Synthesis of α-Aminoalkyl Phosphonate Derivatives of Resveratrol as Potential Antitumour Agents

2008 ◽  
Vol 61 (6) ◽  
pp. 472 ◽  
Author(s):  
Lei Shi ◽  
Xian-Feng Huang ◽  
Zhen-Wei Zhu ◽  
Huan-Qiu Li ◽  
Jia-Yu Xue ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Tumour Cell Line ◽  
Partial Synthesis ◽  
Antitumour Agents ◽  
Inhibition Concentration ◽  
Ic50 Values ◽  
Epidermoid Tumour ◽  
Derivatives Of

Several α-aminoalkyl phosphonate derivatives of resveratrol were first prepared by partial synthesis from resveratrol. Antitumour activities of the synthesized compounds were determined against a human nasopharyngeal epidermoid tumour cell line KB and a human normal cell line L02 in vitro. The results indicated that these compounds showed good cytotoxic activity against KB but weak cytotoxic activity against L02. Compounds 5c and 5d showed significant cytotoxic activity against KB, with median inhibition concentration (IC50) values of 0.4 μM and 0.9 μM, respectively. On the basis of the biological results, the structure–activity relationship is discussed concisely. The potent antitumour activities shown by 5c and 5d make these resveratrol phosphonate derivatives of great interest for further investigations.

Synthesis, Characterization, and Antibacterial and Cytotoxic Study of Metal Complexes with Schiff Base Ligands

2008 ◽  
Vol 61 (4) ◽  
pp. 288 ◽  
Author(s):  
Lei Shi ◽  
Rui-Qin Fang ◽  
Jia-Yu Xue ◽  
Zhu-Ping Xiao ◽  
Shu-Hua Tan ◽  
...  
Keyword(s):  
Schiff Base ◽  
Metal Complexes ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Primary Amines ◽  
Tumour Cell Line ◽  
Cytotoxic Activities ◽  
Ionization Mass ◽  
Schiff Base Ligands

The synthesis of 16 metal complexes from four Schiff bases prepared from 5-chloro-2-hydroxybenzaldehyde and primary amines has been described. The synthesized Schiff base ligands and their complexes were characterized by elemental analyses, spectroscopic (UV, IR, 1H and 13C NMR, electrospray ionization-mass spectrometry) methods, and magnetic and conductance measurements. Furthermore, complexes 1a, 1b, 3d, 4a, and 4d were characterized by X-ray diffraction analysis. After the structural characterization, all the compounds were tested in vitro for their antibacterial (Bacillus subtilis, Escherichia coli, Pseudomonas fluorescens, and Staphylococcus aureus) activities. The cytotoxic activities of the synthesized compounds were evaluated in vitro against human chronic myeloid leukaemia cells (K562) and a human nasopharyngeal epidermoid tumour cell line. The results indicated that most of the complexes showed good cytotoxic activity against human cancer cell lines but weak cytotoxic activity against a human normal cell line (L02). Among the compounds tested, the cobalt complexes 1a, 2a, 3a, and 4a showed the most favourable antibacterial and cytotoxic activities.

scholarly journals Platinum derivatives: generic brands vs. original, in vitro tests

2015 ◽  
Vol 23 (4) ◽  
pp. 439-448
Author(s):  
Sînziana Cetean ◽  
Călin Căinap ◽  
Olga Soriţău ◽  
Corina Tatomir ◽  
Piroska Virag ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Generic Drugs ◽  
Response To Therapy ◽  
In Vitro Tests ◽  
Ic50 Values ◽  
The Difference ◽  
Different Response ◽  
Ht 29

