scholarly journals Synthesis and Biological Evaluation of Some 1,8-Naphthalimide-Acridinyl Hybrids

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Rui Chen ◽  
Caiying Yuan ◽  
Yogini Jaiswal ◽  
Lini Huo ◽  
Dianpeng Li ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Inhibition Activity ◽  
Dna Topoisomerase ◽  
Human Cancer Cell Lines ◽  
Pharmacological Mechanism ◽  
Electrophorus Electricus ◽  
Synthesis And Biological Evaluation ◽  
Mcf 7

In the present study, the synthesis of three 1,8-naphthalimide-acridinyl hybrids (2a, 2b, and 5b) using N-amido-1,8-naphthalimides (1 and 4) and acridinyl isothiocyanates is reported. The newly synthesized hybrids were evaluated for their anticancer activity in six human cancer cell lines (HL-60, MT-4, HepG2, HeLa, SK-OV-3, and MCF-7). Their inhibition activity against DNA-topoisomerase I (Topo I) and Electrophorus electricus acetylcholinesterase (AChE) was also studied. The results indicate that 2b displayed good cytotoxicity for MT-4, HepG2, HeLa, and SK-OV-3 with the IC50 values of 14.66 ± 0.31, 27.32 ± 2.67, 17.51 ± 0.34, and 32.26 ± 1.74 μM, respectively. All compounds, especially 2b, exhibited obvious bands corresponding to DNA fragments at 0.5 mM concentration, further confirming the pharmacological mechanism related to the Topo I inhibitory activities. In addition, compound 2a exhibited higher inhibition activity against AChE than 2b and 5b, with IC50 values of 0.32 ± 0.04 mM, and the acridinyl ring may contribute to the activity of 2a.

scholarly journals Synthesis and Biological Evaluation of Oseltamivir Analogues from Shikimic Acid

2014 ◽  
Vol 9 (7) ◽  
pp. 1934578X1400900
Author(s):  
Van Hung Nguyen ◽  
Van Cuong Pham ◽  
Thi Thao Do ◽  
Huong Doan Thi Mai ◽  
Nguyen Thanh Le ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Influenza A ◽  
Shikimic Acid ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Inhibition Activity ◽  
Azide Group ◽  
Human Cancer Cell Lines ◽  
Synthesis And Biological Evaluation

New oseltamivir analogues were designed and synthesized, starting from shikimic acid. Biological evaluation against three human cancer cell lines (KB, MCF7 and Lu-1) showed that many of them exhibited cytotoxic activity. Azides 5 are more active than the corresponding amines 6. Thus, the reduction of the azide group into amine led to the loss of cytotoxicity. The compounds with a cyclohexanemethyloxy group at C-3 were more active than the other investigated compounds belonging to the same series. This cyclohexanemethyloxy group seems to be critical for the cytotoxic activity of this class of compounds. The synthetic oseltamivir analogues 6a-e had no inhibition activity, even at the concentration of 50 μM when they were evaluated for their in vitro influenza A neuraminidase inhibitory activity by an enzymatic assay.

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.

scholarly journals Synthesis and Biological Evaluation of New (−)-Gossypol-Derived Schiff Bases and Hydrazones

2017 ◽  
Vol 2017 ◽  
pp. 1-8 ◽  
Author(s):  
Vu Van Vu ◽  
Trinh Thi Nhung ◽  
Nguyen Thi Thanh ◽  
Luu Van Chinh ◽  
Vu Dinh Tien ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Schiff Bases ◽  
Cell Lines ◽  
Human Cancer ◽  
Structural Data ◽  
Biological Evaluation ◽  
Human Cancer Cell Lines ◽  
High Yields ◽  
Synthesis And Biological Evaluation

A series of 14 new (-)-gossypol Schiff bases and hydrazones have been synthesized via an in situ procedure in high yields. Structural data showed that all target compounds exist as the enamine tautomer. Bioassays showed that several compounds exhibited cytotoxic effects against three human cancer cell lines. Compound 8a showed the greatest cytotoxic effect against hepatocellular carcinoma (HepG2), lung carcinoma (LU-1), and breast cancer (MCF-7) cell lines with IC50 values of 20.93, 13.58, and 9.40 μM, respectively. However, in an antibacterial test, compounds 8a and 8b inhibited Staphylococcus aureus and Bacillus cereus and compound 8e inhibited only Staphylococcus aureus at the same MIC values of 1024 μg/ml.

scholarly journals Synthesis and Biological Evaluation of 1,3,4-Oxadiazole Fused Resveratrol Derivatives as Anticancer Agents

2020 ◽  
Vol 32 (8) ◽  
pp. 1967-1971
Author(s):  
Vema Venkata Naresh ◽  
Y. Bharathi Kumari ◽  
Mussulla Sridhar ◽  
Addada Ramakrishnam Raju ◽  
A. Srinivasa Rao
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Positive Control ◽  
Biological Evaluation ◽  
Human Cancer Cell Lines ◽  
Control Drug ◽  
Novel Target ◽  
Synthesis And Biological Evaluation ◽  
A549 Lung

A novel target compounds (9a-j) were design and synthesized and characterized by 1H & 13C NMR, ESI-MS spectral analysis. Further, these were tested for their anticancer activity against three human cancer cell lines such as MCF-7, MDA MB-231 (breast), A549 (Lung) and adriamycin was used as positive control. Among ten compounds, two compounds like 9b and 9j were showed a significant anticancer activity compared to control drug.

Synthesis and biological evaluation of sapinofuranones A,B and 1,2,3-triazole-sapinofuranone hybrids as cytotoxic agents

RSC Advances ◽  
2016 ◽  
Vol 6 (103) ◽  
pp. 101501-101512 ◽  
Author(s):  
K. Siva Nagi Reddy ◽  
Gowravaram Sabitha ◽  
Y. Poornachandra ◽  
C. Ganesh Kumar
Keyword(s):  
Total Synthesis ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Synthesis And Biological Evaluation

The total synthesis of sapinofuranones A,B and ent-sapinofuranones A,B and L-factor and a series of novel 1,2,3-triazole-sapinofuranone hybrids is described and their cytotoxicity against four human cancer cell lines (A549, MDA-MB-231, DU145 and HepG2) was evaluated.

scholarly journals Synthesis and Biological Evaluation of Lipophilic 1,4-Naphthoquinone Derivatives against Human Cancer Cell Lines

Molecules ◽  
2015 ◽  
Vol 20 (7) ◽  
pp. 11994-12015 ◽  
Author(s):  
Shao-Hung Wang ◽  
Chih-Yu Lo ◽  
Zhong-Heng Gwo ◽  
Hong-Jhih Lin ◽  
Lih-Geeng Chen ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Synthesis And Biological Evaluation

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.

Fused imidazoles as potential chemical scaffolds for inhibition of heat shock protein 70 and induction of apoptosis. Synthesis and biological evaluation of phenanthro[9,10-d]imidazoles and imidazo[4,5-f][1,10]phenanthrolines

2016 ◽  
Vol 14 (16) ◽  
pp. 3889-3905 ◽  
Author(s):  
Alpa Patel ◽  
Swee Y. Sharp ◽  
Katelan Hall ◽  
William Lewis ◽  
Malcolm F. G. Stevens ◽  
...  
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Cell Lines ◽  
Heat Shock Protein 70 ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Induction Of Apoptosis ◽  
Synthesis And Biological Evaluation

Fused imidazoles inhibit growth of human cancer cell lines, and the Hsp70 pathway in cells, and induce apoptosis.

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