Design, Synthesis, Characterization of Geminal Bisphosphonates and Bioactivity Evaluation

Cancer is a deadly disease evading all human efforts to understand its etiology, prevention, and cure. In cancer, chronic myelogenous leukemia is one type. It is also known as chronic myeloid leukemia. It is a malignant cancer of the myeloid line of cells in the bone marrow that results in the uncontrolled growth of white blood cells in the bone marrow, bloodstream, and body tissues. Colorectal cancer is another type of cancer that occurs in the colon or rectum. Sometimes it is called colon cancer. Management of these cancers is highly difficult. In persuasion of our goal to synthesize cancer active compounds, the author accomplished the synthesis of substituted amino methylene bisphosphonates (3a-j) and studied their antitumor activity. © 2020 Author(s)

Synthesis and Cytotoxic Activity of Various alkyl 2-{di[(diethoxy phosphoryl) methyl]amino}ester Derivatives

We have been synthesized simple, efficient various alkyl 2-{di[(diethoxy phosphoryl) methyl]amino}ester derivatives by reacting amino acid esters 1(a-j), paraformaldehyde and two molar equivalents of diethyl hydrogenphosphonate (2) in tetrahydrofuran at 55-65 °C for 10 hrs. All the compounds 3(a-j) were assessed for cytotoxicity against some important types of human chronic myeloid leukemia cells (K-562) and human colon carcinoma cells (Colo-205) along with noncancerous human embryonic kidney cells (HEK-293). © 2020 Author(s)

Trust Based Participant Driven Privacy Control in Participatory Sensing

Widespread use of sensors and multisensory personal devices generate a lot of personal information. Sharing this information with others could help in various ways. However, this information may be misused when shared with all. Sharing of information between trusted parties overcomes this problem. This paper describes a model to share information based on interactions and opinions to build trust among peers. It also considers institutional and other controls, which influence the behaviour of the peers. The trust and control build confidence. The computed confidence bespeaks whether to reveal information or not thereby increasing trusted cooperation among peers.Comment: 14 page

Ethnomedicinal Observations Among the Kondareddis of Khammam District, Andhra Pradesh, India

Ethnomedicinal information of Kondareddis has been collected from Khammam district of Andhra Pradesh, India during 2006-2008. A total of 40 plant species belonging to 39 genera and 31 families were used in traditional medicine to heal different diseases. The present work is an attempt to identify and conserve the medicinal plants in Khammam district. The study shows a high degree of ethnobotanical novelty and the use of plants among the Kondareddis reflects the revival of interest in traditional folk culture

Node activity based trust and reputation estimation approach for secure and QoS routing in MANET

Achieving safe and secure communication in MANETs is a key challenge due to its dynamic nature. A number of security studies disclose that reputation management systems are able to be effectual with less overhead. The reputation of a node is calculated by using automated assessment algorithms depend on predefined trust scheme. This paper proposes a Node Activity-based Trust and Reputation estimation (NA-TRE) approach for the security and QoS routing in MANET. NA-TRE aims to find trust estimation and reputation of a node. The NA-TRE approach monitors the activity changes, packet forwarding or dropping in a node to find the status of the node. The various activities of a node like Normal State (NS), Resource Limitation State (RS) and Malicious State (MS) are monitored. This status of a node is helpful in computing trust and reputation. In this paper NA-TRE approach compared with existing protocols AODV, FACE and TMS to evaluate the efficiency of MANET. The experiment results show that 20% increasing of throughput, 10% decrease of overhead and end to end delay

Changes in the ducts of the glands of the hard palate in reverse smokers

Three hundred fifty-nine cases of stomatitis nicotina were studied in reverse smokers of home made chuttas. One hundred thirty-five biopsies of papular unbilicated lesions of stomatitis nicotina were studied histopathologically. The biopsies were chosen after toluidine blue staining. Mild dysplastic to severe dysplastic changes were seen around the openings of the ducts of the glands. There were three cases of microinvasive carcinoma in the one hundred thirty-five biopsies. Cystic dilatation of the ducts, due to obstruction of the ducts by keratotic plugging, was not seen in stomatitis nicotina lesions but was seen in elderly women who had smoked reverse for more than 4 to 5 decades. The ducts of the glands could probably form a portal of entry for the tobacco pyrolytic products which may act as carcinogenics