Abstract The entry of the generic drugs on the market was an impressive development of the pharmaceutical industry and due to their lower prices also a decrease in the cost price for the treatment of patients. The difference in price (sometimes even 50%) between generics and original and different response to therapy sometimes raised serious questions related to their therapeutic equivalence. The scientific community is increasingly interested in this aspect, with studies (in vitro and on patients) demonstrated statistically significant differences in terms of differences generic / original drug. In this context, the aim of our study was to assess the in vitro cytotoxic activity of oxaliplatin (original and generic drug) on DLD-1 cell lines, HT-29, and carboplatin cytotoxic activity (and the reference molecule from Santa Cruz Biotechnology) on cell line A2780. Cell viability was evaluated using the MTT assay. Regarding the cell line DLD-1, IC50 values of generics was lower than the original after exposure for 24 hours to oxaliplatin but after 48 hours of exposure were not statistically significant differences. HT-29 line has a higher resistance to chemotherapy compared with oxaliplatin, the IC 50 values after 48 hours of exposure are higher than those for the line DLD-1. IC50 values are confirmed by morphological analysis of cells. Regarding carboplatin were not recorded statistically significant differences between the two generic drugs tested. Although other studies reported differences between generic and branded drugs in terms of hypersensibility reactions, adverse effects and efficacity, we cannot extrapolate our findings to the patients. Further studies on patients are neeeded for a better evaluation of the efficacity of generic vs. original drugs.

scholarly journals Cytotoxic activity of ethanolic extracts of Eleutherococcus species cultivated in Poland on HL60 leukemia cell line

2014 ◽  
Vol 27 (1) ◽  
pp. 41-45 ◽  
Author(s):  
Daniel Zaluski ◽  
Helena Danuta Smolarz ◽  
Anna Bogucka-Kocka
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Morphological Changes ◽  
Leukemia Cell ◽  
Ethanol Extract ◽  
Leukemia Cell Line ◽  
Lymphoid Leukemia ◽  
Ethanolic Extracts ◽  
Ic50 Values

Abstract The Eleutherococcus species including 40 species native to Asia are medicinal plants widely used in traditional medicine. Some of these species are cultivated at the botanical gardens in Europe. On the basis on our earlier studies it was concluded that the extracts of analyzed species act as antioxidants, inhibitors of MMPs, and cytotoxic against Jurkat 45 leukemia cell line. In this study, the anti-leukemic potential of roots and leaves from six Eleutherococcus species cultivated in Poland was determined. The in vitro cytotoxic activity towards human promyelotic leukemia cell line HL60 using trypan blue assay was evaluated. The induction of apoptosis in stimulated leukemia cells was determined by AnnexinV method. Morphological changes in treated cells were observed by microscopic investigations. The results showed that ethanolic extracts from the roots and the leaves of E. senticosus, E. setchuensis, E. sessiliflorus, E.gracilistylus, E. henryi and E. divaricatus exhibit cytotoxic effect towards leukemic HL60 cells. The received IC50 values for roots ranged from 49- 208 μg/mL and for the leaves from 116-518 μg/mL. The ethanol extract from the roots of E. divaricatus showed the highest cytotoxic and proapoptotic effect on HL60 human lymphoid leukemia cell line.

Synthesis of Novel 1,2,3-Triazole Derivatives of Isocoumarins and 3,4-Dihydroisocoumarin with Potential Antiplasmodial Activity In Vitro

2020 ◽  
Vol 16 ◽  
Author(s):  
Lucas da Silva Santos ◽  
Matheus Fillipe Langanke de Carvalho ◽  
Ana Claudia de Souza Pinto ◽  
Amanda Luisa da Fonseca ◽  
Julio César Dias Lopes ◽  
...  
Keyword(s):  
Triazole Ring ◽  
Antiplasmodial Activity ◽  
World Health ◽  
Dipolar Cycloaddition ◽  
Terminal Alkynes ◽  
The World ◽  
Ic50 Values ◽  
Derivatives Of ◽  
Active Substances

Background: Malaria greatly affects the world health, having caused more than 228 million cases only in 2018. The emergence of drug resistance is one of the main problems in its treatment, demonstrating the urge for the development of new antimalarial drugs. Objective: Synthesis and in vitro antiplasmodial evaluation of triazole compounds derived from isocoumarins and a 3,4- dihydroisocoumarin. Method: The compounds were synthesized in 4 to 6-step reactions with the formation of the triazole ring via the Copper(I)-catalyzed 1,3-dipolar cycloaddition between isocoumarin or 3,4-dihydroisocoumarin azides and terminal alkynes. This key reaction provided compounds with an unprecedented connection of isocoumarin or 3,4-dihydroisocoumarin and the 1,2,3-triazole ring. The products were tested for their antiplasmodial activity against a Plasmodium falciparum chloroquine resistant and sensitive strains (W2 and 3D7, respectively). Results: Thirty-one substances were efficiently obtained by the proposed routes with an overall yield of 25-53%. The active substances in the antiplasmodial test displayed IC50 values ranging from 0.68-2.89 μM and 0.85-2.07 μM against W2 and 3D7 strains, respectively.

