As dioxolane and oxathiolane nucleosides have exhibited promising antiviral anticancer activities, it was of interest to synthesize isoelectronically substituted oxaselenolane nucleosides, in which the 3'-CH2 is replaced by a selenium atom. To study structure−activity relationships, various pyrimidine purine were synthesized from key intermediate, (±)-2-benzoyloxymethyl-1,2-oxaselenolane 5-acetate (6). Among racemic cytosine 5-fluorocytosine analogues potent anti-HIV anti-HBV activities. It...

The recent outbreak of severe acute respiratory syndrome (SARS), which is an illness, caused by newly discovered SARS coronavirus (SARS-CoV). Herein we describe the antiviral activity several classes nucleoside analogues evaluated against SARS-CoV in Vero 76 cells, some exhibited moderate activity.

Shigella flexneri is an enteropathogen responsible for severe dysentery in humans. VirF a key transcriptional regulator that activates the expression of downstream virulence factors required cellular invasion and cell-to-cell spread this pathogen. There are several environmental induce translation including temperature, pH, osmolarity post-transcriptional RNA modification. Durand colleagues (vacC, virulence-associated chromosomal locus flexneri, homologous to tgt, gene encoding tRNA-guanine...

It has been established that the growth of most prostate carcinomas depends on androgen stimulation. The inhibition cytochrome P450-17 (CYP17) to block biosynthesis is therefore regarded as a promising approach therapy. Based our previously identified lead compound Ref 1, series fluorine-substituted biphenyl methylene imidazoles were designed, synthesized, and evaluated CYP17 inhibitors elucidate influence fluorine in vitro vivo activity. was found meta-fluoro substitution at C ring improved...

Human protein kinase CK2 is an ubiquitous serine/threonine that typically found in tetrameric complexes consisting of two catalytic (α and/or α′) and regulatory β subunits. Although there growing evidence besides the participation a complex series cellular functions, this involved cell viability, proliferation, neoplastic transformation. In present study, 3-(substituted-benzylidene)-1,3-dihydro-indolin-2-thione derivatives corresponding indolin-2-one congeners were tested for their...

A few series of indole derivatives were screened for antimicrobial, antifungal and anti-HBV activities. The compounds tested their in vitro antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli Candida albicans using a disc diffusion method, which measures the diameter inhibition zone around paper soaked solution test compounds. antimicrobial results showed that all are as active standard compound ampicillin aureus. It was also found carboxamide...

Background: Recent studies showed that the cooperation between c-SRC and EGFR is responsible for more aggressive phenotype in diverse tumors, including glioblastomas carcinomas of colon, breast, lung. Studies show combination SRC inhibitors can induce apoptosis delay acquired resistance to chemotherapy. Therefore, such may lead a new therapeutic strategy treatment EGFR-mutant lung cancer. Osimertinib was developed as third-generation EGFR-TKI combat toxicity mutant inhibitors. Due adverse...

The anti-lipid peroxidation (LP) activity and anti-superoxide formation (SOD) of new N-H N-substituted indole derivatives were evaluated to determine their antioxidant activity. results showed that compounds 1, 2, 5, 9 12 demonstrate considerable inhibition lipid mouse liver homogenate. On the other hand, 5 at a concentration 10−4 M. Consequently, it can be concluded these exhibit important compared with reference compound α-tocopherol (vitamin E).

Indole-2 and 3-carboxamides (IDs) are proposed to be selective cyclooxygenase inhibitors. Since cyclooxygenase-1 may involved in reactive oxygen species (ROS) production, we hypothesize that these indole derivatives have antioxidative properties. We employed chemiluminescence (CL) electron spin resonance (ESR) trapping examine this hypothesis. report here the results of a study reactivity 10 selected towards ROS. The following generators ROS were applied: potassium superoxide (KO2) as source...

The hydroxyl radical (HO*)- and superoxide anion (O* (2))-scavenging activity, as well the singlet oxygen ((1)O(2))-quenching property of N-substituted indole-2-carboxylic acid esters (INDs) were investigated by deoxyribose degradation assay, a chemiluminescence method electron spin resonance (ESR) spin-trapping technique. This novel group compounds was developed search for cyclooxygenase-2 (COX-2)-selective enzyme inhibitors. results obtained demonstrated that 16 examined, five inhibited...

In recent years, antioxidant compounds play an important role as a health-protecting factor. Antioxidants protect cells against the damaging effects of reactive oxygen species (ROS). An imbalance between antioxidants and ROS results in oxidative stress, which leads to cellular damage it is linked many vital diseases. It was shown that heme oxygenase (HO) provides efficient cytoprotection stress. this study, series indole-2-carboxamide 3-acetamide derivatives tested for vitro on HO activity...

Abstract The title compounds, 1,2‐dialkyl‐benzimidazole‐5(6)‐carboxylic acids 34–45 were prepared at four steps; 1) preparation of mono amide derivatives 1–11 by the reaction methyl 3,4‐diaminobenzoate and substituted phenyl or phenoxyacetic acid chlorides; 2) benzimidazolecarboxyl‐ates 12–22 , with zinc chloride dry hydrogen gas; 3) alkaline hydrolysis esters 23–33 ; 4) substitution imidazole ring benzyl p ‐fluorobenzyl bromide, in alkali medium. 2‐Aryl‐benzimidazole‐5(6)‐carboxylic 50–53...

Therapy with receptor tyrosine kinase inhibitors provides an improved treatment option in a number of diseases such as cancer, myocardial infection, osteoporosis, stroke, and neurodegeneration. We have designed, synthesized, evaluated series novel 2-amino-5-[(benzyl)imino]methyl-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidine-4-one 7a 2-amino-5-[(substituted-benzyl)imino]methyl-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidine-4-one 7b-e derivatives potential inhibitors. These compounds were synthesized by...

In this study, the synthesis and potential enzyme interactions of new Pyrrolo[2,3-d]pyrimidine derivatives along with their inhibitory activity against SFK enzymes such as Fyn, Lyn, Hck, c-Src were reported. The results indicated that compounds slightly active tested in comparison PP2 for A-419259 Lyn CGP77675 c-Src. Compound N-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)-4-(3,4-dimethoxyphenyl)butanamide (5) was identified a non-selective slight inhibitor However, did...

Abstract We report the synthesis of SAHAquines and related primaquine (PQ) derivatives. are novel hybrid compounds that combine moieties suberoylanilide hydroxamic acid (SAHA), an anticancer agent with weak antiplasmodial activity, PQ, antimalarial drug low antiproliferative activity. The preparation is simple, cheap, high yielding. It includes following steps: coupling reaction between a dicarboxylic monoester, hydrolysis, new O ‐protected hydroxylamine, deprotection. 5 – d showed...

A series of N-substituted indole-2-carboxamide and indole-3-acetamide derivatives have been prepared their in vitro effects on rat liver lipid peroxidation levels superoxide anion formation were determined. The results clearly demonstrate that indole 4, 5, 10, 15, 17 are very efficient antioxidants compared to alpha-tocopherol.

D- and L-2',3'-dideoxy-2',3'-endo-methylene nucleosides were synthesized as potential antiviral agents. The key intermediates 5-O-tert-butyldiphenylsilyl-D- L-2,3-dideoxy-2, 3-endo-methylenepentofuranoses (20 33, respectively) obtained by selective protection of the 3-endo-methylenepentose derivatives 19 32 which prepared from 1,2:5,6-di-O-isopropylidene-D-mannitol L-gulonic gamma-lactone, respectively, converted to 3-endo-methylenepentofuranosyl acetates (21 34, or chlorides 22 35....