SYNTHESIS AND IN-VITRO STUDY OF NOVEL (Z)-1-BENZHYDRYL-4-CINNAMYLPIPERAZINE DERIVATIVES AS POTENTIAL ANTICANCER AGENTS
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2015, Vol 7, Issue 1
Abstract
Objective: The objective of this study was to synthesize Z- 1-benzhydryl-4-cinnamylpiperazines by novel stereo selective synthetic method and evaluation of their anticancer properties.Methods: A series of novel (Z)-1-benzhydryl-4-cinnamylpiperazine derivatives (9a-j) were synthesized, starting from benzophenones in six steps. Wittig condensation of appropriate benzyltriphenyl phosphonium halides with various 1-benzhydryl- 4-(2-ethanal) piperazines (3a-j), and column purification over silica gel afforded pure Z- 1-benzhydryl-4-cinnamylpiperazines.Results: The structures of newly synthesized compounds 9a-j were established by 1H & 13C NMR and mass spectral analysis. The anticancer potential (MTT assay) of synthesized compounds was tested against human cervical cancer (HeLa) and murine microglial (BV-2) cell lines. Results indicated that the most of the Z-derivatives exhibited moderate to good anticancer activity on both the cell lines over their E- antipodes.Conclusion: Compound 9i (cis- flunarizine) exhibited exceptionally superior activity against both HeLa and BV-2 cell lines with IC50 value of 13.23±3.51 µM and 23.1±4.12 µM respectively. Hence, this compound may be considered to be a potential lead molecule for further developmentÂ
Authors and Affiliations
S. Shivaprakash, K. R. Kiran, Latha Diwakar, Chandrasekara G Reddy
Keywords
Related Articles
- EP ID EP579229
- DOI -
- Views 84
- Downloads 0
PROTECTIVE EFFECT OF COMMIPHORA MUKUL GUM RESIN ON BRAIN IN STREPTOZOTOCIN-INDUCED DIABETIC RATS
Objective: The present study was undertaken to investigate the hypolipidemic activity of ethanolic extract of Commiphora mukul gum resin (EtCMGR) on the brain of streptozotocin (STZ) induced diabetic Wistar rats.Methods:...
ANTIBACTERIAL ACTIVITY OF OIL EXTRACT OF TRIGONA PROPOLIS
Objective: This research is aimed to determine antibacterial activity of some solvents of raw propolis extracts of Trigona sp from Sulawesi, Indonesia and compare it with antibacterial activities of ethanolic and aqueous...
ADSORPTION OF ERLOTINIB TO MULTIWALLED CARBON NANOTUBES
Objective: The objective of this research was to assess for the first time the adsorption of erlotinib (ERL) in three types of multi walled carbon nanotubes, as feasible alternative method to removal antineoplastic from...
SIMULTANEOUS ESTIMATION OF TELMISARTAN AND HYDROCHLOROTHIAZIDE BY DERIVATIVE SPECTROSCOPY
Objective: The objective of this investigation is to present the simple and sensitive method for the analysis of Telmisartan and Hydrochlorothiazide and apply the proposed method for the analysis of said drugs in pharmac...
HIPPOPHAE SALICIFOLIA D DON- A PLANT WITH MULTIFARIOUS BENEFITS
Hippophae salicifolia (commonly known as Seabuckthorn) can be regarded as a rich natural source of multivitamins. High amounts of vitamins A, B1, B12, E, K and polyphenols account for its vast nutraceutical properties. S...