scholarly journals Synthesis and Evaluation of Novel Organogermanium Sesquioxides As Antitumor Agents

2009 ◽  
Vol 2009 ◽  
pp. 1-8 ◽  
Author(s):  
Chun Li Zhang ◽  
Tai Hua Li ◽  
Shuang Huan Niu ◽  
Rong Fu Wang ◽  
Zhan Li Fu ◽  
...  
Keyword(s):  
Reaction Time ◽  
Antitumor Activity ◽  
Elemental Analysis ◽  
Therapeutic Agent ◽  
Antitumor Agents ◽  
Uptake Ratio ◽  
Antitumor Activities ◽  
Normal Tissues ◽  
Tumor Clearance

Five new organogermanium sesquioxides have been synthesized and characterized by elemental analysis and IR spectra. All the compounds were tested for antitumor activities against KB, HCT, and Bel cells in vitro. Compound 5 (-thiocarbamido propyl germanium sesquioxide) showed excellent antitumor activity, and its inhibition yield to KB, HCT, and Bel cells was 92.9%, 84.9%, and 70.9%, respectively. A rapid method was described for the labeling compound 5 with , and the optimum labeling conditions were investigated. The labeling yield is above 90% in pH 7.0, , reaction time greater than 10 minutes, 1 mg of compound 5, and 0.0750.1 mg of . The biodistribution of labeled compound 5 in nude mice bearing human colonic xenografts was studied. The result showed that the tumor uptakes were 0.73, 0.97, 0.87, and 0.62 ID%/g at 1-hour, 3-hour, 6-hour, and 20-hour postinjection, respectively. T/NT (the uptake ratio for per gram of tumor over normal tissues) was 18.3 for tumor versus brain and 5.81 for tumor versus muscle at 20-hour postinjection. The tumor clearance was slow. The results showed that compound 5 may be developed to be a suitable cancer therapeutic agent.

scholarly journals Aspirin suppresses chemoresistance and enhances antitumor activity of 5-Fu in 5-Fu-resistant colorectal cancer by abolishing 5-Fu-induced NF-κB activation

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Jinbo Fu ◽  
Yiming Xu ◽  
Yushan Yang ◽  
Yun Liu ◽  
Lulu Ma ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Antitumor Activity ◽  
Therapeutic Agent ◽  
Inhibitory Effect ◽  
Antitumor Activities ◽  
Tumor Cell Apoptosis ◽  
Tumor Growth And Metastasis ◽  
Resistant Cells

AbstractChemoresistance to 5-fluorouracil (5-Fu)-based chemotherapy is a leading obstacle in achieving effective treatment for colorectal cancer (CRC). Typically, NF-κB activation induced by the chemotherapeutics themselves is an important cause resulting in chemoresistance. Specifically, NF-κB activation can inhibit tumor cell apoptosis and induce chemoresistance. Drugs that can prevent NF-κB activation induced by chemotherapeutics are urgently needed to overcome chemoresistance. Obviously, aspirin is one of these agents, which has been demonstrated to possess antitumor activities and as an inhibitor of NF-κB. The current study aimed to investigate whether aspirin was able to overcome the chemoresistance to 5-Fu in CRC, together with the potential synergistic mechanisms. Our results suggested that aspirin remarkably potentiated the inhibitory effect of 5-Fu on the growth and invasion of resistant cells in vitro. In vivo, aspirin markedly enhanced the antitumor activity of 5-Fu in suppressing tumor growth and metastasis, and down-regulating the expression of NF-κB-regulated genes in the 5-Fu-resistant cells. Obviously, aspirin completely eradicated the 5-Fu-induced NF-κB activation, without inducing pronounced adverse effects. Taken together, findings in this study suggest that aspirin can reverse chemoresistance and potentiate the antitumor effect of 5-Fu, which is achieved through abolishing the 5-Fu-induced NF-κB activation, suggesting that aspirin may be a promising adjuvant therapeutic agent for CRC.