Synthesis, Cytotoxicity and Antioxidant Activity of New Analogs of RC-121 Synthetic Derivatives of Somatostatin

2019 ◽  
Vol 18 (10) ◽  
pp. 1417-1424 ◽  
Author(s):  
Emilia Naydenova ◽  
Diana Wesselinova ◽  
Svetlana Staykova ◽  
Ivan Goshev ◽  
Ljubomir Vezenkov
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Capacity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Colorectal Cancer Cell Line ◽  
Cervical Cancer Cell Line ◽  
Synthetic Derivatives ◽  
Derivatives Of

Background: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity. Objectives: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine). Methods: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (Human Colorectal Cancer Cell Line), MDA-MB-23 (Human Breast Cancer Cell Line), Hep G-2 (Human Hepatocellular Carcinoma Cell Line) and HeLa (cervical cancer cell line). The antioxidant capacities were tested by ORAC (Oxygen Radical Antioxidant Capacity) and HORAC (Hydroxyl Radical Averting Capacity) methods. Results: All substances expressed significantly higher antioxidant capacity by comparison with galic acid and Trolox. All substances showed considerable antioxidant capacity as well. Compound 2T (D-Phe-c(Cys-Tyr-DTrp- Dap-Tle-Cys)-Thr-NH2)had the highest antioxidant effect. The compound 4T (D-Phe-c(Cys-Tyr-D-Trp- Orn-Tle-Cys)-Thr-NH2) displayed antiproliferative effect on HeLa cells with IC50 30 µM. The peptide analog 3T (D-Phe-c(Cys-Tyr-D-Trp-Lys-Tle-Cys)-Thr-NH2) exerted the most pronounced inhibition on the cell vitality up to 53%, 56% and 65% resp. against MDA-MB-23, Hep G-2, HeLa in the higher tested concentration. Conclusion: The somatostatin analogs showed moderate influence on the vitality of different tumor cells and could be used in changing their pathology.

scholarly journals Current Status, Distribution, and Future Directions of Natural Products against Colorectal Cancer in Indonesia: A Systematic Review

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4984
Author(s):  
Didi Nurhadi Illian ◽  
Ihsanul Hafiz ◽  
Okpri Meila ◽  
Ahmad Rusdan Handoyo Utomo ◽  
Arif Nuryawan ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Systematic Review ◽  
Natural Products ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Cell Line ◽  
Current Status ◽  
Vitro Assay ◽  
Colorectal Cancer Cells

In 2020, an estimated 19.3 million new cancer cases and nearly 10 million cancer deaths have occurred worldwide, with colorectal cancer ranking as the third most frequently diagnosed (10.0%). Several attempts have been conducted against cancer, including surgery, radiation, monoclonal antibodies, and chemotherapy. Many people choose natural products as alternatives against cancer. These products will not only help in human life preservation but also work as a source of up-to-date information, leading people away from incorrect information. We discuss the current status, distribution, and future implications of protecting populations with natural products as an alternative against colorectal cancer in Indonesia. Thirty-eight studies were included in this review for data extraction. The distribution of natural products in Indonesia that have potential activity against colorectal cancer cells was predominated by terpenoids, followed by phytosterols, phenolics, alkaloids, and polyisoprenoids. The type of cell line utilized in the cytotoxic activity analysis of natural products was the WiDr cell line, followed by HT-29 cells and HCT-116 cells. This review showed that MTT in vitro assay is a general method used to analyze the cytotoxic activity of a natural product against colorectal cancer cells, followed by other in vitro and in vivo methods. The systematic review provided predictions for several secondary metabolites to be utilized as an alternative treatment against colorectal cancer in Indonesia. It also might be a candidate for a future co-chemotherapy agent in safety, quality, and standardization. In addition, computational methods are being developed to predict the drug-likeness of compounds, thus, drug discovery is already on the road towards electronic research and development.

scholarly journals Novel Synthesis Method of Micronized Ti-Zeolite Na-A and Cytotoxic Activity of Its Silver Exchanged Form

