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.

Design, synthesis and biological evaluation of a novel series of glycosylated platinum(iv) complexes as antitumor agents

2016 ◽  
Vol 45 (25) ◽  
pp. 10366-10374 ◽  
Author(s):  
Qingpeng Wang ◽  
Zhonglv Huang ◽  
Jing Ma ◽  
Xiaolin Lu ◽  
Li Zhang ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Antitumor Activities ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

A new series of glycosylated Pt(iv) complexes were designed, synthesized and evaluated for antitumor activities in vitro and in vivo.

Design, Synthesis and Biological Evaluation of Sunitinib Analogues to Improve Aqueous Solubility

2013 ◽  
Vol 749 ◽  
pp. 350-353 ◽  
Author(s):  
Ke Tao Chen ◽  
Zheng Fang ◽  
Zhao Yang ◽  
Kai Guo
Keyword(s):  
Aqueous Solubility ◽  
Positive Control ◽  
Biological Evaluation ◽  
Antitumor Activities ◽  
Design Synthesis ◽  
H Nmr ◽  
Mtt Method ◽  
Antitumor Bioactivity ◽  
Synthesis And Biological Evaluation

In order to improve aqueous solubility of Sunitinib, based on the structure-activity relationship, four analogues were designed and synthesized. The obtained structures were identified by1H NMR, MS and elemental analysis.In vitroevaluation of antitumor bioactivity was performed by MTT method. All of synthesized compounds showed antitumor activities, especially, compounds A1, which were better than or equal to the antitumor activity of positive control.

Naproxen platinum(iv) hybrids inhibiting cycloxygenases and matrix metalloproteinases and causing DNA damage: synthesis and biological evaluation as antitumor agents in vitro and in vivo

2020 ◽  
Vol 49 (16) ◽  
pp. 5192-5204 ◽  
Author(s):  
Yan Chen ◽  
Qingpeng Wang ◽  
Zuojie Li ◽  
Zhifang Liu ◽  
Yanna Zhao ◽  
...  
Keyword(s):  
Dna Damage ◽  
Matrix Metalloproteinases ◽  
Antitumor Agents ◽  
Biological Evaluation ◽  
Antitumor Activities ◽  
Synthesis And Biological Evaluation

Naproxen platinum(iv) hybrids display effective antitumor activities by inhibiting cycloxygenases and matrix metalloproteinases and by causing DNA damage.

scholarly journals Synthesis and Biological Evaluation of Novel 4-(4-Formamidophenylamino)-N-methylpicolinamide Derivatives as Potential Antitumor Agents

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1150
Author(s):  
Nana Meng ◽  
Shuyan Zhou ◽  
Min Hu ◽  
Youzhi Xu ◽  
Yong Xia ◽  
...  
Keyword(s):  
Cell Lines ◽  
Antitumor Agents ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Human Cancer Cell Lines ◽  
Apoptosis And Necrosis ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor

A novel series of 4-(4-formamidophenylamino)-N-methylpicolinamide derivatives were synthesized and evaluated against different tumor cell lines. Experiments in vitro showed that these derivatives could inhibit the proliferation of two kinds of human cancer cell lines (HepG2, HCT116) at low micromolar concentrations and the most potent analog 5q possessed broad-spectrum antiproliferative activity. Experiments in vivo demonstrated that 5q could effectively prolong the longevity of colon carcinoma-burdened mice and slow down the progression of cancer cells by suppression of angiogenesis and the induction of apoptosis and necrosis.

Synthesis and Biological Evaluation of Novel 4-Phenylaminobenzofuro[2,3-d]pyrimidine Derivatives

2020 ◽  
Vol 42 (4) ◽  
pp. 564-564
Author(s):  
Ju liu Ju liu ◽  
Jun Li Jun Li ◽  
Jian tao Shi Jian tao Shi ◽  
Jie Li Jie Li ◽  
Xue chen Hao Xue chen Hao ◽  
...  
Keyword(s):  
Cell Lines ◽  
A549 Cells ◽  
Positive Control ◽  
Biological Evaluation ◽  
Dependent Manner ◽  
Pyrimidine Derivatives ◽  
Concentration Dependent Manner ◽  
Ic50 Value ◽  
Synthesis And Biological Evaluation

A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.