Design, Syntheses and Biological Evaluation of 5-Fluoroindolin-2-One Derivatives with Urea Linkage

2013 ◽  
Vol 634-638 ◽  
pp. 926-929
Author(s):  
Bao Hua Zou ◽  
Zheng Fang ◽  
Zhao Yang ◽  
Kai Guo
Keyword(s):  
Antitumor Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Positive Control ◽  
Biological Evaluation ◽  
Antitumor Activities ◽  
Mtt Method ◽  
Antitumor Bioactivity ◽  
Better Than

Nine 5-fluoroindolin-2-one derivatives with urea linkage were designed and synthesized. The obtained structures were identified by 1H NMR, MS and elemental analysis. In vitro evaluation of antitumor bioactivity was performed by MTT method. Most of synthesized compounds showed antitumor activities, especially, compounds 6e and 6f, which were better than or equal to the antitumor activity of positive control.

scholarly journals Recent Advances in Improved Anticancer Efficacies of Camptothecin Nano-Formulations: A Systematic Review

Biomedicines ◽  
2021 ◽  
Vol 9 (5) ◽  
pp. 480
Author(s):  
Maryam Ghanbari-Movahed ◽  
Tea Kaceli ◽  
Arijit Mondal ◽  
Mohammad Hosein Farzaei ◽  
Anupam Bishayee
Keyword(s):  
Systematic Review ◽  
Antitumor Activity ◽  
Cancer Treatment ◽  
Topoisomerase I ◽  
Antitumor Agents ◽  
Critical Evaluation ◽  
Antitumor Activities ◽  
Passive Targeting

Camptothecin (CPT), a natural plant alkaloid, has indicated potent antitumor activities via targeting intracellular topoisomerase I. The promise that CPT holds in therapies is restricted through factors that include lactone ring instability and water insolubility, which limits the drug oral solubility and bioavailability in blood plasma. Novel strategies involving CPT pharmacological and low doses combined with nanoparticles have indicated potent anticancer activity in vitro and in vivo. This systematic review aims to provide a comprehensive and critical evaluation of the anticancer ability of nano-CPT in various cancers as a novel and more efficient natural compound for drug development. Studies were identified through systematic searches of PubMed, Scopus, and ScienceDirect. Eligibility checks were performed based on predefined selection criteria. Eighty-two papers were included in this systematic review. There was strong evidence for the association between antitumor activity and CPT treatment. Furthermore, studies indicated that CPT nano-formulations have higher antitumor activity in comparison to free CPT, which results in enhanced efficacy for cancer treatment. The results of our study indicate that CPT nano-formulations are a potent candidate for cancer treatment and may provide further support for the clinical application of natural antitumor agents with passive targeting of tumors in the future.

scholarly journals Synthesis, biological evaluation, and molecular docking of ((4-([1,2,4]triazolo[4,3-b][1,2,4,5]tetrazin-6-yl) piperazin-1-yl)methyl) benzohydrazide derivatives

2020 ◽  
Vol 44 (9-10) ◽  
pp. 543-550
Author(s):  
Xiaoyu Wu ◽  
Feng Xu ◽  
Zhenzhen Yang ◽  
Zhonglu Ke ◽  
Lei Shi ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antitumor Activity ◽  
Tumor Cells ◽  
Elemental Analysis ◽  
Biological Evaluation ◽  
Significant Inhibition ◽  
Antitumor Activities ◽  
H Nmr ◽  
C Nmr

A series of ((4-([1,2,4]triazolo[4,3- b][1,2,4,5] methyl) benzo-hydrazide derivatives was designed, synthesized, and evaluated for their inhibition activities against five tumor cells and c-Met kinase in vitro. These compounds were fully characterized by 1H NMR, 13C NMR, MS, and elemental analysis. Antitumor experiments indicated that some compounds exhibited significant inhibition activities against A549 and Bewo. Especially, the IC50 values of 5f (12 μM), 5h (7.1 μM), 6a (8.4 μM), and 6d (9.2 μM) demonstrated better antitumor activities against A549 than the positive agent cisplatin (13.3 μM), and the IC50 value of 6a (5.2 μM) exhibited better antitumor activity against Bewo than cisplatin (7.7 μM).

