28668-95-3Relevant articles and documents
Synthesis and anticancer screening of triazine analogues
Tiwari, Anshuly,Modi, Siddharth J.,Mahadik, Kakasaheb R.,Suryawanshi, Mugdha R.
, p. 114 - 121 (2019)
Objective: The study was aimed to investigate the cytotoxic effect of S-5H-[1,2,4]-triazino (5,6-b) indol-3-yl-3,4-phenylethane-thioate derivatives as epidermal growth factor Receptor (EGFR) inhibitors. Methods: In the present study 14 novel triazine analogues were synthesized and characterized using different spectroscopic techniques such as FTIR, NMR and Mass Spectroscopy. The anticancer activity was performed using MCF-7 (breast cancer) and K-562 (leukaemia) cell lines. Further, molecular docking was carried out using Vlife Molecular Docking Software (MDS) on crystal structure of epidermal growth factor receptor (EGFR) to identify the binding mode of interaction with an active site. Results: Compounds MA-7, MA-8, MA-12, MA-13 and MA-14 show potent activity against cancer cell lines in the range of10 to 84.4 μg/ml. Further molecular docking on EGFR also supports that there is a strong correlation between in silico and in vitro biological activity. The results of this study may be further useful for lead optimization process. Conclusion: The results of this study indicates that the synthesized triazine analogues can give a potential lead as an anticancer agent.
Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies
Rahim, Fazal,Ullah, Khadim,Ullah, Hayat,Wadood, Abdul,Taha, Muhammad,Rehman, Ashfaq Ur,Uddin, Imad,Ashraf, Muhammad,Shaukat, Ayesha,Rehman, Wajid,Hussain, Shafqat,Khan, Khalid Mohammed
, p. 81 - 87 (2015)
A new series of triazinoindole analogs 1-11 were synthesized, characterized by EI-MS and 1H NMR, evaluated for α-glucosidase inhibitory potential. All eleven (11) analogs showed different range of α-glucosidase inhibitory potential with IC
New triazinoindole bearing thiazole/oxazole analogues: Synthesis, α-amylase inhibitory potential and molecular docking study
Rahim, Fazal,Tariq, Sundas,Taha, Muhammad,Ullah, Hayat,Zaman, Khalid,Uddin, Imad,Wadood, Abdul,Khan, Aftab Ahmad,Rehman, Ashfaq Ur,Uddin, Nizam,Zafar, Salman,Shah, Syed Adnan Ali
, (2019)
New triazinoindole bearing thiazole/oxazole analogues (1–21) were synthesized and characterized through spectroscopic techniques such as HREI-MS, 1H and 13C NMR. The configuration of compound 2i and 2k was confirmed through NOESY. Al
New synthesis of the [1, 3]thiazolo- [3', 2':2, 3][1, 2, 4]triazino[5, 6-b]indole system
Kim,Zhuravlyova
, p. 1281 - 1282 (2009)
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Synthesis, in-vitro and in-silico studies of triazinoindole bearing bis-Schiff base as β-glucuronidase inhibitors
Ahmad, Shakeel,Aziz, Aamir,Khan, Fahad,Rahim, Fazal,Sarfraz, Maliha,Taha, Muhammad,Ullah, Hayat,Wadood, Abdul
, (2021/07/16)
Triazinoindole bearing bis-Schiff base analogs (1–20) were synthesized by triazinoindole-thione ring formation, triazinoindole-thiol-phenylethanone, followed by triazinoindole bis-Schiff base formation. Synthesized analogs showed β-glucuronidase potential with IC50 value ranging between 2.60 ± 0.10 to 55.40 ± 1.60 μM as compared to standard D-saccharic acid 1,4-lactone (IC50 = 48.10 ± 1.2 μM). Analog 20 was the most potent one with IC50 value 2.60 ± 0.10 μM. Analogs 17, 4 showed IC50 values 5.20 ± 0.20 and 5.70 ± 0.20 μM respectively and withstand 2nd and 3rd ranked scaffolds among the synthesized analogs. All other sixteen analogs showed many-fold better potency with IC50 values ranging from 7.9 ± 0.2 to 48.1 ± 1.2 μM. The structure-activity relationship was established and confirmed of binding interactions through molecular docking studies.
Novel Multitarget Directed Triazinoindole Derivatives as Anti-Alzheimer Agents
Patel, Dushyant V.,Patel, Nirav R.,Kanhed, Ashish M.,Patel, Sagar P.,Sinha, Anshuman,Kansara, Deep D.,Mecwan, Annie R.,Patel, Sarvangee B.,Upadhyay, Pragnesh N.,Patel, Kishan B.,Shah, Dharti B.,Prajapati, Navnit K.,Murumkar, Prashant R.,Patel, Kirti V.,Yadav, Mange Ram
, p. 3635 - 3661 (2019/08/20)
The multifaceted nature of Alzheimer's disease (AD) demands treatment with multitarget-directed ligands (MTDLs) to confront the key pathological aberrations. A novel series of triazinoindole derivatives were designed and synthesized. In vitro studies revealed that all the compounds showed moderate to good anticholinesterase activity; the most active compound 23e showed an IC50 value of 0.56 ± 0.02 μM for AChE and an IC50 value of 1.17 ± 0.09 μM for BuChE. These derivatives are also endowed with potent antioxidant activity. To understand the plausible binding mode of the compound 23e, molecular docking studies and molecular dynamics simulation studies were performed, and the results indicated significant interactions of 23e within the active sites of AChE as well as BuChE. Compound 23e successfully diminished H2O2-induced oxidative stress in SH-SY5Y cells and displayed excellent neuroprotective activity against H2O2 as well as Aβ-induced toxicity in SH-SY5Y cells in a concentration dependent manner. Furthermore, it did not show any significant toxicity in neuronal SH-SY5Y cells in the cytotoxicity assay. Compound 23e did not show any acute toxicity in rats at doses up to 2000 mg/kg, and it significantly reversed scopolamine-induced memory deficit in mice model. Additionally, compound 23e showed notable in silico ADMET properties. Taken collectively, these findings project compound 23e as a potential balanced MTDL in the evolution process of novel anti-AD drugs.
