Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds were synthesized and characterized by successfully by ART-FTIR, NMR and ESI- Ms. Assessed for their cytotoxic activity against human colon adenocarcinoma MCF-7 (IC50, I=105.15, II=60.00, III=54.11, IV=56.57, vorinostat=28.41) and hepatoblastoma HepG2 (IC50, I=63.91, II=135.18, III=118.85, IV=51.46, vorinostat=37.50). Most of them exhibited potent HDAC inhibitory activity and significant cytotoxicity. Conclusions: The synthesized compounds (I, II, III and IV) showed cytotoxicity toward MCF-7 and HepG2 cancer cell lines and their docking analysis provided a preliminary indication that they are viable [HDAC6] candidates.
In this work the strain energy of tetrahedrane and its nitrogen substituted molecules were calculated by isodesmic reaction method according to DFT quantum chemical fashion, the used basis set was 6-31G/B3-LYP, in addition all structures were optimized by RM1 semi-empirical method. From the obtained data we estimate an empirical equation connect between strain energy of the molecule with charge functions represented by dipole moment of the molecule plus accumulated charge density involved within the tetrahedron frame plus the number of nitrogen atoms. The results indicate the charge spreading factors by polarization and processes are the most important factors in decreasing the strain energy.
Cephalexin and its derivatives are commonly utilized in the pharmaceutical and medicinal industry due to their biological and pharmaceutical activities, including anti-microbial, anti-cancer, anti-bacterial, and herbicidal activities as well as possessing high palatability and being useful for skin and joint infections. Interestingly, some organic drugs, including cephalexin, which exhibit toxicological and pharmacological properties, can be administered in forms of metal complexes. Many researchers have synthesized organic ligands derived from cephalexin in forms of Schiff bases and azo compounds which exhibited higher biological and medicinal properties when compared to cephalexin alone. One of the important features that make Schiff base
... Show MoreThis study was conducted in a lath house, Dept of Hort. and Landscape, College of Agricultural Engineering Sciences, Univ. During the 2021 growing season, Baghdad will investigate the influence of organic and Biological fertilizers on three Citrus rootstocks' growth and leaf mineral content. The first factor is the addition of liquid organic fertilizers Vit-Org (O) at three levels without addition (O0), soil addition at 10 ml.L-1 (O10) and soil addition at 20 ml.L-1 (O20). The second factor is the addition of nitrogen-fixing bacteria without addition (N1), add 30 ml.Transplant-1 of Azotobacter chroococcum (N2) and add 30 ml.Transplant-1 of Azospirillum brasilemse (N3). The third factor is three citrus rootstocks: sour orange (R1), R
... Show MoreThe results of studying the effects of M. anisopiliae spores on mosquito, C. quinquefasciatus showed a biological effects represented by immature mortality. The mortality increased proportionally with the concentrations of fungal spores, which reached (at high concentration 2×1011 spores / ml), to 86.6, 56.6% in first and late instar larvae, respectively. An important to mention that cumulative death rate was significantly associated with the time, which reached to 56% at 7 day after treatment. In addition, M. anisopiliae had a long period permanence in aquatic habitats; in which the residual effects stay 30 days in aquatic habitats after treatment at laboratory conditions. Interestingly, the long period exposure of fungal spores (30 minut
... Show Moreأجريت هذه الدراسة في محافظة النجف بالعراق لتحليل عينات بيولوجية من المدخنين وغير المدخنين. تم استخدام العينات، بما في ذلك مصل الدم والبول والشعر والأظافر، كمؤشرات حيوية لتحديد تركيزات اليورانيوم (UC) ونظائره (238U، 235U، و234U). وباستخدام طريقة التعرض الطبيعي، تم استخدام كاشف المسار النووي (CR-39، المملكة المتحدة) لقياس تركيزات اليورانيوم في العينات. تم جمع خمسة وسبعين عينة من مصل الدم والبول والشعر والأظافر للمد
... Show MoreVariable-Length Subnet Masks (VLSM), often referred to as "subnetting a subnet", is used to maximize addressing efficiency. The network administrator is able to use a long mask on networks with few hosts, and a short mask on subnets with many hosts. This addressing scheme allows growth and does not involve wasting addresses. VLSM gives a way of subnetting a network with minimal loses of IP addresses for a specific range. Unfortunately, the network administrator has to perform several mathematical steps (or use charts) to get the required results from VLSM. In this paper, a simple graph simulator is proposed (using Visual Basic 6.0 Language) to perform all the required mathematical steps and to display the obtained required information (the
... Show MoreIn developing countries, individual students and researchers are not able to afford the high price of the subscription to the international publishers, like JSTOR, ELSEVIER,…; therefore the governments and/or universities of those countries aim to purchase one global subscription to the international publishers to provide their educational resources at a cheaper price, or even freely, to all students and researchers of those institutions. For realizing this concept, we must build a system that sits between the publishers and the users (students or researchers) and act as a gatekeeper and a director of information: this system must register its users and must have an adequate security to e
... Show MoreVariable-Length Subnet Masks (VLSM), often referred to as "subnetting a subnet", is used to maximize addressing efficiency. The network administrator is able to use a long mask on networks with few hosts, and a short mask on subnets with many hosts. This addressing scheme allows growth and does not involve wasting addresses. VLSM gives a way of subnetting a network with
minimal loses of IP addresses for a specific range. Unfortunately, the network administrator has to perform several mathematical steps (or use charts) to get the required results from VLSM. In this paper, a simple graph simulator is proposed (using Visual Basic 6.0 Language) to perform all the required mathematical steps and to display the obtained required informatio
An indoor spraying robot is built in this research to solve numerous challenges associated with manual spraying. The mechanical, hardware and essential technologies used are all detailed and designed. The proposed spraying robot's conceptual design is split into two parts: hardware and software. The mechanical design, manufacturing, electrical, and electronics systems are described in the hardware part, while the control of the robot is described in the software section. This robot's kinematic and dynamic models were developed using three links that move in the x, y, and z directions. The robot was then designed using SolidWorks software to compute each connection's deflection and maximum stresses. The characteristics of the stepper moto
... Show MoreTo obtain the approximate solution to Riccati matrix differential equations, a new variational iteration approach was proposed, which is suggested to improve the accuracy and increase the convergence rate of the approximate solutons to the exact solution. This technique was found to give very accurate results in a few number of iterations. In this paper, the modified approaches were derived to give modified solutions of proposed and used and the convergence analysis to the exact solution of the derived sequence of approximate solutions is also stated and proved. Two examples were also solved, which shows the reliability and applicability of the proposed approach.