Synthesis and In Vitro Anti-HCV and Antitumor Evaluation of Schisan-dronic acid derivatives

2020 ◽  
Vol 16 ◽  
Author(s):  
Kai-Xia Zhang ◽  
Xi-Jing Qian ◽  
Wei-Zheng ◽  
Meng-Cheng Cai ◽  
Ying Ma ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Antitumor Activities ◽  
Lead Compounds ◽  
Huh7 Cells ◽  
Derivatives Of ◽  
Hcvcc Infection ◽  
Antitumor Evaluation ◽  
Entry Inhibition

Background: Schisandronic acid (SA), a triterpenoid from fruits of Schisandra sphenanthera, inhibited pan-genotypic HCV entry into human hepatocytes by interfering with virion-cell membrane fusion. It was a promising lead compound for development of novel HCV entry inhibition agents. Objective: To search for compounds with more potent anti-HCV and antitumor activities and explore SARs, a series of nov-el derivatives of SA were designed and synthesized and evaluated for in vitro their anti-HCV and antitumor activities. Methods: SA derivatives were synthesized by reduction, condensation, esterification or amidation. The anti-HCV activity of title compounds was tested by inhibition on HCVcc infection of Huh7 cells, and preliminary MOA study was conducted by determining inhibition on HCVpp entry into Huh7 cells. The antitumor activity in vitro was determined by MTT methods. Results: Totally 24 novel derivatives were synthesized. Most of the compounds inhibited HCVcc infection. Compounds 5hand 6 showed most potent anti-HCVcc activities and inhibition of HCVpp entry into Huh7 cells without obvious cytotoxici-ty. Most of title compounds showed potent in vitro antitumor activities against Bel7404 and SMMC7721 tumor cell lines. Compounds 5j and 6 exhibited more potent antitumor activity than positive controlSA and DOX. Conclusion: Structural modification of SA could lead to the discovery of potent anti-HCV or antitumor agents. Compounds 5h, 5j and 6 werepromising lead compounds development of novel HCV entry inhibition or antitumor agents.

Synthesis and Antitumor Activity Evaluation of New Phenanthrene-Based Tylophorine Derivatives

2019 ◽  
Vol 16 (6) ◽  
pp. 462-467
Author(s):  
Songtao Li ◽  
Hongling Zhao ◽  
Zhifeng Yin ◽  
Shuhua Deng ◽  
Yang Gao ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Antitumor Activities ◽  
Human Carcinoma ◽  
Carcinoma Cell Lines ◽  
Structure Activity ◽  
Human Carcinoma Cell ◽  
Ic50 Values ◽  
Relationship Of

A series of new phenanthrene-based tylophorine derivatives (PBTs) were synthesized in good yield and their structures were characterized by 1H-NMR spectroscopy and ESI MS. In vitro antitumor activity of these compounds against five human carcinoma cell lines, including HCT116 (colorectal), BGC-823 (gastric), HepG-2 (hepatic), Hela (cervical) and H460 (lung) cells, was evaluated by MTT assay. Among these PBTs, compound 6b showed the highest antitumor activities against HCT116 and HepG-2 cell lines with IC50 values of 6.1 and 6.4 μM, respectively, which were comparable to that of adriamycin hydrochloride. The structure-activity relationship of these compounds was also discussed based on the results of their antitumor activity.

scholarly journals Design, Synthesis, Molecular Modeling and Antitumor Evaluation of Novel Indolyl-Pyrimidine Derivatives with EGFR Inhibitory Activity

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1838
Author(s):  
Naglaa M. Ahmed ◽  
Mahmoud M. Youns ◽  
Moustafa K. Soltan ◽  
Ahmed M. Said
Keyword(s):  
Molecular Modeling ◽  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Antitumor Agents ◽  
Cancer Cell Lines ◽  
Normal Cells

