ABSTRACT
Two new Mg(II)-based and Zn(II)-based coordination polymers, {[Mg3(BTB)(DMA)4](DMA)2}n (1, H3BTB=1,3,5-benzenetrisbenzoic acid, DMA=N,N-dimethylacetamide) and {(H2NMe2)2[Zn3(BTB)2(OH)(Im)](DMF)9(MeOH)7}n (2, Im=imidazole, DMF=N,N-dimethylformamide), have been successfully synthesized and structurally characterized under solvothermal conditions. 1 contains a linear [Mg3(COO)6] cluster that connected by the fully deprotonated BTB3- ligands to give a kgd-type 2D bilayer structure; 2 represents a microporous 3D pillar-layered system based on the binuclear Zn units and pillared Im ligands, which shows a (3,5)-connected hms topological net. In addition, in vitro anticancer activities of compounds 1 and 2 on 4 human liver cancer cells (HB611, HHCC, BEL-7405 and SMMC-7721) were determined.
Subject(s)
Humans , Benzimidazoles/pharmacology , Metal-Organic Frameworks/pharmacology , Liver Neoplasms/drug therapy , Antineoplastic Agents/pharmacology , Zinc/chemistry , Benzimidazoles/chemical synthesis , Molecular Structure , Cell Line, Tumor , Metal-Organic Frameworks/chemical synthesis , Ligands , Liver Neoplasms/pathology , Magnesium/chemistry , Antineoplastic Agents/chemical synthesisABSTRACT
A set of heterocyclic benzimidazole derivatives bearing 1,3,5-triazine group with different substituents at C-2 and C-5 of the benzimidazole ring have been synthesized and evaluated for their antiviral activities against HSV-1. The structures of these compounds have been established by analytical data, IR spectra, [1]H NMR, and mass spectra. Compounds 8a and 8b proved to be the most active antiherpetic agents in this study, at EC[50]% concentrations of 2.9, 3.4 mg/ml, respectively. Computational evaluation of the quantum chemical descriptors such as hydrophobicity [log P], HOMO and LUMO, and the gap energy, were calculated and correlated with the antiviral activity. The tested compounds showed proper degree of hydrophobicity [<0.5 - >5]. The HOMO-LUMO gap energy values of the tested compounds are comparable with the observed values for the antiviral drug, Acyclovir
Subject(s)
Benzimidazoles/chemical synthesis , Antiviral Agents , Drug Design , Drug Evaluation , Hydrophobic and Hydrophilic Interactions , TriazinesABSTRACT
New derivatives of 6-nitro-2-substituted acetamidobenzothiazole [2a, 3a-e], 3-substituted 2-iminothiazolidin-4-one [4a-e] and 5-arylidene-2-iminothiazolidin-4-one [5a-j] were prepared. The testing for the anthelminitic activity of two of the newly prepared compounds using the earthworm method showed that they produce a promising effect. The detailed synthesis, spectroscopic and biological data are reported
Subject(s)
Benzimidazoles/chemical synthesis , Thiazoles/chemical synthesis , Anthelmintics/chemical synthesis , Thiazoles/pharmacologyABSTRACT
Alpha -cyano - [xanthen-9-yl]-hydrazides 2 were cyclised to give 3-amino-4 [substituted-xanthen-9-yl]-pyrazolo-5 [4H] ones 3. Benzimidazole -[9-xanthen] 2-acetonitrilss 7 were formed by condensation of benzimidazole jole-2-acetonitrile with xanthen-9-olea. 3 and 7 were pyrolysed under reduced pressure to give 9-substituted-xanthenes. Various classes of nitrogen hetegocydes such as benzimidazoles, pyrazolones and analogous hetegocydes have been previously prepared and investigated for their biological activities. The aim of this work is to synthesise such compounds in an attempt to obtain newer compounds of anticipated broad spectrum biological activities