GREEN SYNTHESIS OF PYRAZOLO [3,4]-PYRIMIDINE-THIONES USING IONIC LIQUID 2-METHYL-IMIDAZOLIUM-OXALATE AS POTENT EHRLICH ASCITES CARCINOMA RECEPTOR ANTAGONISTS

Objective: Pyrazolopyrimidines are heterocyclic molecules containing nitrogen as the main composition, and hence, they exhibit pharmacological efficacy. They are analogs of purines so that possessing wide applications in the field of medicinal chemistry. The main objective of this study is to synthesize different derivatives of pyrazole-pyrimidine classes by adopting simple methodology as well as by employing green chemistry. The purpose of the synthesis of these molecules is to study the antitumor activity against Ehrlich ascites carcinoma (EAC) cell lines. Methods: After literature studies, it makes us to involve in the research of synthetic organic chemistry, especially to synthesize new compounds of pyrazolopyrimidines. We are reported solvent-free synthesis of pyrazolo [3,4-d]-pyrimidine-thiones through ethyl acetoacetate, hydrazine hydrate, thiourea, and different benzaldehydes. An ionic liquid 2-methyl-imidazolium-oxalate catalyzed the reactions under ultrasonication bath. Both conventional and ultrasonic methods were employed and comparison studies have been made. It was found that ultrasonic method completed the reaction quicker than the conventional method. All the synthesized compounds were confirmed their structures by 1HNMR, Fourier transform infrared, 13C-NMR, and elemental analysis spectra. The compounds were tested for in vitro anticancer activity against EAC cell lines. Most compounds revealed significant anticancer activity relative to doxorubicin as a positive control with inhibitory concentration (IC50) values. Results: Ultrasonication method is a simple method under which all the reactions were completed at faster time (<7 min) compared to the convention method. Among eight molecules, 8a and 8d completed the reactions at a faster rate. We reported IC50 values of all the molecules, in which 8e and 8g were exhibited excellent potency against EAC cell lines at different concentrations . Conclusions: Ultrasonication method is an excellent method for the organic synthesis. We are herein reported that under this method, all the reactions are completed within 7 min. Hence, it is superior method than the conventional method. All synthesized molecules have shown good inhibitor potency against EAC cell lines. Among them, two molecules 8e and 8g have shown excellent inhibitor potency

Mass function and dynamical study of the open clusters Berkeley 24 and Czernik 27

We present a $UBVI$ photometric study of the open clusters Berkeley 24 (Be 24) and Czernik 27 (Cz 27). The radii of the clusters are determined as 2\farcm7 and 2\farcm3 for Be 24 and Cz 27, respectively. We use the Gaia Data Release 2 (GDR2) catalogue to estimate the mean proper motions for the clusters. We found the mean proper motion of Be 24 as $0.35\pm0.06$ mas yr$^{-1}$ and $1.20\pm0.08$ mas yr$^{-1}$ in right ascension and declination for Be 24 and $-0.52\pm0.05$ mas yr$^{-1}$ and $-1.30\pm0.05$ mas yr$^{-1}$ for Cz 27. We used probable cluster members selected from proper motion data for the estimation of fundamental parameters. We infer reddenings $E(B-V)$ = $0.45\pm0.05$ mag and $0.15\pm0.05$ mag for the two clusters. Analysis of extinction curves towards the two clusters show that both have normal interstellar extinction laws in the optical as well as in the near-IR band. From the ultraviolet excess measurement, we derive metallicities of [Fe/H]= $-0.025\pm0.01$ dex and $-0.042\pm0.01$ dex for the clusters Be 24 and Cz 27, respectively. The distances, as determined from main sequence fitting, are $4.4\pm0.5$ kpc and $5.6\pm0.2$ kpc. The comparison of observed CMDs with $Z=0.01$ isochrones, leads to an age of $2.0\pm0.2$ Gyr and $0.6\pm0.1$ Gyr for Be 24 and Cz 27, respectively. In addition to this, we have also studied the mass function and dynamical state of these two clusters for the first time using probable cluster members. The mass function is derived after including the corrections for data incompleteness and field star contamination. Our analysis shows that both clusters are now dynamically relaxedComment: 16 pages including 8 tables. 22 figures. Accepted by MNRA

The dyad gene is required for progression through female meiosis in Arabidopsis

In higher plants the gametophyte consists of a gamete in association with a small number of haploid cells, specialized for sexual reproduction. The female gametophyte or embryo sac, is contained within the ovule and develops from a single cell, the megaspore which is formed by meiosis of the megaspore mother cell. The dyad mutant of Arabidopsis, described herein, represents a novel class among female sterile mutants in plants, dyad ovules contain two large cells in place of an embryo sac. The two cells represent the products of a single division of the megaspore mother cell followed by an arrest in further development of the megaspore. We addressed the question of whether the division of the megaspore mother cell in the mutant was meiotic or mitotic by examining the expression of two markers that are normally expressed in the megaspore mother cell during meiosis. Our observations indicate that in dyad the megaspore mother cell enters but fails to complete meiosis, arresting at the end of meiosis 1 in the majority of ovules, This was corroborated by a direct observation of chromosome segregation during division of the megaspore mother cell, showing that the division is a reductional and not an equational one. In a minority of dqad ovules, the megaspore mother cell does not divide. Pollen development and male fertility in the mutant is normal, as is the rest of the ovule that surrounds the female gametophyte. The embryo sac is also shown to have an influence on the nucellus in wild type. The dyad mutation therefore specifically affects a function that is required in the female germ cell precursor for meiosis. The identification and analysis of mutants specifically affecting female meiosis is an initial step in understanding the molecular mechanisms underlying early events in the pathway of female reproductive development

Simulation Model for Assessing Transient Performance of Capacitive Voltage Transformers

In determining the correct operation of relays of a protection scheme, proper representation of instrument transformers and their behavior in conditions where there can be transient is very critical. This paper presents a simulation model for assessing the transient performance of capacitive voltage transformers (CVTs). In order to test the validity of the developed model, four CVT operational conditions are considered using field data collected from one of the Nigerian electric utility 330/132/33 kV substations. The model simulation results revealed various configuration performance responses that could affect relay protection schemes to different degrees. As expected, the CVT responses showed that faults initiated at zero voltage crossing, which is the worst transient condition, produced transient voltage magnitude up to 40% of the nominal voltage while faults initiated at the crest produced minimum transient voltage magnitude. It is shown that the model developed for the selected instrument transformer yielded satisfactory results

Adaptive Load Frequency Control of Nigerian Hydrothermal System Using Unsupervised and Supervised Learning Neural Networks

This work presents a novel load frequency control design approach for a two-area power system that relies on unsupervised and supervised learning neural network structure. Central to this approach is the prediction of the load disturbance of each area at every minute interval that is uniquely assigned to a cluster via unsupervised learning process. The controller feedback gains corresponding to each cluster center are determined using modal control technique. Thereafter, supervised learning neural network (SLNN) is employed to learn the mapping between each cluster center and its feedback gains. A real time load disturbance in either or both areas activates the appropriate SLNN to generate the corresponding feedback gains. The effectiveness of the control framework is evaluated on the Nigerian hydrothermal system. Several far-reaching simulation results obtained from the test system are presented and discussed to highlight the advantages of the proposed approach