scholarly journals Chloroquine Urea Derivatives: Synthesis and Antitumor Activity in Vitro

2018 ◽  
Vol 68 (4) ◽  
pp. 471-483 ◽  
Author(s):  
Kristina Pavić ◽  
Zrinka Rajić ◽  
Zvonimir Mlinarić ◽  
Lidija Uzelac ◽  
Marijeta Kralj ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Urea Derivatives ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Lead Compounds ◽  
Insight Into

Abstract In the current paper, we describe the design, synthesis and antiproliferative screening of novel chloroquine derivatives with a quinoline core linked to a hydroxy or halogen amine through a flexible aminobutyl chain and urea spacer. Synthetic pathway leading to chloroquine urea derivatives 4-10 includes two crucial steps: i) synthesis of chloroquine benzotriazolide 3 and ii) formation of urea derivatives through the reaction of compound 3 with the corresponding amine. Testing of antiproliferative activity against four human cancer cell lines revealed that chloroquine urea derivatives 9 and 10 with aromatic moieties show activity at micromolar concentrations. Therefore, these molecules represent interesting lead compounds that might provide an insight into the design of new anticancer agents.

scholarly journals Design, Synthesis, and Cytotoxic Evaluation of Novel Lupane Triterpenoid Derived Hydroxamates

2020 ◽  
Vol 15 (6) ◽  
pp. 1934578X2093196
Author(s):  
Dang Thi Tuyet Anh ◽  
Dinh Thi Cuc ◽  
Le Nhat Thuy Giang ◽  
Nguyen Thi Hien ◽  
Vu Ngoc Doan ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Lupane Triterpenoids ◽  
Lead Compounds ◽  
Diphenyltetrazolium Bromide ◽  
Derivatives Of

A series of new hydroxamate derivatives of lupane triterpenoids has been designed and successfully synthesized. The synthesized compounds were evaluated for their in vitro antitumor activity using the 3-[4,5-dimethylthiazol-2-yl]−2,5-diphenyltetrazolium bromide-based assay against the human cancer cell lines KB and HepG2. Most of these derivatives possess at least moderate cytotoxic activity and the hydroxamate derivative compounds 3c, 3e, 7a, and 15b could be lead compounds for further optimization to develop novel anticancer agents.

scholarly journals Design, synthesis and biological evaluation of imidazopyridine–propenone conjugates as potent tubulin inhibitors

MedChemComm ◽  
2017 ◽  
Vol 8 (5) ◽  
pp. 1000-1006 ◽  
Author(s):  
Ibrahim Bin Sayeed ◽  
V. Lakshma Nayak ◽  
Mohd Adil Shareef ◽  
Neeraj Kumar Chouhan ◽  
Ahmed Kamal
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Tubulin Inhibitors ◽  
Synthesis And Biological Evaluation

A library of imidazopyridine–propenone conjugates (8a–8u) were synthesized and evaluated for their antitumor activity against four human cancer cell lines.

Synthesis and Antitumor Activity of Novel 1-Substituted 3-(4,5-Substituted 1,2,4-Triazol-3-yl)-β-carboline Derivatives

Synthesis ◽  
2018 ◽  
Vol 51 (02) ◽  
pp. 573-577 ◽  
Author(s):  
Maria Sarragiotto ◽  
George Brand ◽  
Carla Gomes ◽  
Willian Costa ◽  
Mary Foglio ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Broad Spectrum ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Mcf 7

Schiff bases, 1,2,4-triazolo[4,3-d][1,2,3,4]thiatriazoles, and 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles carrying the β-carboline nucleus were synthesized from 3-(4-amino-5-mercapto-1,2,4-triazol-3-yl)-β-carbolines. The compounds were evaluated for their in vitro antitumor activity against eight human cancer cell lines. The 1,2,4-triazolo[4,3-d][1,2,3,4]thiatriazole derivatives showed a broad spectrum of antitumor activity, with GI50 values lower than 13 μM for all cell lines tested. In general, all tested compounds showed potent activity against the breast (MCF-7) cancer cell line, with GI50 values in the range of 2.07 to 4.58 μM.

scholarly journals Design, Synthesis and Characterization of Novel Amine Derivatives of 5-[5-(Chloromethyl)-1, 3, 4-Oxadiazol-2-yl]- 2-(4-Fluorophenyl)-Pyridine as a New Class of Anticancer Agents

2017 ◽  
Vol 16 (1) ◽  
pp. 11-19 ◽  
Author(s):  
Adimule Vinayak ◽  
Medapa Sudha ◽  
Kumar S Lalita
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Secondary Amines ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Ic50 Values ◽  
High Cytotoxicity ◽  
Hepg2 Cell Lines

