Bridged Dibenzocycloalkane Derivatives

Novel fused chromenes (4,7–11) and pyrimidines (12–16) were designed, synthesized, and evaluated for their mammary gland breast cancer (MCF-7), human colon cancer (HCT-116), and liver cancer (HepG-2) activities. The structural identity of the synthesized compounds was established according to their spectroscopic analysis, such as FT-IR, NMR, and mass spectroscopy. The preliminary results of the bioassay disclosed that some of the target compounds were proven to have a significant antiproliferative effect against the three cell lines, as compared to Doxorubicin, Vinblastine, and Colchicine, used as reference drugs. Particularly, compounds 7 and 14 exerted promising anticancer activity towards all cell lines and were chosen for further studies, such as cell cycle analysis, cell apoptosis, caspase 3/7 activity, DNA fragmentation, cell invasion, and migration. We found that these potent cytotoxic compounds induced cell cycle arrest at the S and G2/M phases, prompting apoptosis. Furtherm...

The present article reports the design of new fused, heterocyclic compounds by cyclocondensation. The structures formulae of designed compounds were identified by 1H-NMRe spectrum Ft-IR spectrum and C, H, N elemental analysis. Antibacterial activity of fused, heterocyclic studied against some pathogenic bacterial strains isolated from patients like E. coli, Klebsiellaae, Acinetobacter, Aeromonas, Staphylococcus and Streptococcus. Eventually, antibacterial of the fused heterocyclic compounds was exhibited significant growth inhibition against some pathogenic bacteria which considered an important source of new Antibacterial compounds. The results of such studies are discussed in this paper.

A general review (138 references) focused on the recent advances in the application of Meldrum's acid reactivity for synthesis of diverse pyridine and pyrimidine derivatives, mostly small and drug-like molecules is presented.

Most all tricyclic compounds derived from theophylline were investigated in the respect of their anticancer, circulatory blood system activity and as anti-inflammatory agents. The synthesis of new tricyclic purine derivatives with anellated in 7,8-position of theophylline five, six, seven membered heterocyclic ring system. of lactam and non-lactam structure modified by a basic substituent at N8, N9 and N10 position. It has been shown that new tricyclic theophylline derivatives possess sedative, analgesic properties, neurolleptic-like activity and hypothermizing properties. Some structural elements modification influence the central nervous system activity in the respect of: - Kind of the additional ring. - Alkylamine substituent in 9 position of tricyclic system. Our goal was to give a wide scope literature review of the tricyclic and tetracyclic theophylline derivatives as adenosine, 5-HT, benzodiazpine receptors, and phosphodiaesterase inhibitors, because the new compounds are of ...

The global spread of drug resistance in bacteria requires new potent and safe antimicrobial agents. Compounds containing the 1,2,4-triazole ring in their structure are characterised by multidirectional biological activity. A large volume of research on triazole and their derivatives has been carried out, proving significant antibacterial activity of this heterocyclic core. This review is useful for further investigations on this scaffold to harness its optimum antibacterial potential. Moreover, rational design and development of the novel antibacterial agents incorporating 1,2,4-triazole can help in dealing with the escalating problems of microbial resistance.

The chemistry of heterocyclic containing, 1,3,4-thiadiazole has been an interesting field of study from ancient years. Subsequently, 1,3,4-thiadiazole nucleus constitutes a significant class of compounds for new drug development. Recently, various 1,3,4-thiadiazole derivatives synthesized and evaluated their biological activities including antimicrobial, antituberculosis, antioxidant, anti-inflammatory, anticonvulsants, antidepressant and anxiolytic, antihypertensive, anticancer and antifungal activity. The search for anticancer compounds with more selective activities and lower side effect continues to be an active area of argument examination in medicinal chemistry. This review elaborately described the medicinal chemistry, their structural activity relationship, and anticancer properties with respect to human cell line based approach related to synthesized 1,3,4-thiadiazole derivatives.

An efficient and green method for the synthesis of phthalide [isobenzofuran-1(3H)-one] fused pyrazoles via the catalyst-free condensation reaction of 2-formylbenzoic acid, hydrazine hydrate, and acetylenic esters in water is reported. Reaction of 2-formylbenzoic acid with 6-amino-uracils or cyclic 1,3-diketones resulted in the formation of phthalide-fused pyrimidine or cyclic 1,3-diketone derivatives.

