scholarly journals Design, synthesis, and biological evaluation of quinazoline derivatives containing piperazine moieties as antitumor agents

2020 ◽  
Vol 44 (9-10) ◽  
pp. 536-542
Author(s):  
Wen Li ◽  
Shu-Yi Chen ◽  
Wei-Nan Hu ◽  
Mei Zhu ◽  
Jia-Min Liu ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Biological Evaluation ◽  
Substitution Reactions ◽  
Migration Ability ◽  
Design Synthesis ◽  
Excellent Activity ◽  
Quinazoline Derivatives ◽  
Synthesis And Biological Evaluation ◽  
Antiproliferative Activities

A series of novel quinazoline derivatives containing piperazine analogs are synthesized via substitution reactions with 6,7-disubstituted 4-chloroquinazoline and benzyl piperazine (amido piperazine). Potent antiproliferative activities are observed against A549, HepG2, K562, and PC-3 with N-(3-chlorophenyl)-2-(4-(7-methoxy-6-(3-morpholino-propoxy)quinazoline-4-yl)piperazine-1-yl)acetamidename C9 showing excellent activity. This active derivative was screened for cell migration ability, proliferation effects, and apoptosis against A549 and PC-3 cells, with the result showing biological activity almost equal to that of the control gefitinib.

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.

Design, synthesis and biological evaluation of novel 2,4-diaminopyrimidine derivatives as potent antitumor agents

2019 ◽  
Vol 43 (25) ◽  
pp. 10190-10202 ◽  
Author(s):  
Gang Hu ◽  
Chu Wang ◽  
Xin Xin ◽  
Shuaikang Li ◽  
Zefei Li ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Two series of 2-aminopyrimidine derivatives possessing triazolopiperazine or 1,4,8-triazaspiro[4.5]decan-3-one scaffolds were designed, synthesized and evaluated for their biological activity.

ChemInform Abstract: Antitumor Agents. Part 202. Novel 2′-Amino Chalcones: Design, Synthesis, and Biological Evaluation.

ChemInform ◽  
2010 ◽  
Vol 31 (29) ◽  
pp. no-no
Author(s):  
Yi Xia ◽  
Zheng-Yu Yang ◽  
Peng Xia ◽  
Kenneth F. Bastow ◽  
Yuka Nakanishi ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals Semisynthetic Analogs of the Antibiotic Fidaxomicin – Design, Synthesis, and Biological Evaluation

2020 ◽  
Author(s):  
Andrea Dorst ◽  
Regina Berg ◽  
Christoph Gertzen ◽  
Daniel Schäfle ◽  
katja zerbe ◽  
...  
Keyword(s):  
Structural Design ◽  
Water Solubility ◽  
Biological Evaluation ◽  
Protecting Group ◽  
Design Synthesis ◽  
Gram Positive Bacteria ◽  
Excellent Activity ◽  
One Step ◽  
Hybrid Antibiotics ◽  
Synthesis And Biological Evaluation

<p>The glycoslated macrocyclic antibiotic fidaxomicin (1, tiacumicin B, lipiarmycin A3) displays good to excellent activity against Gram-positive bacteria and was approved for the treatment of Clostridium difficile infections (CDI). Main limitations of the compound include low water solubility, which impacts further clinical use. We report on the synthesis of new fidaxomicin derivatives based on structural design and utilizing an operationally simple one-step protecting group-free preparative approach from the natural product. An increase in solubility of up to 25-fold with largely retained activity was observed. Furthermore, hybrid antibiotics were prepared that show improved antibiotic activities</p>

Design, synthesis and biological evaluation of thiourea and nicotinamide-containing sorafenib analogs as antitumor agents

MedChemComm ◽  
2015 ◽  
Vol 6 (5) ◽  
pp. 867-870 ◽  
Author(s):  
Xiangkai Kong ◽  
Zeyu Yao ◽  
Zuopeng He ◽  
Wenfang Xu ◽  
Jianwen Yao
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Thiourea and nicotinamide-containing sorafenib analogs with better antiproliferative and anti-angiogenic activities than sorafenib were well designed and synthesized.

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