ANTICANCER ACTIVITY AND MOLECULAR DOCKING OF SOME SYNTHESIZED 2-THIOHYDANTOIN DERIVATIVES
Journal Title: WORLD JOURNAL PHARMACY AND PHARMACEUTICAL SCIENCE - Year 2017, Vol 6, Issue 11
Abstract
Objective: the present work is designed for synthesis of a series of novel 2- thiohydantoin derivatives, description of the electron impact (EI) ionization mass spectral fragmentation patterns and evaluation of them against human breast cancer cells (MCF-7) and human prostate cancer cells (PC-3). Methods: A series of novel 3-[(2,5-dihydroxybenzylidene)amino]-2-thiohydantoin derivatives have been synthesized. The structures of the synthesized compounds were characterized by spectroscopic methods such as IR, HNMR, 13CNMR, mass spectroscopy and elemental analysis. The anti-tumor activity of the new compounds were evaluated against human breast cancer cells (MCF-7) and human prostate cancer cells (PC-3). Molecular docking also evaluated. Results: The spectroscopic data clearly confirmed the structure of the newly synthesized compounds. The anticancer activity and molecular docking for the compounds were evaluated. Among the tested compounds 3 and 7 exhibited the highest activity. Conclusion: 2-thiohydantoin derivatives containing (2,3-dihydroxybenzylidene)amino substituent were synthesized. The synthesized compounds exhibited moderate anticancer activities. On docking study, the most favorable interaction between the synthesized compounds and the protein receptor (3hb5) were with compounds 6 and 2.
Authors and Affiliations
Maha El-Ashry
ROLE OF PROPHYLACTIC ANTIBIOTICS IN PREVENTING SURGICAL SITE INFECTION
Background: Surgical site infections (SSIs) account for 14-16% of the estimated 2 million nosocomial infections affecting hospitalized patients in the United States. Internationally, the frequency of SSI is difficult to...
SYNTHESIS, STRUCTURAL CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF SOME NEW PYRROLIDINE DERIVATIVES
2-naphthyl chalcones where prepared by using Claisen-Schmidt condensation. In addition, Schiff bases were produced by condensation of benzyl amine with substituted benzaldehyde, adding the latter to the chalcones by 1,3-...
DEVELOPMENT AND VALIDATION OF A UPLC METHOD FOR SIMULTANEOUS QUANTIFICATION OF DICLOFENAC POTASSIUM AND CHLORZOXAZONE IN THEIR BINARY MIXTURES AND PHARMACEUTICAL FORMULATION
A simple, precise, accurate and rapid isocratic reverse phase Ultra high performance liquid chromatographic method was developed for simultaneous determination of diclofenac potassium and chlorzoxazone in binary mixture...
THE EFFECTS OF BUTYLATED HYDROXYL TOLUENE ON THE TOTAL ANTİOXİDANT STATUS/ TOTAL OXİDANT STRESS AND BİOCHEMİCAL PARAMETERS IN RATS
Background: The aim of this study was to investigate the effects of butylated hydroxyl toluene (BHT) in different doses on the serum total oxidant stress (TOS), antioxidant status (TAS) and biochemical parameters in rats...
EVALUATION OF THE EFFICACY OF CLEANING AND DISINFECTION IN BROILER FARMS BETWEEN REST PERIODS IN KHARTOUM STATE, SUDAN.
This study was carried out during the period from November 2015 to November 2017 in Bahri locality, Sudan. The objectives of the study were to determine the efficacy of cleaning and disinfection of broiler farms between...