Antioxidant, α-glucosidase inhibitory and in vitro antitumor activities of coumarin-benzothiazole hybrids

2018 ◽  
Vol 24 (5) ◽  
pp. 243-247 ◽  
Author(s):  
Moustafa T. Gabr
Keyword(s):  
Ovarian Cancer ◽  
Central Nervous System ◽  
Nervous System ◽  
Cell Lines ◽  
Antitumor Agents ◽  
Maximal Growth ◽  
Antitumor Activities ◽  
Cns Cancer ◽  
Inhibitory Activities

Abstract Coumarin-benzothiazole hybrids are antitumor agents based on their antioxidant and α-glucosidase inhibitory activities. Compounds 5a–c were selected by National Cancer Institute (NCI), USA, to be screened for antitumor activity at a single dose (10 μm) against a panel of 60 cancer cell lines. The most active compound 5c was further screened at a five-dose level by NCI. Compound 5c displays half maximal growth inhibition (GI50) values of 0.24 and 0.33 μm against central nervous system (CNS) cancer (SNB-75) and ovarian cancer (OVCAR-4) cell lines, respectively. Compounds 5a–c were also screened for their antioxidant and α-glucosidase inhibitory activities.

Design, synthesis, and biological evaluation of new series of 2-amido-1,3,4-thiadiazole derivatives as cytotoxic agents

2016 ◽  
Vol 71 (3) ◽  
pp. 205-210 ◽  
Author(s):  
Ali Almasirad ◽  
Loghman Firoozpour ◽  
Maliheh Nejati ◽  
Najmeh Edraki ◽  
Omidreza Firuzi ◽  
...  
Keyword(s):  
Human Tumor ◽  
Inhibitory Effect ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
Antitumor Activities ◽  
Design Synthesis ◽  
Ethidium Bromide Staining ◽  
Thiadiazole Derivatives ◽  
Synthesis And Biological Evaluation

AbstractA series of novel 1,3,4-thiadiazole derivatives bearing an amide moiety were designed, synthesized, and evaluated for their in vitro antitumor activities against HL-60, SKOV-3 and MOLT-4 human tumor cell lines by MTT assay. Ethyl 2-((5-(4-methoxybenzamido)-1,3,4-thiadiazol-2-yl)thio)acetate (5f) showed the best inhibitory effect against SKOV-3 cells, with an IC50 value of 19.5 μm. In addition, the acridine orange/ethidium bromide staining assay in SKOV-3 cells suggested that the cytotoxic activity of 5f occurs via apoptosis.

scholarly journals Synthesis and Biological Evaluation of Achiral Indole-Substituted Titanocene Dichloride Derivatives

2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Anthony Deally ◽  
Frauke Hackenberg ◽  
Grainne Lally ◽  
Matthias Tacke
Keyword(s):  
Cell Lines ◽  
Titanium Tetrachloride ◽  
Biological Evaluation ◽  
Titanocene Dichloride ◽  
Synthesis And Biological Evaluation

Six new titanocene compounds have been isolated and characterised. These compounds were synthesised from their fulvene precursors using Super Hydride (LiBEt3H) followed by transmetallation with titanium tetrachloride to yield the corresponding titanocene dichloride derivatives. These complexes are bis-[((1-methyl-3-diethylaminomethyl)indol-2-yl)methylcyclopentadienyl] titanium (IV) dichloride (5a), bis-[((5-methoxy-1-methyl,3-diethylaminomethyl)indol-2-yl)methylcyclopentadienyl] titanium (IV) dichloride (5b), bis-[((1-methyl,3-diethylaminomethyl)indol-4-yl)methylcyclopentadienyl] titanium (IV) dichloride (5c), bis-[((5-bromo-1-methyl)indol-3-yl)methylcyclopentadienyl] titanium (IV) dichloride (5d), bis-[((5-chloro-1-methyl)indol-3-yl)methylcyclopentadienyl] titanium (IV) dichloride (5e), and bis-[((5-fluoro-1-methyl)indol-3-yl)methylcyclopentadienyl] titanium (IV) dichloride (5f). All six titanocenes 5a–5f were tested for their cytotoxicity through MTT-based in vitro tests on CAKI-1 cell lines using DMSO and Soluphor P as solubilising agents in order to determine their IC50 values. Titanocenes 5a–5f were found to have IC50 values of 10 (±2), 21 (±3), 29 (±4), 140 (±6), and 450 (±10) μM when tested using DMSO.

