The disease of cancer has been ranked second after cardiovascular diseases and plant-derived molecules have played an important role for the treatment of cancer. Nine cytotoxic plant-derived molecules such as vinblastine, vincristine, navelbine, etoposide, teniposide, taxol, taxotere, topotecan and irinotecan have been approved as anticancer drugs. Recently, epothilones are being emerging as future potential anti-tumor agents. However, targeted cancer therapy has now been rapidly expanding and small organic molecules are being exploited for this purpose. Amongst target specific small organic molecules, quinazoline was found as one of the most successful chemical class in cancer chemotherapy as three drugs namely Gefitinib, Erlotinib and Canertinib belong to this series. Now, quinazoline related chemical classes such as quinolines and naphthyridines are being exploited in cancer chemotherapy and a number of molecules such as compounds EKB-569 (52), HKI-272 (78) and SNS-595 (127a) are in different phases of clinical trials. This review presents the synthesis of quinolines and naphthyridines derivatives, screened for anticancer activity since year 2000. The synthesis of most potent derivatives in each prototype has been delineated. A brief structure activity relationship for each prototype has also been discussed. It has been observed that aniline group at C-4, aminoacrylamide substituents at C-6, cyano group at C-3 and alkoxy groups at C-7 in the quinoline ring play an important role for optimal activity. While aminopyrrolidine functionality at C-7, 2'-thiazolyl at N-1 and carboxy group at C-3 in 1,8-naphthyridine ring are essential for eliciting the cytotoxicity. This review would help the medicinal chemist to design and synthesize molecules for targeted cancer chemotherapy.
Laser has emerged as an adjunct in several treatment modalities in dentistry in the past few decades. This less invasive bladeless technique is bringing revolutionary outcomes in a plethora of periodontal treatment procedures as well. A unique ameliorative approach termed LANAP, described as laser-assisted new attachment procedure was developed by Gregg and McCarthy. In 1990 they introduced an innovative treatment for diseases of gums incorporating pulsed neodymium yttrium aluminum garnet (Nd: YAG) 1064 nm wavelength laser (PerioLase MVP7). The LANAP concept was endorsed by Yukna et al who conducted a study according to the protocol reinforced at the1996 world workshop in periodontics, which established specific histologic criteria to prove regeneration. Yukna's histological study found that regeneration of the periodontally compromised root could be achieved by Nd: YAG laser. LANAP facilitates refurbishing of new tissues from supporting structures of the periodontium wherein the unhealthy surface of the roots exhibit pristine attachments in human beings. This paper is a review providing a detailed report of LANAP from its inception to recent advances.
In this paper, finite element approach using two-dimensional unsteady state problem has been developed to study radial and angular calcium diffusion problem in neurons. Calcium is responsible messenger for transmitting information in communication process between neurons. The most important Ca 2+ binding proteins for the dynamics of Ca 2+ is itself buffer and other physiological parameters are located in Ca 2+ stores. In this study, the model incorporates the physiological parameters like diffusion coefficient, receptors, exogenous buffers etc. Appropriate boundary conditions have been framed in view of the physiological conditions. Computer simulations in MATLAB 7.11 are employed to investigate mathematical models of reaction–diffusion equation, the details of the implementation can heavily affect the numerical solutions and, thus, the outcome simulated on Core(TM) i3 CPU M 330 @ 2.13 GHz processing speed and 3 GB memory.
The study of calcium diffusion in neuron cells has gained interest among research workers during the last two decades, due to its wide variety of roles in human body like muscle contraction, secretion, metabolism, signal transduction etc. Na[Formula: see text] is the first ion that comes in the hierarchy of ions affecting cytosolic Ca[Formula: see text] concentration. This Na[Formula: see text] ion helps in intracellular Ca[Formula: see text] regulation in cytosol via Na[Formula: see text]/Ca[Formula: see text] exchanger protein (NCX protein). Most of the theoretical investigations on calcium diffusion in neuron cells have been carried out for one and two dimensional cases by various research workers and that too by incorporating a point source of influx. In order to have more realistic study the more details of geometry, microstructure and physiological parameters need to be incorporated in the models. In view of above a three dimensional unsteady state model of Calcium dynamics in a neuron cell has been developed. Apart from the point source, the line and surface sources of an influx of Ca[Formula: see text]as well as the Na[Formula: see text]/Ca[Formula: see text] exchanger, have been incorporated in the model. Appropriate initial and boundary conditions have been framed. The region is discretized using three dimensional circular sectoral elements. Variational finite element method has been employed to obtain the solution. The numerical results have been computed to study effect of Na[Formula: see text]/Ca[Formula: see text] exchanger, point source, line source and surface source of an influx on Ca[Formula: see text] distribution in a neuron cell.
A new series of functionalized amino acid derivatives N-substituted 1-N-(tert-butoxycarbonyl)-2,2-dimethyl-4-phenyl-5-oxazolidine carboxamide (1-17) and 1-N-substituted-3-amino-2-hydroxy-3-phenylpropane-1-carboxamide (18-34) were synthesized and evaluated for their in vitro cytotoxicity against human cancer cell lines. Compound 6 has shown interesting cytotoxicity (IC 50 ¼ 5.67 mm) in ovarian cancer, while compound 10 exhibited promising cytotoxicity in ovarian (IC 50 ¼ 6.1 mm) and oral (IC 50 ¼ 4.17 mm) cancers. These compounds could be of use in designing new anti-cancer agents.
Calcium is known to play an important role in various circular functions like muscle contraction, secretion, metabolism etc. The study of calcium dynamics in various cells like neuron cell is crucial for understanding the functions, processes involved in the cell. A number of investigations on calcium diffusion in a neuron cell are reported for one dimensional case. But very few attempts are reported in the literature for the study of calcium diffusion in a neuron cell for two and three dimensional cases. In this paper an attempts has been made to develop a model of calcium concentration variation in a neuron cell for a two dimensional unsteady state case. The model is obtained in the form of initial boundary value problem involving in partial differential equation along with appropriate initial and boundary conditions. A model incorporates the effect of buffer, diffusion coefficients, flux etc. analytical solutions has been obtained using Laplace transform. The results have been computed and use to study relationships among various parameters.
Dendritic spine plays an important role in calcium regulation in a neuron cell. It serves as a storage site for synaptic strength and receives input from a single synapse of axon. In order to understand the calcium dynamics in a neuron cell, it is crucial to understand the calcium dynamics in dendritic spines. In this paper, an attempt has been made to study the calcium dynamics due to the exogenous buffers, in dendritic spines with the help of a sectional model. The compartments of dendritic spines are discretized using triangular elements. Appropriate boundary conditions have been framed. Finite element method has been employed to obtain the solution in the region for a two-dimensional unsteady state case. MATLAB 7.11 is used for simulation of the problem and numerical computations. The numerical results have been used to study the effect of exogenous buffers on calcium distribution in dendritic spines.
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