FtsZ and ZipA are essential components of the septal ring apparatus, which mediates cell division in Escherichia coli. FtsZ is a cytoplasmic tubulin-like GTPase that forms protofilament-like homopolymers in vitro. In the cell, the protein assembles into a ...

In the quest for discovery of novel bioactive molecules, new heterocyclic ring systems provide templates for exploration of uncharted chemical space. Herein, we describe the synthesis of a new benzo[4,5]imidazo[1,2-b][1,2,4,6]thiatriazine derivative from readily available 1,2-diaminobenzimidazole and N,N-diethyl-N′-chlorosulfonyl chloroformamidine. The product structure, confirmed by X-ray crystallography, bears an exocyclic NH2 group, which should enable synthesis of an extended range of derivatives of this unusual scaffold.

The construction of cis-fused heterobicyclic system involved in neuroactive natural products such as dysiherbaine has been accomplished by employing Prins strategy using 1,3,5-trioxane as an equivalent for formaldehyde. The reactions allowed stereoselective construction of the trisubstituted cis-fused hexahydro-2H-furo[3,2-b]pyran with maximum yield of 60%. The tetrahydropyrans are crucial class of ring system that exist as constituents in many bioactive natural products. 1 They play significant role as critical parts of structures in drug discovery and research. 1,2 In our laboratory we have been specially paying attention to the cis-fused heterobicyclic system that can be found in neuronally active agents such as dysiherbaine. 3 It has been noted that the reaction of homoallylic alcohols with aldehyde in the presence of acid catalyst produces a lots of tetrahydropyran derivatives. 2 This reaction is known as Prins cyclization. 4 It has also been recognized that the rate of Prins cyclization relies on the type of aldehyde used; the reaction proceeds smoothly with cinnamaldehyde in comparison with benzaldehyde or acrolein. 2,3 It has been predicted, however, that Prins cyclization would be challenging using formaldehyde or the equivalents to assemble tetrahydropyran structure. 5 Stereoselectivity in Prins cyclization has been also of interest. Although Prins cyclization leading to trisubstituted cis-fused hexahydro-2H-furo[3,2-b]pyran derivatives (cis-fused THP derivatives) had not been well explored and the stereochemical course could not be predicted until recently, in 2002, Alder et al. had described the theoretical examination for this type of transformation, 6 and stereoselective Prins cyclization of homoallylic alcohol for trisubstituted cis-fused THP derivatives was thereafter disclosed in

A highly efficient stereoselective synthesis of sugar fused 1,2-annu-lated isochromans is reported by utilizing the oxa-Pictet-Spengler cyclization reaction. The process is found to be very general as both glucal and galactal derived C2-hydroxy-α-C-aryl glycosides lead to the target molecules in good yields. The utility of this strategy was extended to the synthesis of sugar fused isochromanones, which are bergenin type molecules.

The synthesis and uses of different kinds of carbohydrate-based lactones are described. This group of compounds includes aldonolactones, other related monocyclic lactones and bicyclic systems. The latter can arise from uronic acids, carboxymethyl ethers or glycosides, or from C-branched sugars.

A novel series of cis-fused 2-N,N-dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo[b,f]furo[2,3-d]oxepin derivatives modified at position C-11 was prepared and evaluated for its potential antidepressant/anxiolytic properties. In vitro affinities for the norepinephrine transporter and for 5-HT(2A) and 5-HT(2C) receptors, as well as the ED(50) values obtained in some in vivo assays predictive for antidepressant and anxiolytic potential are reported.

A new series of pyrano-chromene and pyrimido pyrano-chromene derivatives were synthesized starting from 2-amino-4-(1-naphthyl)-5-oxo-4H,5H-pyrano[3,2-c]chromene-3-carbonitrile (6). The structures of the synthesized compounds were elucidated by spectral data. Compounds 6–11, 13–15 and 18 have been selected for their inhibitory activity screening against HIV-1 and HIV-2 in MT-4 cells.

novel synthesis of 3,4-fused furans (both tricyclic and bicyclic) through platinumcatalyzed cyclization of 3-(2-formylcycloalkenyl)-acrylic amides 2 in methanol is described (up to 90% yield). Tricyclic 3,4-fused dihydrofuran derivatives were also obtained via reductive cyclization of 2. The substrates 2 were obtained from β- bromovinyl aldehydes by a Pd-catalyzed Heck reaction.