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.

scholarly journals Design, synthesis and biological evaluation of tryptamine salicylic acid derivatives as potential antitumor agents

MedChemComm ◽  
2019 ◽  
Vol 10 (4) ◽  
pp. 573-583 ◽  
Author(s):  
Runde Xiong ◽  
Dongxiu He ◽  
Xiangping Deng ◽  
Juan Liu ◽  
Xiaoyong Lei ◽  
...  
Keyword(s):  
Gastric Cancer ◽  
Salicylic Acid ◽  
Antitumor Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Combination Principle ◽  
Salicylic Acid Derivatives ◽  
Synthesis And Biological Evaluation ◽  
Tumor Agent ◽  
Potential Antitumor

According to the combination principle, target compounds were designed, and compound E20 might be a promising anti-tumor agent targeting gastric cancer.

scholarly journals Design, Synthesis, and Biological Evaluation of Triazolyl- and Triazinyl-Quinazolinediones as Potential Antitumor Agents

2019 ◽  
Vol 2019 ◽  
pp. 1-12
Author(s):  
Abeer N. Al-Romaizan ◽  
Nesreen S. Ahmed ◽  
Sherin M. Elfeky
Keyword(s):  
Antitumor Agents ◽  
Human Colon ◽  
Biological Evaluation ◽  
Human Cell Lines ◽  
Hep G2 ◽  
Design Synthesis ◽  
Reference Drug ◽  
Human Colon Carcinoma ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor

Novel 6(3-1H-1,2,4-triazol-1-yl)-3-phenylquinazoline-2,4(1H,3H)-diones (7a–e) were synthesized from different enaminones (6a–e) with 6-hydrazinyl-3-phenylquinazoline-2,4(1H,3H)-dione. 2,6(4-2-Substituted-1,3,5-triazin-1(2H)-yl)-3-phenylquinazoline-2,4(1H,3H)-diones (8a–k) were synthesized from the reaction of 1-(2,4-dioxo-3-phenyl-1,2,3,4-tetrahydroquinazolin-6-yl)thiourea, urea, or guanidine (3a–c) with enaminones (6a–e), and a series from 3-substituted-2-imino-1,3,5-triazin-1(2H)-yl-sulfonyl-phenyl-1-methylquinazoline-2,4(1H,3H)-dione (12a–j) were obtained from the reaction of N-(diaminomethylene)-4-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)benzenesulfonamide (11) with the enaminone (6a–j). The antitumor activity of the synthesized compounds was evaluated against two human cell lines: human colon carcinoma HCT116 and human hepatocellular carcinoma HEP-G2. Some of the tested compounds showed significant potency compared to the reference drug staurosporin.

scholarly journals Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents

Molecules ◽  
2014 ◽  
Vol 19 (7) ◽  
pp. 10177-10188 ◽  
Author(s):  
Kaiyong Tang ◽  
Qingqing Huang ◽  
Jafeng Zeng ◽  
Guangming Wu ◽  
Jinwen Huang ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor

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%.

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