Synthesis and biological evaluation of some new pyrimidine bearing 2,5-disubstituted 1,3,4-oxadiazole derivatives as cytotoxic agents

2016 ◽  
Vol 42 (2) ◽  
Author(s):  
Betül Kaya ◽  
Zafer Asım Kaplancıklı ◽  
Leyla Yurttaş ◽  
Gülşen Akalın Çiftçi
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
Phenacyl Bromide ◽  
Cytotoxic Activities ◽  
Pyridine Moiety ◽  
Oxadiazole Derivatives ◽  
Ft Ir ◽  
New Compounds ◽  
Synthesis And Biological Evaluation

AbstractObjective:As a result of adverse effects including drug-resistance, toxicity and low bioavailability, there has been a crucial need for novel anticancer agents. In this present study, some novel 2,5-disubstituted 1,3,4-oxadiazole derivatives bearing pyridine moiety were synthesized and their potential cytotoxic activities were examined.Materials and methods:A series of seven new compounds of 2-[(5-(3-(pyrimidin-2-yl)thio)propyl)-1,3,4-oxadiazol-2-yl)thio)]-1-(4-substituted)ethan-1-one derivatives were synthesized by reacting 5-[(3-(pyrimidin-2-yl)thio)propyl]-1,3,4-oxadiazole-2-thiol and 4-substituted phenacyl bromide derivatives in acetone with potassium carbonate. The structures of the obtained compounds were elucidated using FT-IR,Results:Among the tested compounds, compoundConclusions:It was determined that some of synthesized compounds had considerable anticancer activity against the A549 cell lines. Compound

Synthesis and Biological Evaluation of Chalcones Possessing Ring Activating Groups as Potent of Anticancer Agents

2017 ◽  
Vol 73 ◽  
pp. 1-8
Author(s):  
Mahammadali M. Khanusiya ◽  
Zakirhusen M. Gadhawala
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
Breast Adenocarcinoma ◽  
Aryl Ring ◽  
Vero Cell Line ◽  
Human Prostate Carcinoma ◽  
Potential Therapeutic Application ◽  
Ft Ir ◽  
Synthesis And Biological Evaluation

Some novel anticancer agents based on chalcone scaffold were synthesized with potential therapeutic application for many types of cancer. Hydroxy and methoxy substitution on aryl ring of chalcone, depending upon positions in aryl ring influence anticancer and other activities. These chalcone molecules were evaluated for their invitro cytotoxic activity against five cancer cell lines including human chronic myelogenus-leukemia K-562, human breast adenocarcinoma MCF-7, human prostate carcinoma DU-145, human lung adenocarcinoma A-549 and normal VERO cell line. Most of the compounds being active cytotoxic agents and were shown to be non-toxic to normal cells. The synthesized compounds were characterized by means of their FT-IR, MASS and 1HNMR spectral study.

scholarly journals Synthesis and Biological Evaluation of New N-Acyl-α-amino Ketones and 1,3-Oxazoles Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 5019
Author(s):  
Theodora-Venera Apostol ◽  
Luminita Gabriela Marutescu ◽  
Constantin Draghici ◽  
Laura-Ileana Socea ◽  
Octavian Tudorel Olaru ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Large Family ◽  
Biological Evaluation ◽  
Reversed Phase ◽  
Bioactive Substances ◽  
Nmr Data ◽  
In Silico Studies ◽  
Ft Ir ◽  
New Compounds ◽  
Synthesis And Biological Evaluation

In order to develop novel bioactive substances with potent activities, some new valine-derived compounds incorporating a 4-(phenylsulfonyl)phenyl fragment, namely, acyclic precursors from N-acyl-α-amino acids and N-acyl-α-amino ketones classes, and heterocycles from the large family of 1,3-oxazole-based compounds, were synthesized. The structures of the new compounds were established using elemental analysis and spectral (UV-Vis, FT-IR, MS, NMR) data, and their purity was checked by reversed-phase HPLC. The newly synthesized compounds were evaluated for their antimicrobial and antibiofilm activities, for toxicity on D. magna, and by in silico studies regarding their potential mechanism of action and toxicity. The 2-aza-3-isopropyl-1-[4-(phenylsulfonyl)phenyl]-1,4-butanedione 4b bearing a p-tolyl group in 4-position exhibited the best antibacterial activity against the planktonic growth of both Gram-positive and Gram-negative strains, while the N-acyl-α-amino acid 2 and 1,3-oxazol-5(4H)-one 3 inhibited the Enterococcus faecium biofilms. Despite not all newly synthesized compounds showing significant biological activity, the general scaffold allows several future optimizations for obtaining better novel antimicrobial agents by the introduction of various substituents on the phenyl moiety at position 5 of the 1,3-oxazole nucleus.

scholarly journals Synthesis and biological evaluation of novel 1,3,4-thiadiazole derivatives as possible anticancer agents

