Synthesis and antiproliferative effect of novel 4-thiazolidinone-, pyridine- and piperazine-based conjugates on human leukemic cells

The present work reveals the synthesis and antiproliferative effect of a series of 2, 3 disubstituted 4-thiazolidinone analogues on human leukemic cells. The chemical structures of newly synthesized compounds were confirmed by IR, H-1 NMR, C-13 NMR and mass spectral analysis. Compound methyl 3-methoxy-4-(4-oxo-3-(5-(piperazin-1-yl)pyridin-2-yl)thiazolidin-2-yl)be nzoate (5) displayed potent activity (IC50 9.71, 15.24 and 19.29 mu M) against Nalm6, K562, Jurkat cells. Cell cycle analysis and mitochondrial membrane potential further confirmed that compound 5 is cytotoxic and able to induce cell death. (C) 2014 Elsevier Masson SAS. All rights reserved.

Sheltered coastal environments as archives of paleo-tsunami deposits: Observations from the 2004 Indian Ocean tsunami

The 2004 earthquake left several traces of coseismic land deformation and tsunami deposits, both on the islands along the plate boundary and distant shores of the Indian Ocean rim countries. Researchers are now exploring these sites to develop a chronology of past events. Where the coastal regions are also inundated by storm surges, there is an additional challenge to discriminate between the deposits formed by these two processes. Paleo-tsunami research relies largely on finding deposits where preservation potential is high and storm surge origin can be excluded. During the past decade of our work along the Andaman and Nicobar Islands and the east coast of India, we have observed that the 2004 tsunami deposits are best preserved in lagoons, inland streams and also on elevated terraces. Chronological evidence for older events obtained from such sites is better correlated with those from Thailand, Sri Lanka and Indonesia, reiterating their usefulness in tsunami geology studies. (C) 2014 Elsevier Ltd. All rights reserved.

Photocytotoxic oxovanadium(IV) complexes of ferrocenyl-terpyridine and acetylacetonate derivatives

Oxovanadium(IV) complexes VO(Fc-tpy)(acac)](ClO4) (1), VO(Fc-tpy)(nap-acac)](ClO4) (2), VO(Fc-tpy)(py-acac)](ClO4) (3) and VO(Ph-tpy)(py-acac)](ClO4) (4) of 4'-ferroceny1-2,2':6',2 `'-terpyridine (Fc-tpy) and 4'-phenyl-2,2':6',2 `'-terpyridine (Ph-tpy) having monoanionic acetylacetonate (acac), naphthylacetylacetonate (nap-acac) or pyrenylacetylacetonate (py-acac) ligand were prepared, characterized and their photocytotoxicity in visible light studied. The ferrocenyl complexes 1-3 showed an intense charge transfer band near 585 nm in DMF and displayed Fc(+)/Fc and V(IV)/V(III) redox couples near 0.66 V and -0.95 V vs. SCE in DMF-0.1 M TBAP. The complexes as avid binders to calf thymus DNA showed significant photocleavage of plasmid DNA in green light (568 nm) forming center dot OH radicals. The complexes that are photocytotoxic in HeLa and MCF-7 cancer cells in visible light (400-700 nm) with low dark toxicity remain nontoxic in normal fibroblast 3T3 cells. ICP-MS and fluorescence microscopic studies show significant cellular uptake of the complexes. Photo-irradiation of the complexes causes apoptotic cell death by ROS as evidenced from the DCFDA assay. (C) 2015 Elsevier Masson SAS. All rights reserved.

Do carboximide-carboxylic acid combinations form co-crystals? The role of hydroxyl substitution on the formation of co-crystals and eutectics