Scaffolds hybridization is a well-known drug design strategy for antitumor agents. Herein, series of novel indolyl-pyrimidine hybrids were synthesized and evaluated in vitro and in vivo for their antitumor activity. The in vitro antiproliferative activity of all compounds was obtained against MCF-7, HepG2, and HCT-116 cancer cell lines, as well as against WI38 normal cells using the resazurin assay. Compounds 1–4 showed broad spectrum cytotoxic activity against all these cancer cell lines compared to normal cells. Compound 4g showed potent antiproliferative activity against these cell lines (IC50 = 5.1, 5.02, and 6.6 μM, respectively) comparable to the standard treatment (5-FU and erlotinib). In addition, the most promising group of compounds was further evaluated for their in vivo antitumor efficacy against EAC tumor bearing mice. Notably, compound 4g showed the most potent in vivo antitumor activity. The most active compounds were evaluated for their EGFR inhibitory (range 53–79 %) activity. Compound 4g was found to be the most active compound against EGFR (IC50 = 0.25 µM) showing equipotency as the reference treatment (erlotinib). Molecular modeling study was performed on compound 4g revealed a proper binding of this compound inside the EGFR active site comparable to erlotinib. The data suggest that compound 4g could be used as a potential anticancer agent.

scholarly journals Design, synthesis and pharmacological evaluation of novel 2-chloro-3-(1H-benzo[d]imidazol-2-yl)quinoline derivatives as antitumor agents: in vitro and in vivo antitumor activity, cell cycle arrest and apoptotic response

RSC Advances ◽  
2018 ◽  
Vol 8 (43) ◽  
pp. 24376-24385 ◽  
Author(s):  
Wen-Bin Kuang ◽  
Ri-Zhen Huang ◽  
Yi-Lin Fang ◽  
Gui-Bin Liang ◽  
Chen-Hui Yang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Quinoline Derivatives ◽  
Apoptotic Response ◽  
Design Synthesis ◽  
Cycle Arrest ◽  
In Vivo Antitumor Activity ◽  
Combination Principle

A series of novel 2-chloro-3-(1H-benzo[d]imidazol-2-yl)quinoline derivatives were designed and synthesized as antitumor agents under the combination principle. The antitumor activity and mechanisms were then evaluated.

Bimetallic DppfM(II) (M = Pt and Pd) dithiocarbamate complexes: Synthesis, characterization, and anticancer activity

2019 ◽  
Vol 43 (9-10) ◽  
pp. 437-442 ◽  
Author(s):  
Shou De Xu ◽  
Xiang Hua Wu
Keyword(s):  
Antitumor Activity ◽  
Platinum Complex ◽  
Spectroscopic Methods ◽  
X Ray Diffraction ◽  
Antitumor Activities ◽  
High Potency ◽  
Promising Candidate ◽  
X Ray ◽  
Mtt Assays

A series of bimetallic dppfM(II) (dppf = 1,1’-bis (diphenyphosphino) ferrocene; M = Pt and Pd) dithiocarbamate complexes is synthesized and characterized by spectroscopic methods and single-crystal X-ray diffraction. Their antitumor activities in vitro are investigated by MTT assays against four cancer cell lines. The anticancer studies indicate most of the complexes display good to excellent antitumor activity. Remarkably, the platinum complex with a pyrrolidinyl substituent (3b) was identified as the most promising candidate due to its high potency and broad spectrum of activity.

scholarly journals Two groups of copperII pyridine–triazole complexes with “open or close” pepper rings and their in vitro antitumor activities

RSC Advances ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 6297-6305
Author(s):  
ZhaoGuo Hong ◽  
Chu Zheng ◽  
Bi Luo ◽  
Xin You ◽  
HeDong Bian ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cancer Cells ◽  
Antitumor Activities ◽  
Group I ◽  
Group Ii

The pepper ring-modified complexes (Group II, C4–C6) exhibited significant antitumor activity than veratrole-modified complexes (Group I, C1–C3) towards several cancer cells with IC50 ranging from 3.45 to 8.59 μM.

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