NOVEL PYRAZOLINES: SYNTHESIS AND EVALUATION OF THEIR DERIVATIVES WITH ANTICANCER AND ANTI-INFLAMMATORY ACTIVITIES

Objective: Synthesis of novel pyrazolines (P2-P4 & P7-P9) from the chalcones (C2-C10) obtained by condensing different aldehydes with 2-acetyl- 5-bromothiophene and evaluates them for in vitro anticancer and anti-inflammatory activities.Methods: The synthesized pyrazolines and chalcones were screened for anticancer activity against human breast cancer cell lines-MCF-7 and MDA-MB-468 in the range of 100 nm to 100 µm. Inhibition of bovine albumin denaturation and heat-induced hemolysis in vitro methods were followed to screen for anti-inflammatory activity. The structures of synthesized compounds were confirmed based on the IR, 1H NMR and mass spectral data.Results: Among the synthesized compounds, methoxy trisubstituted pyrazoline derivative (P6) exhibited an interesting profile of anticancer activity against MCF-7 cell line with GI50<0.1 μ M. similar to that of the standard drug doxorubicin. Compounds C8, P8, P3 have moderate anti-inflammatory activity in bovine denaturation and heat induced hemolytic method.Conclusion: Novel pyrazolines and chalcones were synthesized and evaluated for anticancer and anti-inflammatory activity. The methoxy containing compounds one of which P6 found to be active against MCF-7 breast cancer cell line. The chloro-substituted compounds found to show anti-inflammatory activity.Â

PPARs in Alveolar Macrophage Biology

PPARs, most notably PPAR-γ, play a crucial role in regulating the activation of alveolar macrophages, which in turn occupy a pivotal place in the immune response to pathogens and particulates drawn in with inspired air. In this review, we describe the dual role of the alveolar macrophage as both a first-line defender through its phagocytotic activity and a regulator of the immune response. Depending on its state of activation, the alveolar macrophage may either enhance or suppress different aspects of immune function in the lung. We then review the role of PPAR-γ and its ligands in deactivating alveolar macrophages—thus limiting the inflammatory response that, if unchecked, could threaten the essential respiratory function of the alveolus—while upregulating the cell's phagocytotic activity. Finally, we examine the role that inadequate or inappropriate PPAR-γ responses play in specific lung diseases

Synthesis and Antimicrobial Activity of 3-[(4-Substituted) (2-oxo-1,3-oxazolidin-3-yl) phosphoryl]- 1,3-oxazolidin-2-ones

3-[(4-Substituted) (2-oxo-1,3-oxazolidin-3-yl)-phosphoryl]-1,3-oxazolidin-2-ones (4a–j) were synthesized through a two-step process. Bis-(2-oxo-1,3-oxazolidin-3-yl)-phosphonic chloride (2) prepared by the reaction of two moles of oxazolidin-2-one (1) with phosphorus oxychloride in dry tetrahydrofuran in the presence of triethylamine and treatment with various heterocyclic aromatic and aliphatic amines under the same experimental conditions afforded the title compounds (4a–j). They were characterized by elemental analysis, IR,NMR(1H, 13Cand 31P) and mass spectroscopy. Their antimicrobial activities were also evaluated.Keywords: 3-[(4-Substituted) (2-oxo-1,3-oxazolidin-3-yl)-phosphoryl]-1,3-oxazolidin-2-ones, oxazolidin-2-one, bis-(2-oxo-1,3-oxazolidin-3-yl)-phosphonic chloride, antimicrobial activity, spectral studie