2015 ◽  
Vol 2015 ◽  
pp. 1-12 ◽  
Author(s):  
H. F. Youssef ◽  
W. H. Hegazy ◽  
H. H. Abo-almaged ◽  
G. T. El-Bassyouni
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Carcinoma Cell ◽  
Synthesis Method ◽  
Carcinoma Cell Line ◽  
Breast Adenocarcinoma ◽  
Synthetic Process ◽  
Colon Cell ◽  
Colon Cell Line

The core-shell method is used as a novel synthetic process of micronized Ti-Zeolite Na-A which involves calcination at 700°C of coated Egyptian Kaolin with titanium tetrachloride in acidic medium as the first step. The produced Ti-coated metakaolinite is subjected to microwave irradiation at low temperature of 80°C for 2 h. The prepared micronized Ti-containing Zeolites-A (Ti-Z-A) is characterized by FTIR, XRF, XRD, SEM, and EDS elemental analysis. Ag-exchanged form of Ti-Z-Ag is also prepared and characterized. The Wt% of silver exchanged onto the Ti-Zeolite structure was determined by atomic absorption spectra. Thein vitrocytotoxic activity of Ti-Z-Ag against human hepatocellular carcinoma cell line (HePG2), colon cell line carcinoma (HCT116), lung carcinoma cell line (A549), and human Caucasian breast adenocarcinoma (MCF7) is reported. The results were promising and revealed that the exchanged Ag form of micronized Ti-Zeolite-A can be used as novel antitumor drug.

IN-SILICO AND IN VITRO ASSESSMENT OF SYNTHESIZED DIAZENYLSULFONAMIDES AS APOPTOSIS INDUCERS AND RADICAL SCAVENGERS

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (06) ◽  
pp. 49-59
Author(s):  
Priyambada Kshiroda Nandini Sarangi ◽  
Jyotirmaya Sahoo ◽  
Chita Ranjan Sahoo ◽  
Sudhir Kumar Paidesetty ◽  
Guru Prasad Mohanta
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Radical Scavenging ◽  
Cancer Cell Line ◽  
Scavenging Effect ◽  
Ic50 Values ◽  
Radical Scavenging Effect ◽  
The Individual ◽  
Mcf 7

A series of eight quinoline-thiazole hybrid-bearing diazenylsulfonamides, 4a-4h, were synthesized and characterized by UV-Vis, FT/IR, 1H NMR and lC-MS. These compounds were formed when two prepared intermediate precursors of Schiff-base compounds, (E)-N-((2-chloroquinolin-3-yl)methylene)-4phenylthiazol-2-amine (3a) and (E)-N-((2-chloroquinolin-3-yl)methylene)-4-chlorophenylthiazol-2-amine (3b) were converted to the corresponding diazenyl compounds 4a-4h by treating and coupling with the individual diazonium salts of sulfa-drugs. The results of in vitro cytotoxic activity of the synthesized compounds in two cancer cell lines MCF 7 (human breast cancer cell line) and K562 (myelogenousleukemia cell line) have shown the IC50 values as given: 4b against MCF 7 19.52 and against K562 20.55µM; 4d against MCF 7 15.96 and against K562 13.05µM. Moreover, the compound 4-(((Z)-(2-chloroquinolin-3yl)(4-phenylthiazol-2-ylimino)methyl)diazenyl)benzenesulfonic acid (4d) induced maximum percentage of apoptosis. Furthermore, the in vitro antioxidant activity study revealed that among all the synthesized compounds, compound 4d has an excellent radical scavenging effect. Molecular docking was additionally performed to investigate the binding affinity of H-bonding interaction of synthesized compounds with a targeted enzyme and to compare it with the anticancer drugs, dasatinib, bosutinib and dacarbazine.

scholarly journals Synthesis and In vitro cytotoxic activity evaluation of (E)-16-(substituted benzylidene) derivatives of dehydroepiandrosterone

2013 ◽  
Vol 21 (1) ◽  
Author(s):  
Mohsen Vosooghi ◽  
Hoda Yahyavi ◽  
Kouros Divsalar ◽  
Hashem Shamsa ◽  
Asma Kheirollahi ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Activity Evaluation ◽  
Derivatives Of
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