6281-57-8Relevant academic research and scientific papers
Synthesis and biological evaluation of 3-amino-1,2,4-triazole derivatives as potential anticancer compounds
Benhida, Rachid,Demange, Luc,Dufies, Maeva,Grytsai, Oleksandr,Hagege, Anais,Martial, Sonia,Pagès, Gilles,Penco-Campillo, Manon,Ronco, Cyril,Valiashko, Oksana
, (2020/10/02)
Two series of compounds carrying 3-amino-1,2,4-triazole scaffold were synthesized and evaluated for their anticancer activity against a panel of cancer cell lines using XTT assay. The 1,2,4-triazole synthesis was revisited for the first series of pyridyl derivatives. The biological results revealed the efficiency of the 3-amino-1,2,4-triazole core that could not be replaced and a clear beneficial effect of a 3-bromophenylamino moiety in position 3 of the triazole for both series (compounds 2.6 and 4.6) on several cell lines tested. Moreover, our results point out an antiangiogenic activity of these compounds. Overall, the 5-aryl-3-phenylamino-1,2,4-triazole structure has promising dual anticancer activity.
Solution-phase microwave assisted parallel synthesis of N,N′-disubstituted thioureas derived from benzoic acid: Biological evaluation and molecular docking studies
Rauf, Muhammad Khawar,Talib, Ammara,Badshah, Amin,Zaib, Sumera,Shoaib, Khurram,Shahid, Mohammad,Fl?rke, Ulrich,Imtiaz-Ud-Din,Iqbal, Jamshed
, p. 487 - 496 (2013/11/19)
An efficient and facile microwave-assisted solution phase parallel synthesis for a 26-member library of N,N′-disubstituted thiourea analogs were accomplished successfully. The reaction time for synthesis of analogs was drastically reduced from a reported 8-12 h to only 10 min. Compounds were more than 95% pure, as characterized by modern analytical techniques, i.e. 1H & 13C NMR and FT-IR. The solid phase structural analysis has also been performed by single crystal XRD analysis. Synthesized compounds were preliminary screened for their in vitro urease inhibition and antifungal activity. Most of the compounds were found to be potent inhibitors of urease. However, the most significant activity was found for 11 with IC 50 of 1.67 μM. The docking scores correlate with the IC 50 values of inhibitors.
New supramolecular ferrocenyl phenylguanidines as potent antimicrobial and DNA-binding agents
Gul, Rukhsana,Khan, Azim,Badshah, Amin,Rauf, Muhammad Khawar,Shah, Afzal,-Rehman, Zia-Ur,Bano, Asghari,Naz, Rabia,Tahir, Muhammad Nawaz
, p. 1959 - 1973 (2013/07/28)
Six new ferrocenyl phenylguanidines have been synthesized and characterized by elemental analysis, FT-IR, multinuclear (1H and 13C) NMR, and single crystal analysis. The latter showed a supramolecular structure for 2 mediated by O H and π H interactions. A subsequent DNA-binding study of these complexes proved them to be good DNA binders with the binding constant varying in the range of 1.2-5.6×105M-1. These compounds were found to have moderate antibacterial and significant antifungal activities, especially for compounds having a chlorophenyl. These compounds may emerge as a new class of anticancer and antifungal agents alone or in combination with other drugs.
CHARACTERIZATION OF THE COMPLEXES OF SOME BIOLOGICALLY ACTIVE N-ARYL-N'-BENZOYLTHIOCARBAMIDES WITH METAL(II) PHTHALIMIDES
Sharma, C. L.,Mishra, V. P.
, p. 3 - 8 (2007/10/02)
The mixed ligand complexes of Cu(II), Pd(II), Pt(II), Co(II) and Ni(II) with phthalimide as primary and N-aryl-N'-benzoylthiocarbamides as secondary ligands have been prepared and characterized on the basis of chemical analysis, conductance, magnetic meas
