scholarly journals Design, Synthesis, and Preliminary Antitumor Activity Evaluation of Novel Alkaloid Derivatives

2020 ◽  
Vol 15 (2) ◽  
pp. 1934578X2090353
Author(s):  
Li-Jiao Wang ◽  
Zhi-Xing Cao ◽  
Li Guo
Keyword(s):  
Antitumor Activity ◽  
Scaffold Hopping ◽  
Antitumor Activities ◽  
Design Synthesis ◽  
Tetrazolium Bromide ◽  
Activity Evaluation ◽  
H460 Cells

A novel alkaloid scaffold was designed through scaffold-hopping strategy based on the active pyrazines alkaloid isolated previously. A total of 25 derivatives were synthesized based on this scaffold and evaluated for their antitumor activities. Among all these tested compounds, 9f exhibited most excellent antitumor activities toward H460 cells, TMD-8 cells, and MV4-11 cells in vitro by 3-(4, 5-dimethyl-2-thiazolyl)-2,5-diphenyl-2 H-tetrazolium bromide assay with IC50 values of 29.8, 14.9, and 18.8 μM, respectively.

scholarly journals Design, Synthesis, and In vitro Antitumor Activity Evaluation of Novel 4-pyrrylamino Quinazoline Derivatives

2011 ◽  
Vol 78 (6) ◽  
pp. 932-940 ◽  
Author(s):  
Xiaoqing Wu ◽  
Mingdong Li ◽  
Wenhua Tang ◽  
Youguang Zheng ◽  
Jiqin Lian ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Design Synthesis ◽  
Activity Evaluation ◽  
Quinazoline Derivatives

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.

Design, synthesis, and antitumor activity evaluation of steroidal oximes

2021 ◽  
pp. 116360
Author(s):  
Ana R. Gomes ◽  
Ana S. Pires ◽  
Ana M. Abrantes ◽  
Ana C. Gonçalves ◽  
Saul C. Costa ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Design Synthesis ◽  
Activity Evaluation

Design, synthesis and antitumor activity evaluation of novel HDAC inhibitors with tetrahydrobenzothiazole as the skeleton

2021 ◽  
Vol 108 ◽  
pp. 104652
Author(s):  
Simin Sun ◽  
Wenwen Zhao ◽  
Yongliang Li ◽  
Ziwei Chi ◽  
Xixi Fang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Hdac Inhibitors ◽  
Design Synthesis ◽  
Activity Evaluation

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.

scholarly journals Chloroquine Urea Derivatives: Synthesis and Antitumor Activity in Vitro

2018 ◽  
Vol 68 (4) ◽  
pp. 471-483 ◽  
Author(s):  
Kristina Pavić ◽  
Zrinka Rajić ◽  
Zvonimir Mlinarić ◽  
Lidija Uzelac ◽  
Marijeta Kralj ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Urea Derivatives ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Lead Compounds ◽  
Insight Into

Abstract In the current paper, we describe the design, synthesis and antiproliferative screening of novel chloroquine derivatives with a quinoline core linked to a hydroxy or halogen amine through a flexible aminobutyl chain and urea spacer. Synthetic pathway leading to chloroquine urea derivatives 4-10 includes two crucial steps: i) synthesis of chloroquine benzotriazolide 3 and ii) formation of urea derivatives through the reaction of compound 3 with the corresponding amine. Testing of antiproliferative activity against four human cancer cell lines revealed that chloroquine urea derivatives 9 and 10 with aromatic moieties show activity at micromolar concentrations. Therefore, these molecules represent interesting lead compounds that might provide an insight into the design of new anticancer agents.

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.

Sign in / Sign up

Export Citation Format

Share Document