scholarly journals Crystal Structure and Biological Evaluation of Two Novel Organic-Inorganic Hybrid Materials as Antitumor Agents in the Treatment of Liver Cancer

2018 ◽  
Vol 2018 ◽  
pp. 1-6 ◽  
Author(s):  
Bao-Hua Song ◽  
Chen Li ◽  
Gui-Feng An
Keyword(s):  
Cell Lines ◽  
Hybrid Materials ◽  
Antitumor Agents ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Single Crystal Diffraction ◽  
Inorganic Hybrid ◽  
X Ray ◽  
Liver Tumor Cell

Two novel organic-inorganic hybrid materials {(Hbiz)6[AsIII2AsVMoVI18O62]}·H2O (1, biz = benzimidazole) and (dim)[AsIII2AsVMoVI18O62] [2, dim = 1,6-bis(imidazol)hexane] have been successfully obtained by using the molybdenum arsenate and different N donor organic compounds and determined through X-ray single-crystal diffraction technique. The in vitro cytotoxicity of compounds 1 and 2 was then investigated against three human liver tumor cell lines (SMMC7721, Bel-7402, and MHCC97) by MTT assay. It was found that the two compounds showed potent use as antitumor agents against the aforementioned cell lines.

scholarly journals Synthesis and biological evaluation of novel benzo[b]xanthone derivatives as potential antitumor agents

2013 ◽  
Vol 78 (9) ◽  
pp. 1301-1308 ◽  
Author(s):  
Lin Luo ◽  
Jiang-Ke Qin ◽  
Zhi-Kai Dai ◽  
Shi-Hua Gao
Keyword(s):  
Cell Lines ◽  
Antitumor Agents ◽  
Biological Evaluation ◽  
Structural Factors ◽  
Anticancer Activities ◽  
Antitumor Activities ◽  
Mtt Method ◽  
Human Solid Tumor ◽  
Synthesis And Biological Evaluation

Nine novel aminoalkoxy substituted benzoxanthones (3a-3i) were synthesized. Their antitumor activities were evaluated in five human solid tumor cell lines including Hep-G2, BEL-7402, HeLa, MGC-803 and CNE by MTT method. The results showed that most of the compounds displayed moderate to good inhibitory activities on the tested cancer cell lines in vitro, among them compounds 3a and 3h showed higher antitumor activity than other tested compounds against most cell lines. The influence of two kinds of structural factors including the terminal amino group and length of carbon spacers on the anticancer activities were explored to discuss the preliminary structure-activity relationships.

Synthesis and Biological Evaluation of New Piperazine Substituted 3, 5-Diarylisoxazolines

2019 ◽  
Vol 16 (2) ◽  
pp. 294-302 ◽  
Author(s):  
Hui Gao ◽  
Bei Liu ◽  
Ping Zhu ◽  
Li-Jun Zhang ◽  
Chun-Ping Wan ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Human Tumor ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

Aim and Objective: Isoxazolines are an important class of nitrogen and oxygen-containing heterocycles, which have gained much importance as the potential biological agents. In order to study structureactivity relationships of isoxazolines, this work has been conducted. Materials and Methods: A series of new piperazine substituted 3, 5-diarylisoxazoline derivatives (6-31) were designed and synthesized, and in vitro anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and anticancer effect against a panel of human tumor cell lines (Hela, A549 and SGC7901) by MTT assay were evaluated. Results: The substituents of the NH group of piperazine ring had an obvious influence on biological activities. Especially, compounds 5, 7, 8, 10, 11, 13 and 27-showed good inhibitory effect on the generation of NO compared to dexamethasone. Furthermore, derivatives 5, 6, 7, 8, 9, 13 and 26 were found to be potential selectively anticancer activity on human tumor cell lines, which displayed better cytotoxic activity to positive control 5- FU. Conclusion: Piperazine substituted 3, 5-diarylisoxazoline derivatives could be considered as new antiinflammatory and anticancer agents.

scholarly journals Synthesis, X-Ray Crystal Structures, Biological Evaluation, and Molecular Docking Studies of a Series of Barbiturate Derivatives