scholarly journals Use of 2-aminoprop-1-ene-1,1,3-tricarbonitrile for the synthesis of tetrahydronaphthalene, hexahydroisoquinoline and hexahydrocinnoline derivatives with potential antitumor activities

2011 ◽  
Vol 61 (1) ◽  
pp. 51-62 ◽  
Author(s):  
Rafat Mohareb ◽  
Hosam Moustafa
Keyword(s):  
Cell Lines ◽  
Antitumor Agents ◽  
Human Tumor ◽  
Breast Adenocarcinoma ◽  
Inhibitory Effects ◽  
Antitumor Activities ◽  
Chemical Reagents ◽  
Tumor Types ◽  
Potential Antitumor

Use of 2-aminoprop-1-ene-1,1,3-tricarbonitrile for the synthesis of tetrahydronaphthalene, hexahydroisoquinoline and hexahydrocinnoline derivatives with potential antitumor activities The aim of the work was to synthesize heterocyclic compounds from 2-aminoprop-1-ene-1,1,3-tricarbonitrile and to study their antitumor activities. The title reagent reacted with cyclohexanone to give the ethylidene derivative 2. The reactivity of the latter product towards different chemical reagents was studied to give tetrahydronaphthalene, hexahydroisoquinoline and hexahydrocinnoline derivatives. The newly synthesized products were screened as antitumor agents on the in vitro growth of three human tumor cell lines representing different tumor types, namely, breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268). It was found that some of these compounds showed inhibitory effects on the three cell lines, indicating their potential use in the development of oncology products.

scholarly journals Design, Synthesis, Molecular Docking, ADME and Biological Evaluation Studies of Some New 1,3,4-oxadiazole Linked Benzimidazoles as Anticancer Agents and Aromatase Inhibitors

2021 ◽  
Author(s):  
ulviye acar çevik ◽  
Ismail Celik ◽  
Ayşen IŞIK ◽  
Yusuf Özkay ◽  
Zafer Asım Kaplancıklı
Keyword(s):  
Molecular Docking ◽  
Cell Line ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Evaluation Studies ◽  
Biological Evaluation ◽  
Binding Modes ◽  
Anticancer Activities ◽  
Mcf 7

Abstract In this study, due to the potential anticancer effects of the benzimidazole ring system, a series of benzimidazole-1,3,4-oxadiazole derivatives were synthesized and characterized by 1H NMR, 13C NMR, and MS spectra analyses. In the in vitro anticancer assay, all the compounds tested anticancer activities using MTT-based assay against five cancer cell lines (MCF-7, A549, HeLa, C6, and HepG2). Among them, compound 5a exhibited the most potent activity with IC50 values of 5,165±0,211 μM and 5,995±0,264 μM against MCF-7 and HepG2 cell lines. Compound 5a was included in the BrdU test to determine the DNA synthesis inhibition effects for both cell types. Furthermore, compound 5c was also found to be more effective than doxorubicin on the HeLa cell line. The selectivity of anticancer activity was evaluated in NIH3T3 (mouse embryo fibroblast cell line) cell line. In vitro, enzymatic inhibition assays of aromatase enzyme were performed for compound 5a acting on the MCF-7 cell line. For compound 5a, in silico molecular docking against aromatase enzyme was performed to determine possible protein-ligand interactions and binding modes.

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