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 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 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)

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.

scholarly journals Design, Synthesis, Antimicrobial and Anticancer Activity of some Novel Benzoxazole-Isatin Conjugates

2021 ◽  
Vol 12 (2) ◽  
pp. 2392-2403
Keyword(s):  
Antibacterial Activity ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Protein Targets ◽  
Human Cancer Cell Lines ◽  
Fungal Organisms ◽  
Isatin Derivatives

A series of novel benzoxazole-isatin conjugates were synthesized by treating 2-amino benzoxazole with 5 and 7 substituted isatin derivatives and were screened for in vitro antimicrobial and cytotoxic activities. The results showed that all the synthesized compounds shown mild to potent antibacterial activity. The MIC values were found between 10 and 100 µg/ml against tested bacterial and fungal organisms. Among all the compounds, 3d & 3c showed good antimicrobial. In vitro cytotoxic activities were evaluated by MTT assay of all the test compounds against the different human cancer cell lines. The compounds having substitution with electron-withdrawing groups (halides) at the 5th position on the isatin ring showed the most significant biological activity than substituted at the 7th position. The molecular docking interactions have shown good binding interactions with the protein targets glucosamine-6-phosphate synthase (GlcN-6-P synthase) and telomerase.

scholarly journals Design, synthesis and biological evaluation of novel 5-bromo derivatives of indole phytoalexins

2020 ◽  
Author(s):  
Mariana Budovská ◽  
Ivana Selešová ◽  
Viera Tischlerová ◽  
Radka Michalková ◽  
Ján Mojžiš
Keyword(s):  
Human Cancer ◽  
Type A ◽  
Biological Evaluation ◽  
Synthetic Approach ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Drug Candidates ◽  
Indole Phytoalexins ◽  
Derivatives Of

The increasing diversity of small molecule libraries is a major source for the discovery of new drug candidates. In term of this trend, we report the synthesis five series 5-bromosubstituted derivatives of indole phytoalexins Type A-E using straightforward synthetic approach. Novel compounds were screened in vitro for antiproliferative/cytotoxic activity against seven human cancer cell lines by MTT assay. Evaluation of their antiproliferative potency showed that the activity of some analogues was better or comparable to that of cisplatin and at the same time the toxicity of these compounds on 3T3 cells was lower than that of cisplatin. We found that all 5-bromosubstituted analogues of indole phytoalexins Type A-E exhibited lower or approximately the same activities as a previously studied corrensponding non-brominated compounds.

scholarly journals Synthesis and Cytotoxic Evaluation of Novel Ester Derivatives of Betulin with AZT, d4T, and 3TC

2017 ◽  
Vol 12 (6) ◽  
pp. 1934578X1701200
Author(s):  
Dang Thi Tuyet Anh ◽  
Le Nhat Thuy Giang ◽  
Nguyen Thi Hien ◽  
Dinh Thi Cuc ◽  
Nguyen Ha Thanh ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Antitumor Activities ◽  
Human Cancer Cell Lines ◽  
Anticancer Properties ◽  
Derivatives Of

Novel ester derivatives of betulin with AZT, d4T, and 3TC were synthesized and assessed for antitumor activities against the KB and HepG2 human cancer cell lines in vitro by MTT assay. Some derivatives displayed high anticancer properties, with IC50 values between 1 and 21 μM on the two cancer cell lines.

N-(2-(Arylmethylimino)Ethyl)-7-Chloroquinolin-4-Amine Derivatives: A New and Potent Class of Anticancer Agents

2018 ◽  
Vol 15 (2) ◽  
pp. 113-117
Author(s):  
Ligia S. da Silveira Pinto ◽  
Marcus V.N. de Souza ◽  
Carlos R. Kaiser ◽  
James L. Wardell ◽  
Solange M.S.V. Wardell
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Starting Point ◽  
Good Starting Point ◽  
Cytotoxicity Activities

Background: In this study, we reported the in vitro cytotoxicity activities of a series of N-(2-(arylmethylimino)ethyl)-7-chloroquinolin-4-amine derivatives against four human cancer cell lines. Methods: Good activities were obtained for compounds having aryl groups = 2-hydroxyphenyl, pyridinyl, 5-nitrofuran-2-yl and 5-nitrothiophen-2-yl. Results and Conclusion: The results indicate that this group of compounds is a good starting point for the potential discovery of new prototypes against cancer.

scholarly journals Design, Synthesis, and Cytotoxic Evaluation of Etodolac-1,3,4-oxadiazole-1,2,3-triazole Molecules

SynOpen ◽  
2018 ◽  
Vol 02 (01) ◽  
pp. 0017-0024 ◽  
Author(s):  
Bhaskar Kummari ◽  
Perla Ramesh ◽  
Naveen Polkam ◽  
Shankaraiah Malthum ◽  
M. Vishnuvardhan ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Synthetic Sequence ◽  
A549 Lung ◽  
Mcf 7

A new series of etodolac-1,3,4-oxadiazole-1,2,3-triazole derivatives was designed and synthesized from commercially available starting materials by employing a simple synthetic sequence. The in vitro evaluation of the synthesized analogues displayed promising cytotoxic activity. Among the tested compounds 7c, 7l, and 7n exhibited highest cytotoxic activity against MCF-7 (breast), A549 (lung), and DU-145 (prostate) human cancer cell lines.

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