2016 ◽  
Vol 2016 ◽  
pp. 1-11 ◽  
Author(s):  
Assem Barakat ◽  
Hazem A. Ghabbour ◽  
Abdullah Mohammed Al-Majid ◽  
Qurat-ul-ain ◽  
Rehan Imad ◽  
...  
Keyword(s):  
Cell Lines ◽  
Thymidine Phosphorylase ◽  
Fibroblast Cell ◽  
Biological Evaluation ◽  
Molecular Structures ◽  
Butylated Hydroxytoluene ◽  
Normal Fibroblast ◽  
Standard Drug ◽  
X Ray

A series of barbiturates derivatives synthesized and screened for different set of bioassays are described. The molecular structures of compounds5a,5d,and5fwere solved by single-crystal X-ray diffraction techniques. The results of bioassay show that compounds4a,4b,4c,4d,4e,4f, and4gare potent antioxidants in comparison to the tested standards, butylated hydroxytoluene (BHT), andN-acetylcysteine. Compounds4a–4e(IC50=101.8±0.8–124.4±4.4 μM) and4g(IC50=104.1±1.9 μM) were more potent antioxidants than the standard (BHT,IC50=128.8±2.1 μM). The enzyme inhibition potential of these compounds was also evaluated,in vitro, against thymidine phosphorylase,α-glucosidase, andβ-glucuronidase enzymes. Compounds4c,4h,4o,4p,4q, 5f,and5mwere found to be potentα-glucosidase inhibitors and showed more activity than the standard drug acarbose, whereas compounds4v,and5hwere found to be potent thymidine phosphorylase inhibitors, more active than the standard drug, 7-deazaxanthine. All barbiturates derivatives (4a–4x,4z,and5a–5m) were found to be noncytotoxic against human prostate (PC-3), Henrietta Lacks cervical (HeLa) and Michigan Cancer Foundation-7 breast (MCF-7) cancer cell lines, and 3T3 normal fibroblast cell line, except4ywhich was cytotoxic against all the cell lines.

scholarly journals Synthesis and Biological Evaluation of Phaeosphaeride A Derivatives as Antitumor Agents

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 3043 ◽  
Author(s):  
Victoria Abzianidze ◽  
Petr Beltyukov ◽  
Sofya Zakharenkova ◽  
Natalia Moiseeva ◽  
Jennifer Mejia ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antitumor Agents ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Hct 116 ◽  
Mcf 7

New derivatives of phaeosphaeride A (PPA) were synthesized and characterized. Anti-tumor activity studies were carried out on the HCT-116, PC3, MCF-7, A549, К562, NCI-Н929, Jurkat, THP-1, RPMI8228 tumor cell lines, and on the HEF cell line. All of the compounds synthesized were found to have better efficacy than PPA towards the tumor cell lines mentioned. Compound 6 was potent against six cancer cell lines, HCT-116, PC-3, K562, NCI-H929, Jurkat, and RPMI8226, showing a 47, 13.5, 16, 4, 1.5, and 7-fold increase in anticancer activity comparative to those of etoposide, respectively. Compound 1 possessed selectivity toward the NCI-H929 cell line (IC50 = 1.35 ± 0.69 μM), while product 7 was selective against three cancer cell lines, HCT-116, MCF-7, and NCI-H929, each having IC50 values of 1.65 μM, 1.80 μM and 2.00 μM, respectively.

Insights into the Biological Evaluation of Pterocarpanquinones and Carbapterocarpans with Anti-tumor Activity against MDR Leukemias

2019 ◽  
Vol 19 (1) ◽  
pp. 29-37 ◽  
Author(s):  
Vivian M. Rumjanek ◽  
Raquel C. Maia ◽  
Eduardo J. Salustiano ◽  
Paulo R.R. Costa
Keyword(s):  
Cell Death ◽  
Tumor Cell ◽  
Cell Lines ◽  
Biological Evaluation ◽  
Ehrlich Carcinoma ◽  
Tumor Cell Lines ◽  
Tumor Cell Death ◽  
Mitochondrial Membrane Depolarization

