ChemInform Abstract: Design, Synthesis, and in vitro Antitumor Evaluation of Novel Diaryl Ureas Derivatives.

ChemInform ◽  
2010 ◽  
Vol 41 (40) ◽  
pp. no-no
Author(s):  
Min Sun ◽  
Xiaoqing Wu ◽  
Junqing Chen ◽  
Jin Cai ◽  
Meng Cao ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Antitumor Evaluation

scholarly journals Betulinic Acid-Nitrogen Heterocyclic Derivatives: Design, Synthesis, and Antitumor Evaluation in Vitro

Molecules ◽  
2020 ◽  
Vol 25 (4) ◽  
pp. 948
Author(s):  
Yuqin Yang ◽  
Tianxin Xie ◽  
Xuehao Tian ◽  
Nana Han ◽  
Xiaojing Liu ◽  
...  
Keyword(s):  
Betulinic Acid ◽  
Antitumor Agents ◽  
In Vitro Cytotoxicity ◽  
Design Synthesis ◽  
Pentacyclic Triterpenoid ◽  
Heterocyclic Derivatives ◽  
Staining Techniques ◽  
Antitumor Evaluation ◽  
Nitrogen Heterocyclic

Betulinic acid (BA) is a star member of the pentacyclic triterpenoid family, which exhibits great prospects for antitumor drug development. In an attempt to develop novel antitumor candidates, 21 BA-nitrogen heterocyclic derivatives were synthetized, in addition to four intermediates, 23 of which were first reported. Moreover, they were screened for in-vitro cytotoxicity against four tumor cell lines (Hela, HepG-2, BGC-823 and SK-SY5Y) by a standard methylthiazol tetrazolium (MTT) assay. The majority of these derivatives showed much stronger cytotoxic activity than BA. Remarkably, the most potent compound 7e (the half maximal inhibitory concentration (IC50) of which was 2.05 ± 0.66 μM) was 12-fold more toxic in vitro than BA-treated Hela. Furthermore, multiple fluorescent staining techniques and flow cytometry collectively revealed that compound 7e could induce the early apoptosis of Hela cells. Structure–activity relationships were also briefly discussed. The present study highlighted the importance of introducing nitrogen heterocyclic rings into betulinic acid in the discovery and development of novel antitumor agents.

Design, Synthesis, and In vitro Antitumor Evaluation of Novel Phenylaminopyrimidine Derivatives

2013 ◽  
Vol 9 (3) ◽  
pp. 340-350
Author(s):  
Youguang Zheng ◽  
Ming Zheng ◽  
Yi Liu ◽  
Yunsheng Xue ◽  
Ling Zhang ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Antitumor Evaluation

Design, synthesis, and in vitro antitumor evaluation of novel diaryl ureas derivatives

2010 ◽  
Vol 45 (6) ◽  
pp. 2299-2306 ◽  
Author(s):  
Min Sun ◽  
Xiaoqing Wu ◽  
Junqing Chen ◽  
Jin Cai ◽  
Meng Cao ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Antitumor Evaluation

Design, synthesis and in vitro antitumor evaluation of novel diaryl urea derivatives bearing sulfonamide moiety

2013 ◽  
Vol 56 (11) ◽  
pp. 1564-1572 ◽  
Author(s):  
Can Luo ◽  
Ke Tang ◽  
Yan Li ◽  
DaLi Yin ◽  
XiaoGuang Chen ◽  
...  
Keyword(s):  
Urea Derivatives ◽  
Design Synthesis ◽  
Antitumor Evaluation

Design, Synthesis, Molecular Docking and Biological Evaluation of 1-(benzo[d]thiazol-2-ylamino)(phenyl)methyl)naphthalen-2-ol Derivatives as Antiproliferative Agents

2019 ◽  
Vol 16 (10) ◽  
pp. 837-845
Author(s):  
Sandhya Jonnala ◽  
Bhaskar Nameta ◽  
Murthy Chavali ◽  
Rajashaker Bantu ◽  
Pallavi Choudante ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Chinese Hamster Ovary Cells ◽  
Chinese Hamster ◽  
Mouse Skin ◽  
Coupling Reaction ◽  
Binding Mode ◽  
Biological Evaluation ◽  
Design Synthesis

A class of 1-((benzo[d]thiazol-2-ylamino)(phenyl)methyl)naphthalen-2-ol derivatives (4a-t) has been synthesized in good yields through a three component coupling reaction. The newly synthesized compounds were evaluated for their in vitro antiproliferative activity against five cell lines such as DU145 (human prostate cancer), MDA-MB-B231 (human breast cancer), SKOV3 (human ovarian cancer), B16-F10 (mouse skin melanoma) and CHO-K1 (Chinese hamster ovary cells), a noncancerous cell line. In vitro inhibitory activity indicates that compounds 4a, 4b, 4c, 4d, 4g, 4j, and 4o exhibited potent anti-proliferative behavior. Among them, compounds 4g, 4j and 4o found to be the most active members exhibiting remarkable growth inhibitory activity. Molecular docking facilitates to investigate the probable binding mode and key active site interactions in tubulins α and β proteins. The docking results are complementary to experimental results.

Discovery of N-Phenyl-4-(1H-pyrrol-3-yl)pyrimidin-2-amine Derivatives as Potent Mnk2 Inhibitors: Design, Synthesis, SAR Analysis, and Evaluation of in vitro Anti-leukaemic Activity

2019 ◽  
Vol 15 (6) ◽  
pp. 602-623 ◽  
Author(s):  
Ahmed M. Abdelaziz ◽  
Sarah Diab ◽  
Saiful Islam ◽  
Sunita K.C. Basnet ◽  
Benjamin Noll ◽  
...  
Keyword(s):  
Proliferative Activity ◽  
Myeloid Cell ◽  
Structural Diversity ◽  
Translation Initiation Factor ◽  
Initiation Factor ◽  
Cell Leukaemia ◽  
Aberrant Expression ◽  
Design Synthesis ◽  
Induced Apoptosis

Background:Aberrant expression of eukaryotic translation initiation factor 4E (eIF4E) is common in many types of cancer including acute myeloid leukaemia (AML). Phosphorylation of eIF4E by MAPK-interacting kinases (Mnks) is essential for the eIF4E-mediated oncogenic activity. As such, the pharmacological inhibition of Mnks can be an effective strategy for the treatment of cancer.Methods:A series of N-phenyl-4-(1H-pyrrol-3-yl)pyrimidin-2-amine derivatives was designed and synthesised. The Mnk inhibitory activity of these derivatives as well as their anti-proliferative activity against MV4-11 AML cells was determined.Results:These compounds were identified as potent Mnk2 inhibitors. Most of them demonstrated potent anti-proliferative activity against MV4-11 AML cells. The cellular mechanistic studies of the representative inhibitors revealed that they reduced the level of phosphorylated eIF4E and induced apoptosis by down-regulating the anti-apoptotic protein myeloid cell leukaemia 1 (Mcl-1) and by cleaving poly(ADP-ribose)polymerase (PARP). The lead compound 7k possessed desirable pharmacokinetic properties and oral bioavailability.Conclusion:This work proposes that exploration of the structural diversity in the context of Nphenyl- 4-(1H-pyrrol-3-yl)pyrimidin-2-amine would offer potent and selective Mnk inhibitors.

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