A linear strategy was adopted in synthesizing the novel amine derivatives 7(a-h) of 5-[5- (chloromethyl)-1, 3, 4-oxadiazol-2-yl]-2-(4-fluorophenyl)-pyridine (6) and screened these compounds for in vitro anticancer activity against three human cancer cell lines (HeLa,Caco-2 and HepG2). The synthesised novel compounds were characterized by 1H NMR, MS and 13C NMR spectroscopic evidences. Microwave irradiation of compound (5) in presence of chloroacetyl chloride and phosphoryl oxychloride yielded the dehydrated cyclized key intermediate 5-[5-(chloromethyl)-1,3,4-oxadiazol-2-yl]-2-(4-fluorophenyl)-pyridine which upon treatment with various primary or secondary amines (a-h) resulted into the corresponding amine derivatives. The IC50 values of the final compounds were compared with that of 5-fluorouracil (5-FU) taken as the standard. Compounds 7a and 7d were found to be highly cytotoxic against HepG2 cell lines with IC50 values of 2.6 ?M (IC50 = 34.0 ± 0.5 ?M) and 5.8 ?M (IC50 = 112 ± 1.4 ?M) respectively. The compound (7f) alone was found to have high cytotoxicity against Caco-2 cell lines with IC50 value of 2.3 ?M (IC50 = 87 ± 2.6 ?M).Dhaka Univ. J. Pharm. Sci. 16(1): 11-19, 2017 (June)

scholarly journals Design, Synthesis, and Biological Evaluation of Aromatic Amide-Substituted Benzimidazole-Derived Chalcones. The Effect of Upregulating TP53 Protein Expression

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1162
Author(s):  
Lintao Wu ◽  
Yuting Yang ◽  
Zhijun Wang ◽  
Xi Wu ◽  
Feng Su ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Mechanistic Study ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Aromatic Amide ◽  
Synthesis And Biological Evaluation ◽  
Tp53 Protein

A series of benzimidazole-derived chalcones containing aromatic amide substituent were designed and synthesized. All of the chalcone compounds were tested for their in vitro antitumor activity against human cancer cell lines (HCT116, HepG2, A549, and CRL-5908). The antiproliferative activity of compounds 3, 6, 9, 14, 15, 16 against HCT116 cells was significantly better than that that of 5-Fluorouracil (IC50: 94.63 µM). The antitumor activity of these compounds showed obvious differences between the wild type HCT116 and mutant HCT116 (TP53−/−) cells. A preliminary mechanistic study suggested that these compounds act by upregulating the expression of TP53 protein in tumor cells without inhibiting the MDM2-TP53 interaction.

Copper(ii) complexes based on tripodal pyridyl amine derivatives as efficient anticancer agents

2019 ◽  
Vol 43 (16) ◽  
pp. 6186-6196 ◽  
Author(s):  
Salah S. Massoud ◽  
Febee R. Louka ◽  
Ada F. Tusa ◽  
Nicole E. Bordelon ◽  
Roland C. Fischer ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

The in vitro cytotoxicity of a series of chlorido-Cu(ii) complexes based on tripod pyridyl N4-donor derivatives revealed significant-to-moderate cytotoxicity against human cancer cell lines with the best results obtained for [Cu(BQPA)Cl]ClO4/PF6 (5-ClO4/PF6) with IC50 values of 4.7–10.8 μM.

Synthesis of Diaryl Pyrrolones Derivatives as Combretastatin A-4

2013 ◽  
Vol 652-654 ◽  
pp. 689-692 ◽  
Author(s):  
Li Wei ◽  
Guo Yuan Lu
Keyword(s):  
Double Bond ◽  
Antitumor Activity ◽  
Natural Product ◽  
13C Nmr ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
New Compounds ◽  
Cis Isomer

Combretastatins-A4 (CA-4) is a natural product with anticancer activity. However, only the cis-isomer exhibits strong antitubulin activity, but the cis-isomer tends to isomerize to the inactive trans-isomer. Thus, this paper reports that an additional pyrrolidone ring was used to replace the cis double bond to arrest the cis-conformation, and a series of 3,4-diaryl pyrrolediones and 3,4-diaryl pyrrolones as CA-4 analogues were synthesized via a four steps reaction from 3,4-dimethoxyacetophenone and 3-fluoro-4-methoxy acetophenone. The structure of the new compounds was confirmed by 1H NMR, 13C NMR, ESI-MS and elemental analysis. The in vitro activities of CA-4 analogues against HL-60, SMMC-7721 and A549 human cancer cell lines were tested using colorimetric MTT assay and the results indicate that they show significant antitumor activity.

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