DESIGN SYNTHESIS OF NOVEL ACRIDINE TAGGED PYRAZOLE DERIVATIVES AS AURORA KINASE INHIBITORS

Objective: A series of novel synthesis of 5-Substituted-3-phenyl-4,5-dihydro-pyrazole-1-carbothioic acid [4-(9, 10-dihydro-acridin-9-yl)-phenyl]- amide (IV) were synthesized using standard procedures and evaluated for cytotoxic studies. Methods: 9-(4-Chloro-phenyl)-9 and 10-dihydro-acridine (I) were formed by cyclization of diphenylamine with substituted acids in the prescience of zinc chloride and synthesis of 5-substituted-3-phenyl-4, 5-dihydro-pyrazole-1-carbothioic acid amide (3) by the cyclization of different chalcones (II) and final compounds were synthesized by fusion of 5-substituted-3-phenyl-4, 5-dihydro-pyrazole-1-carbothioic acid amide (III) with 9-(4-Chloro-phenyl)-9, 10-dihydro-acridine (I) by microwave irradiation method. Characterization of synthesized compounds by infrared, 1H nuclear magnetic resonance (NMR), 13C NMR, and mass spectroscopic methods. Obtained compounds were evaluated for their cytotoxicity against human breast cancer cell lines (MCF/wt) by sulforhodamine-B assay. Docking studies with Aurora kinase protein were performed to elucidate the possible mechanistic insights of these novel acridine tagged pyrazole derivatives. Results: Moderate to good in vitro cytotoxic potentials of the newly synthesized molecules was reported against selected human breast cancer cell lines. Among the tested molecules, compound C6 showed good cytotoxic activity against MCF/wt (08.2±0.4 μM). The dock scores of the tested compounds were ranged between −8.926 and −5.139. Compound C6 which has been reported as the most effective cytotoxic agent among the series also reported the highest dock score of -8.926 and showed hydrogen bond interaction with GLU-211, LYS-162, and LYS-143. Ligand binding energy with protein suggested compound C6 has shown the highest binding energy of −86.32133 kcal/mol. Conclusion: The in vitro studies of the newly synthesized acridine tagged pyrazole derivatives reported considerable cytotoxic potentials against human breast cancer cell lines and structure-activity relationship studies to suggest that acridine tagged pyrazole derivatives with hydroxy group present on phenyl ring at fifth position of pyrazole ring could probably increase the cytotoxic potentials. With the reported bioactivities of these derivatives, further studies on the derivatization could elucidate the broader cytotoxic potentials

Knowledge and attitude of 2,000 parents (urban and rural - 1,000 each) with regard to avulsed permanent incisors and their emergency management, in and around Davangere

It is well recognized today that for long-term success, the management of traumatized teeth optimally should be carried out as soon as possible. Since, majority of traumatic injuries occur at home, the ultimate prognosis of an avulsed tooth may depend on knowledge of the treatment procedure, possessed by his or her parents. The purpose of this study was therefore to evaluate the parental knowledge and attitude regarding the emergency management of avulsed teeth in children (in Davangere - both urban and rural, 1,000 each)

Role of electronic energy loss on the magnetic properties Of Mg0.95Mn0.05Fe2O4 nanoparticles

Effects of 100 MeV Si7+ and Ni8+ ion irradiation on Mg-Mn ferrite nanoparticles have been studied. The bulk sample was synthesized using the solid-state reaction technique. For obtaining nanoparticles, the bulk sample was milled using high-energy ball mill for 12 h. The well-characterized nanoparticles having an average particle size of similar to 6 nm were irradiated with 100 MeV Si and Ni ions at various fluences in the range 5 x 10(12)-5 x 10(13) ions/cm(2) to see the effects of increasing electronic energy loss on their magnetic properties. The magnetization measurements performed on the 100 MeV Si ion irradiated nanoparticles sample revealed that the values of coercivity and the saturation magnetization have been enhanced about two times as compared to the unirradiated sample. It is explained on the basis that after irradiation by 100 MeV Si ions, the surface states pinning of domains is released which causes enhancement in the saturation magnetization and coercivity. On the other hand, the saturation magnetization decreases slightly after irradiation by Ni ions. The results have been explained on the basis of electronic energy loss dependence in the nanoparticles. (c) 2006 Elsevier B.V. All rights reserved.2481374

Expression of VP1 protein of serotype A and O of foot-and-mouth disease virus in transgenic sunnhemp plants and its immunogenicity for guinea pigs

Recently, transgenic plants expressing immunogenic proteins of foot-and-mouth disease virus (FMDV) have been used as oral or parenteral vaccines against foot-and-mouth disease (FMD). They exhibit advantages like cost effectiveness, absence of processing, thermostability, and easy oral application. FMDV VP1 protein of single serotype has been mostly used as immunogen. Here we report the development of a bivalent vaccine with tandem-linked VP1 proteins of two serotypes, A and O, present in transgenic forage crop Crotalaria juncea. The expression of the bivalent protein in the transgenic plants was confirmed by Western blot analysis. Guinea pig reacted to orally or parenterally applied vaccine by humoral as well as cell-mediated immune responses including serum antibodies and stimulated lymphocytes, respectively. The vaccine protected the animals against a challenge with the virus of serotype A as well as O. This is the first report on the development of a bivalent FMD vaccine using a forage crop

