. falciparum.
Synthesis and antimalarial-activity evaluation of tetraoxane-triazine hybrids and spiro[piperidine-4,3′-tetraoxanes]
Kumar, Nitin,Khan, Shabana I.,Rawat, Diwan S.
experimental part, p. 1181 - 1197 (2012/09/22)
A series of tetraoxane-triazine hybrids and spiro[piperidine-4,3′- tetraoxanes] have been synthesized, and all the compounds were screened for in vitro antimalarial activity against chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains of Plas