Carboxylic acids, amides and imides are key organic systems which provide understanding of molecular recognition and binding phenomena important in biological and pharmaceutical settings. In this context, studies of their mutual interactions and compatibility through co-crystallization may pave the way for greater understanding and new applications of their combinations. Extensive co-crystallization studies are available for carboxylic acid/amide combinations, but only a few examples of carboxylic acid/imide co-crystals are currently observed in the literature. The non-formation of co-crystals for carboxylic acid/imide combinations has previously been rationalized, based on steric and computed stability factors. In the light of the growing awareness of eutectic mixtures as an alternative outcome in co-crystallization experiments, the nature of various benzoic acid/cyclic imide combinations is established in this paper. Since an additional functional group can provide sites for new intermolecular interactions and, potentially, promote supramolecular growth into a co-crystal, benzoic acids decorated with one or more hydroxyl groups have been systematically screened for co-crystallization with one unsaturated and two saturated cyclic imides. The facile formation of an abundant number of hydroxybenzoic acid/cyclic carboximide co-crystals is reported, including polymorphic and variable stoichiometry co-crystals. In the cases where co-crystals did not form, the combinations are shown invariably to result in eutectics. The presence or absence and geometric disposition of hydroxyl functionality on benzoic acid is thus found to drive the formation of co- crystals or eutectics for the studied carboxylic acid/imide combinations.

Reduction in DNA topoisomerase I level affects growth, phenotype and nucleoid architecture of Mycobacterium smegmatis

The steady-state negative supercoiling of eubacterial genomes is maintained by the action of DNA topoisomerases. Topoisomerase distribution varies in different species of mycobacteria. While Mycobacterium tuberculosis (Mtb) contains a single type I (Topol) and a single type II (Gyrase) enzyme, Mycobacterium smegmatis (Msm) and other members harbour additional relaxases. Topol is essential for Mtb survival. However, the necessity of Topol or other relaxases in Msm has not been investigated. To recognize the importance of Topol for growth, physiology and gene expression of Msm, we have developed a conditional knock-down strain of Topol in Msm. The Topol-depleted strain exhibited extremely slow growth and drastic changes in phenotypic characteristics. The cessation of growth indicates the essential requirement of the enzyme for the organism in spite of having additional DNA relaxation enzymes in the cell. Notably, the imbalance in Topol level led to the altered expression of topology modulatory proteins, resulting in a diffused nucleoid architecture. Proteomic and transcript analysis of the mutant indicated reduced expression of the genes involved in central metabolic pathways and core DNA transaction processes. RNA polymerase (RNAP) distribution on the transcription units was affected in the Topol-depleted cells, suggesting global alteration in transcription. The study thus highlights the essential requirement of Topol in the maintenance of cellular phenotype, growth characteristics and gene expression in mycobacteria. A decrease in Topol level led to altered RNAP occupancy and impaired transcription elongation, causing severe downstream effects.

Query Click and Text Similarity Graph for Query Suggestions

Query suggestion is an important feature of the search engine with the explosive and diverse growth of web contents. Different kind of suggestions like query, image, movies, music and book etc. are used every day. Various types of data sources are used for the suggestions. If we model the data into various kinds of graphs then we can build a general method for any suggestions. In this paper, we have proposed a general method for query suggestion by combining two graphs: (1) query click graph which captures the relationship between queries frequently clicked on common URLs and (2) query text similarity graph which finds the similarity between two queries using Jaccard similarity. The proposed method provides literally as well as semantically relevant queries for users' need. Simulation results show that the proposed algorithm outperforms heat diffusion method by providing more number of relevant queries. It can be used for recommendation tasks like query, image, and product suggestion.

Sound radiation from a perforated panel set in a baffle with a different perforation ratio

A finite flexible perforated panel set in a differently perforated rigid baffle is considered. The radiation efficiency from such a panel is derived using a 2-D wavenumber domain formulation. This generalization is later used to represent a more practical case of a perforated panel fixed in an unperforated baffle. The perforations are in the form of an array of uniformly distributed circular holes. A complex impedance model for the holes available in the literature is used. An averaged fluid particle velocity is derived using the continuity equation and the surface pressure is derived using an appropriate momentum equation. The discontinuity in the perforate impedance (due to different hole dimensions or perforation ratio) at the panel-baffle interface is carefully taken into account. It is found that there exists a `coupling' of different wavenumbers of the spatially mean fluid particle velocity field. The change in the resonance frequencies and the modeshapes of the panel due to the perforations is taken into account using the Receptance method. Analytical expressions for the radiated power and radiation efficiency are derived in an integral form and numerical results are presented. Several comparisons are made to understand the radiation efficiency curves. Since both the resistive and reactive components of the hole impedance are taken into account, the model is directly applicable to micro-perforated panels also. (C) 2016 Elsevier Ltd. All rights reserved.