Role of interparticle interactions on the magnetic behavior of Mg0.95Mn0.05Fe2O4 ferrite nanoparticles

We present here a detailed investigation of the static and dynamic magnetic behavior of a Mg0.95Mn0.05Fe2O4 spinel ferrite nanoparticle system synthesized by high-energy ball milling of almost identical particle size distributions ( = 4.7, 5.1 and 6.0 +/- 0.6 nm). The samples were characterized by using x-ray diffraction, Mossbauer spectroscopy, dc magnetization and frequency dependent real. chi'(T) and imaginary chi ''(T) parts of ac susceptibility measurements. The zero-field-cooled (ZFC) and field-cooled (FC) magnetization have been recorded in a low field and show a behavior typical of superparamagnetic particles above a temperature of 185 +/- 5 K, which is further supported from the temperature dependent Mossbauer measurements. The fact that the blocking temperature calculated from the ZFC magnetization and Mossbauer data are almost similar gives a clear indication of the interparticle interactions among these nanoparticle systems. This is further supported from the FC magnetization curves, which are almost flat below a certain temperature (less than the blocking temperature), as compared with the monotonically increasing behavior characteristics of non-interacting superparamagnetic particles. A shift of the blocking temperature with increasing frequency was observed in the real. chi'(T) and imaginary. chi ''(T) parts of the ac susceptibility measurements. The analysis of the results shows that the data fit well with the Vogel-Fulcher law, whereas trials using the Neel -Brown and power law are unproductive. The role of magnetic interparticle interactions on the magnetic behavior, namely superparamagnetic relaxation time and magnetic anisotropy, are discussed.202

Magnetic study of Mg0.95Mn0.05Fe2O4 ferrite nanoparticles

The magnetic properties of Mg0.95Mn0.05Fe2O4 ferrite samples with an average particle size of similar to 6.0 +/- 0.6 nm have been studied using X-ray diffraction, Mossbauer spectroscopy, dc magnetization and frequency dependent real chi'(T) and imaginary chi'(T) parts of ac susceptibility measurements. A magnetic transition to an ordered state is observed at about 195 K from Mossbauer measurements. The zero-field-cooled (ZFC) and field-cooled (FC) magnetization have been recorded at low field and show the typical behavior of a small particle system. The ZFC curve displays a broad maximum at T-mean = 195 +/- 5 K, a temperature which depends upon the distribution of particle volumes in the sample. The FC curve was nearly flat below T-mean, as compared with monotonically increasing characteristics of non-interacting superparamagnetic systems indicating the existence of strong interactions among the nanoparticles. A frequency-dependent peak observcd in chi'(T) is well described by Vogel-Fulcher law, yielding a relaxation time tau(0) = 5.8 x 10(-12) s and an interaction parameter T-0 = 195 +/- 3 K. Such values show the strong interactions and rule out the possibility of spin-glass (SG) features among the nanoparticle system. On the other hand fitting with the Neel-Brown model and the power law yields an unphysical large value of tau(0) (similar to 6 x 10(-69) and 1.2 x 10(-22) s respectively). (c) 2006 Elsevier Ltd. All rights reserved.141420320

Growth kinetics and immune response of chimeric foot-and-mouth disease virus serotype `O' produced through replication competent mini genome of serotype Asia 1, 63/72, in BHK cell lines

Regular vaccinations with potent vaccine, in endemic countries and vaccination to live in non-endemic countries are the methods available to control foot-and-mouth disease. Selection of candidate vaccine strain is not only cumbersome but the candidate should grow well for high potency vaccine preparation. Alternative strategy is to generate an infectious cDNA of a cell culture-adapted virus and use the replicon for development of tailor-made vaccines. We produced a chimeric `O' virus in the backbone of Asia 1 and studied its characteristics. The chimeric virus showed high infectivity titre (>10(10)) in BHK 21 cell lines, revealed small plague morphology and there was no cross reactivity with antiserum against Asia I. The virus multiplies rapidly and reaches peak at 12 h post infection. The vaccine prepared with this virus elicited high antibody titres

The relationship between a primary maxillary incisor with a talon cusp and the permanent successor: A study of 57 cases

Background. Most reported cases of talon cusps in the primary dentition have been on the maxillary central incisors and. the permanent successors have remained unaffected. Four of the five reported cases on a maxillary lateral incisor, however, have been associated with a supernumerary permanent successor. Aim. This paper describes the relationship between the presence of talon cusps on a primary maxillary incisor, and the morphology and number of the permanent successors in a opulation of Chinese children.Design. The dental records of children diagnosed with a talon cusp on a primary incisor were retrieved for review. The diagnoses took place in a regional school dental clinic in Hong Kong between April 2002 and August 2005. Results. Fifty-eight primary maxillary incisors with talon cusps were found. When the central incisors were involved, 32 of the 35 (91.4%) underlying permanent successors were not found to be associated with any odontogenic abnormalities. When the lateral incisors were involved, however, 18 of the 23 cases (78.3%) showed odontogenic abnormalities, 14 of which were associated with supernumerary teeth. Conclusions. The present study shows that, when there is a talon cusp on a primary maxillary lateral incisor, a high proportion of the underlying permanent successors can be expected to exhibit odontogenic abnormalities. © 2007 BSPD, IAPD and Blackwell Publishing Ltd.link_to_subscribed_fulltex