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.

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.

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 dihydro-2-quinolone platinum(iv) hybrids as antitumor agents displaying mitochondria injury and DNA damage mechanism

2021 ◽  
Vol 50 (1) ◽  
pp. 362-375
Author(s):  
Zhifang Liu ◽  
Zuojie Li ◽  
Tao Du ◽  
Yan Chen ◽  
Qingpeng Wang ◽  
...  
Keyword(s):  
Dna Damage ◽  
Antitumor Agents ◽  
Cisplatin Resistance ◽  
Damage Mechanism ◽  
Biological Evaluation ◽  
Antitumor Activities ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Dihydro-2-quinolone platinum(iv) hybrids exhibit effective antitumor activities by causing serious mitochondria injury and DNA damage, and show great potential in reversing cisplatin resistance and improving antitumor efficacies.

Synthesis and biological evaluation of novel bivalent β-carbolines as potential antitumor agents

MedChemComm ◽  
2014 ◽  
Vol 5 (7) ◽  
pp. 953-957 ◽  
Author(s):  
Qifeng Wu ◽  
Zhushuang Bai ◽  
Qin Ma ◽  
Wenxi Fan ◽  
Liang Guo ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Lewis Lung ◽  
Lewis Lung Cancer ◽  
Synthesis And Biological Evaluation ◽  
Tumor Inhibition Rate ◽  
Potential Antitumor

A series of bivalent β-carbolines with a spacer between the 3-carboxyl oxygens was synthesized and their cytotoxic activities in vitro and antitumor efficacies in vivo were evaluated. Compound 22 exhibited potent antitumor activity against Lewis lung cancer in mice with a tumor inhibition rate of 64.2%.

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.

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]

2017 ◽  
Vol 46 (21) ◽  
pp. 7005-7019 ◽  
Author(s):  
Benjamin W. J. Harper ◽  
Emanuele Petruzzella ◽  
Roman Sirota ◽  
Fernanda Fabiola Faccioli ◽  
Janice R. Aldrich-Wright ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Synthesis and biological evaluation in vitro and in vivo of functionalized Pt(iv) derivatives of Pt56MeSS.

scholarly journals Design, Synthesis and Biological Evaluation of Novel 1, 3, 4-Oxadiazole Bearing Pyridine Moiety

2019 ◽  
pp. 300-307
Author(s):  
Asma D. Ambekari ◽  
Shrinivas K. Mohite
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Pyridine Moiety ◽  
Anti Inflammatory ◽  
Physicochemical Data ◽  
Synthesis And Biological Evaluation

Series of novel substituted Synthesis of N-{[5-(substituted)-1,3,4-oxadiazole-2-yl] carbamothioyl} derivatives containing 1,3,4-oxadiazole moiety were synthesized by microwave as a green chemistry method and conventional method by using pyridine 3- carboxylic acid as a starting material. The structures of the synthesized compounds were characterized by physicochemical data, IR, Mass spectra and 1HNMR. All the newly synthesized compound screened for their antimicrobial and In-vivo and In-vitro Anti-inflammatory studies. Anti-inflammatory studies revealed that compound 4f showed significant in-vivo and in-vitro anti-inflammatory activity as well potent antimicrobial activity.

scholarly journals Synthesis and Biological Evaluation of O-[3-18F-fluoropropyl]-α-methyl Tyrosine in Mesothelioma-Bearing Rodents

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
I-Hong Shih ◽  
Fan-Lin Kong ◽  
Mohammad S. Ali ◽  
Yinhan Zhang ◽  
Dong-Fang Yu ◽  
...  
Keyword(s):  
Radiochemical Purity ◽  
Biological Evaluation ◽  
Synthesis Methods ◽  
Automated Synthesis ◽  
Imaging Studies ◽  
Biodistribution Studies ◽  
Synthesis And Biological Evaluation ◽  
Automated Methods

Radiolabeled tyrosine analogs enter cancer cells via upregulated amino acid transporter system and have been shown to be superior to18F-fluoro-2-deoxy-D-glucose (18F-FDG) in differential diagnosis in cancers. In this study, we synthesized O-[3-19F-fluoropropyl]-α-methyl tyrosine (19F-FPAMT) and used manual and automated methods to synthesize O-[3-18F-fluoropropyl]-α-methyl tyrosine (18F-FPAMT) in three steps: nucleophilic substitution, deprotection of butoxycarbonyl, and deesterification. Manual and automated synthesis methods produced18F-FPAMT with a radiochemical purity >96%. The decay-corrected yield of18F-FPAMT by manual synthesis was 34% at end-of-synthesis (88 min). The decay-corrected yield of18F-FPAMT by automated synthesis was 15% at end-of-synthesis (110 min).18F-FDG and18F-FPAMT were used forin vitroandin vivostudies to evaluate the feasibility of18F-FPAMT for imaging rat mesothelioma (IL-45).In vitrostudies comparing18F-FPAMT with18F-FDG revealed that18F-FDG had higher uptake than that of18F-FPAMT, and the uptake ratio of18F-FPAMT reached the plateau after being incubated for 60 min. Biodistribution studies revealed that the accumulation of18F-FPAMT in the heart, lungs, thyroid, spleen, and brain was significantly lower than that of18F-FDG. There was poor bone uptake in18F-FPAMT for up to 3 hrs suggesting itsin vivostability. The imaging studies showed good visualization of tumors with18F-FPAMT. Together, these results suggest that18F-FPAMT can be successfully synthesized and has great potential in mesothelioma imaging.

Synthesis and biological evaluation of clovamide analogues as potent anti-neuroinflammatory agents in vitro and in vivo

2018 ◽  
Vol 151 ◽  
pp. 261-271 ◽  
Author(s):  
Xiao-Long Hu ◽  
Jun Lin ◽  
Xian-Yu Lv ◽  
Jia-Hao Feng ◽  
Xiao-Qi Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Synthesis And Biological Evaluation
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