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%.

Synthesis and biological evaluation of piperazine group-linked bivalent β-carbolines as potential antitumor agents

MedChemComm ◽  
2015 ◽  
Vol 6 (12) ◽  
pp. 2170-2174 ◽  
Author(s):  
Rongqin Sun ◽  
Rui Liu ◽  
Chi Zhou ◽  
Zhenghua Ren ◽  
Liang Guo ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Antitumor Agents ◽  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor

A series of bivalent β-carbolines with a piperazine group spacer between 3-methylene units were synthesized and their cytotoxic activities in vitro were evaluated. Compounds 7e and 7g exhibited potent cytotoxic activity.

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.

Strong In Vitro And Vivo Cytotoxicity Of Two Platinum(II) Complexes With Cryptolepine Derivatives

2021 ◽  
Author(s):  
Li-Qin Qin ◽  
Zu-Zhuang Wei ◽  
Lin Yang ◽  
Qi-Pin Qin ◽  
Jia-Jing Zeng ◽  
...  
Keyword(s):  
Mitochondrial Dysfunction ◽  
Cancer Cells ◽  
Cell Apoptosis ◽  
Antitumor Agents ◽  
Cytotoxic Activities ◽  
Antitumor Activities ◽  
Branched Chain ◽  
Potential Antitumor

Abstract Two mononuclear Pt(II) compounds, [Pt(BQL1)Cl]Cl (BQL1-Pt) and [Pt(BQL2)Cl]Cl (BQL2-Pt) with [5-(benzo[4,5]furo[3,2-b]quinolin-11-yloxy)-pentyl]-bis-pyridin-2-ylmethyl-amine (BQL1) and [9-(benzo[4,5]furo[3,2-b]quinolin-11-yloxy)-nonyl]-bis-pyridin-2-ylmethyl-amine (BQL2), were prepared as new chemotypes for potential antitumor agents. This study evaluated the influence of cryptolepine derivatives in BQL1-Pt, 2,2′-dipicolylamine Pt(II) complex, and BQL2-Pt on cellular Pt(II) accumulation, cytotoxicity, and in vitro and in vivo antitumor activities against T-24 cancer cells and normal HL-7702 cells. BQL1-Pt and BQL2-Pt displayed cytotoxic activities in the micromole range (1.3±0.1 and 0.2±0.2 μM, respectively) on T-24 cancer cells; however, they did not exhibit any toxicity against HL-7702 cells. They triggered T-24 cell apoptosis through a mitochondrial dysfunction pathway. Compared to 2,2′-dipicolylamine, the neutral BQL1 and BQL2 ligands with cryptolepine derivatives increased the planarity and branched chain resulting in BQL1-Pt and BQL2-Pt with favorable antitumor activities. Further, BQL2-Pt effectively inhibited the growth of bladder T-24 tumor in vivo. BQL2-Pt can act as a potential therapeutic candidate for cancer treatment.

Design, synthesis and biological evaluation of C(6)-indole celastrol derivatives as potential antitumor agents

RSC Advances ◽  
2015 ◽  
Vol 5 (25) ◽  
pp. 19620-19623 ◽  
Author(s):  
Kaiyong Tang ◽  
Jinwen Huang ◽  
Junfang Pan ◽  
Xuan Zhang ◽  
Wei Lu
Keyword(s):  
Cancer Cells ◽  
Antitumor Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
New Class ◽  
Synthesis And Biological Evaluation ◽  
Antiproliferative Activities ◽  
Potential Antitumor

A new class of C(6)-indole substituted celastrol derivatives were designed and synthesized. Among all these synthesized molecules, compound 4f and 4h displayed excellent in vitro antiproliferative activities against Bel7402 cancer cells.

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.

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.

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.

Synthesis and Biological Evaluation of Diaryl Ether Linked DC-81 Conjugates as Potential Antitumor Agents

2013 ◽  
Vol 13 (10) ◽  
pp. 1590-1600 ◽  
Author(s):  
Ahmed Kamal ◽  
A. Viswanath ◽  
M. Ramaiah ◽  
J. Murty ◽  
Farheen Sultana ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Diaryl Ether ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor
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