2020 ◽  
Vol 70 (4) ◽  
pp. 499-513
Author(s):  
Ulviye Acar Çevik ◽  
Derya Osmaniye ◽  
Serkan Levent ◽  
Begüm Nurpelin Sağlik ◽  
Betül Kaya Çavuşoğlu ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Mouse Embryonic Fibroblast ◽  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Anticancer Activities ◽  
Nih3t3 Cell Line ◽  
New Compounds ◽  
Mcf 7

AbstractThe synthesis of new N-(5-substituted-1,3,4-thiadiazol-2-yl)-2-[(5-(substituted amino)-1,3,4-thiadiazol-2-yl)thio]acetamide derivatives and investigation of their anticancer activities were the aims of this work. All the new compounds’ structures were elucidated by elemental analyses, IR, 1H NMR, 13C NMR and MS spectral data. Anticancer activity studies of the compounds were evaluated against MCF-7 and A549 tumor cell lines. In addition, with the purpose of determining the selectivity of cytotoxic activities, the most active compound was screened against a noncancer NIH3T3 cell line (mouse embryonic fibroblast cells). Among the tested compounds, compound 4y (N-(5-ethyl-1,3,4-thiadiazol-2-yl)-2-((5-(p-tolylamino)-1,3,4-thiadiazol-2-yl)thio)acetamide), showed promising cytotoxic activity against MCF7 cancer cell with an IC50value of 0.084 ± 0.020 mmol L−1 and against A549 cancer cell with IC50 value of 0.034 ± 0.008 mmol L−1, compared with cisplatin. The aromatase inhibitory activity was evaluated for compound 4y on MCF-7 cell line showing promising activity with IC50 of 0.062 ± 0.004 mmol L−1.

scholarly journals Design, synthesis and biological evaluation of novel 1,3-diarylpyrazoles as cyclooxygenase inhibitors, antiplatelet and anticancer agents

MedChemComm ◽  
2018 ◽  
Vol 9 (5) ◽  
pp. 795-811 ◽  
Author(s):  
Nazan Inceler ◽  
Yesim Ozkan ◽  
Nilufer Nermin Turan ◽  
Deniz Cansen Kahraman ◽  
Rengul Cetin-Atalay ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Cyclooxygenase Inhibitors ◽  
Cytotoxic Activities ◽  
Design Synthesis ◽  
Cox 2 ◽  
Synthesis And Biological Evaluation ◽  
Cox 1

(E)-3-[3-(Pyridin-3/4-yl)-1-(phenyl/sulfonylmethylphenyl)-1H-pyrazol-4-yl]acrylamides were synthesized and their COX-1 and COX-2 inhibitory, antiplatelet and cytotoxic activities were evaluated.

Design, synthesis and biological evaluation of novel podophyllotoxin derivatives bearing 4β-disulfide/trisulfide bond as cytotoxic agents

RSC Advances ◽  
2015 ◽  
Vol 5 (125) ◽  
pp. 103172-103183 ◽  
Author(s):  
Shi-Jun Zhu ◽  
Hua-Zhou Ying ◽  
Yan Wu ◽  
Ni Qiu ◽  
Tao Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Kb Cells ◽  
Design Synthesis ◽  
Podophyllotoxin Derivatives ◽  
Synthesis And Biological Evaluation

A novel series of podophyllotoxin derivatives bearing 4β-disulfide/trisulfide were designed, synthesized and biologically evaluated for their cytotoxic activities against KB cells and KB/VCR cells.

scholarly journals Synthesis and Biological Evaluation of Novel Piperazine Containing Hydrazone Derivatives

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Betül Kaya ◽  
Yusuf Özkay ◽  
Halide Edip Temel ◽  
Zafer Asım Kaplancıklı
Keyword(s):  
Aromatic Aldehydes ◽  
Biological Evaluation ◽  
Standard Drug ◽  
H Nmr ◽  
Chemical Structures ◽  
Ft Ir ◽  
Inhibition Potency ◽  
New Compounds ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

Some hydrazone derivatives were synthesized and their potential anticholinesterase activities were examined. A series of eleven new compounds of N′-(2,4-disubstitutedbenzylidene)-2-(4-(4-nitrophenyl)piperazin-1-yl)acetohydrazide derivatives were obtained via reaction of 2-[4-(4-nitrophenyl)piperazin-1-yl]acetohydrazide with aromatic aldehydes. The chemical structures of the compounds were enlightened by FT-IR,1H-NMR,13C-NMR, and HRMS (ESI) spectral data. The inhibition potency of the compounds3a–kagainst AChE and BuChE was measured and evaluated using a modification of Ellman’s spectrophotometric method. Among the tested compounds, compound3cwas assigned to be the most active derivative. Galantamine was used as a standard drug.

Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives as Anticancer Agents

2017 ◽  
Vol 14 (10) ◽  
Author(s):  
Zahra Rezaei ◽  
Setareh Moghimi ◽  
Rezvan Javaheri ◽  
Mehdi Asadi ◽  
Mohammad Mahdavi ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation
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