64374-52-3Relevant academic research and scientific papers
Synthesis and antimalarial activity of novel dihydro-artemisinin derivatives
Liu, Yang,Cui, Kunqiang,Lu, Weiqiang,Luo, Wei,Wang, Jian,Huang, Jin,Guo, Chun
, p. 4527 - 4538 (2011/08/10)
The Plasmodium falciparum cysteine protease falcipain-2, one of the most promising targets for antimalarial drug design, plays a key role in parasite survival as a major peptide hydrolase within the hemoglobin degradation pathway. In this work, a series of novel dihydroartemisinin derivatives based on (thio)semicarbazone scaffold were designed and synthesized as potential falcipain-2 inhibitors. The in vitro biological assay indicated that most of the target compounds showed excellent inhibition activity against P. falciparum falcipain-2, with IC50 values in the 0.29-10.63 μM range. Molecular docking studies were performed to investigate the binding affinities and interaction modes for the inhibitors. The preliminary SARs were summarized and could serve as a foundation for further investigation in the development of antimalarial drugs.
Synthesis, characterization and spectral evaluation of some new substituted thiosemicarbazides and thiosemicarbazones
Pareek, Alok K.,Joseph,Seth, Daya S.
experimental part, p. 1549 - 1552 (2011/10/12)
A new series of substituted thiosemicarbazides and substituted thiosemicarbazones containing different functional groups, thiosemicarbazones have been synthesized by the condensation reaction between newly synthesized substituted thiosemicarbazides with s
Synthesis, anticancer and antibacterial activity of some novel mononuclear Ru(II) complexes
Mazumder, Upal Kanti,Gupta, Malaya,Karki, Subhas Somalingappa,Bhattacharya, Shiladitya,Rathinasamy, Suresh,Thangavel, Sivakumar
, p. 178 - 185 (2007/10/03)
In search of potential anticancer drug candidates in ruthenium complexes, a series of mononuclear ruthenium complexes of the type [Ru(phen) 2(nmit)]Cl2 (Ru1), [Ru(bpy)2(nmit)]Cl 2 (Ru2), [Ru(phen)2(icpl)]Cl2 (Ru3), Ru(bpy)2(icpl)]Cl2 (Ru4) (phen51,10-phenanthroline; bpy=2,2′-bipyridine; nmit=N-methyl-isatin-3-thiosemicarbazone, icpl=isatin-3-(4-Cl-phenyl)thiosemicarbazone) and [Ru(phen)2(aze)] Cl2 (Ru5), [Ru(bpy)2(aze)]Cl2 (Ru6) (aze=acetazolamide) and [Ru(phen)2(R-tsc)](ClO4) 2 (R=methyl (Ru7), ethyl (Ru8), cyclohexyl (Ru9), 4-Cl-phenyl (10), 4-Br-phenyl (Ru11), and 4-EtO-phenyl (Ru12), tsc=thiosemicarbazone) were prepared and characterized by elemental analysis, FTIR, 1H-NMR and FAB-MS. Effect of these complexes on the growth of a transplantable murine tumor cell line (Ehrlich Ascites Carcinoma) and their antibacterial activity were studied. In cancer study the effect of hematological profile of the tumor hosts have also been studied. In the cancer study, the complexes Ru1-Ru4, Ru10 and Ru11 have remarkably decreased the tumor volume and viable ascitic cell count as indicated by trypan blue dye exclusion test (p0.05). Treatment with the ruthenium complexes prolonged the lifespan of Ehrlich Ascites Carcinoma (EAC) bearing mice. Tumor inhibition by the ruthenium chelates was followed by improvements in hemoglobin, RBC and WBC values. All the complexes showed antibacterial activity, except Ru5 and Ru6. Thus, the results suggest that these ruthenium complexes have significant antitumor property and antibacterial activity. The results also reflect that the drug does not adversely affect the hematological profiles as compared to that of cisplatin on the host.