In an attempt to find anticancer agents that could overcome multidrug resistance (MDR), two new classes of modified isoflavonoids were designed and synthesized, and their effectiveness evaluated against a vast array of tumor cell lines. Pterocarpanquinone (LQB-118) and 11a-aza-5-carbapterocarpan (LQB-223) were the most promising. LQB-118 induced cell death, in vitro, in the µM range, to a number of human cancer cell lines as well as to fresh tumor cells obtained from patients with acute or chronic myeloid leukemia, independent on whether they exhibit the MDR phenotype or not. Furthermore, leukemic cells were more sensitive to LQB- 118 compared to cells from solid tumors. Given to mice, in vivo, LQB-118 affected the growth of melanoma, Ehrlich carcinoma and prostate cancer cells. Conversely, no general toxicity was observed in vivo, by biochemical, hematological, anatomical or histological parameters and toxicity in vitro against normal cells was low. The process involved in tumor cell death seemed to vary according to cell type. Apoptosis was studied by externalization of phosphatidylserine, DNA fragmentation, caspase-3 activation, reduced expression of XIAP and survivin, ER stress, cytosolic calcium increase and mitochondrial membrane depolarization. Autophagy was also evaluated inhibiting caspase-9, with no effect observed in beclin 1, whereas pre-treatment with rapamycin increased cytotoxicity induced by LQB-118. In addition, LQB-118 increased ROS, inhibited NFκB nuclear translocation and secretion of TNF-α, modulated microRNAs miR-9 and miR-21 and modified the cell cycle. Despite being less studied, the cytotoxic effect of the 11a-aza-5-carbapterocarpan LQB-223 was present against several tumor cell lines, including those with the MDR phenotype.

scholarly journals Synthesis, X-ray Analysis, Biological Evaluation and Molecular Docking Study of New Thiazoline Derivatives

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1654
Author(s):  
Yahia N. Mabkhot ◽  
H. Algarni ◽  
Abdulrhman Alsayari ◽  
Abdullatif Bin Muhsinah ◽  
Nabila A. Kheder ◽  
...  
Keyword(s):  
Cell Lines ◽  
Docking Study ◽  
Biological Evaluation ◽  
Significant Activity ◽  
Inhibition Activity ◽  
Antitumor Activities ◽  
Molecular Docking Study ◽  
X Ray ◽  
Hct 116

A series of new thiazoline derivatives were synthesized. Structure analyses were accomplished employing 1H-NMR, 13C-NMR, X-ray and MS techniques. The in vitro antitumor activities were assessed against human hepatocellular carcinoma (HepG-2) and colorectal carcinoma (HCT-116) cell lines. The results revealed that the thiazolines 5b and 2c exhibited significant activity against the two cell lines. The in vitro antimicrobial screening showed that the thiazolines 2c, 5b and 5d showed promising inhibition activity against Salmonella sp. Additionally, the inhibition activity of thiazolines 2e and 5b against Escherichia coli was comparable to that of the reference compound gentamycin.

Synthesis and biological evaluation of novel hybrid compounds between chalcone and piperazine as potential antitumor agents

RSC Advances ◽  
2016 ◽  
Vol 6 (10) ◽  
pp. 7723-7727 ◽  
Author(s):  
Zewei Mao ◽  
Xi Zheng ◽  
Yan Qi ◽  
Mengdi Zhang ◽  
Yao Huang ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Human Tumor ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Hybrid Compounds ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor

A series of novel hybrid compounds between chalcone and piperazine have been synthesized, and their in vitro antitumor activity was evaluated against a panel of human tumor cell lines by MTT assay.

Synthesis and biological evaluation of novel derivatives of gambogenic acid as anticancer agents

MedChemComm ◽  
2015 ◽  
Vol 6 (2) ◽  
pp. 334-338 ◽  
Author(s):  
Peng Huang ◽  
Zhong Hu ◽  
Liqin He ◽  
Xiaoshan Wang ◽  
Yaxian Wu
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Antiproliferative Activity ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel derivatives of gambogenic acid (GNA) were synthesized and evaluated for their in vitro antiproliferative activity against four kinds of tumor cell lines. These compounds displayed potent antiproliferative activity. In particular, compound 3f exhibited superior antiproliferative activity against these tumor cell lines than GNA.

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