Novel Podophyllotoxin Derivatives as Potential Tubulin Inhibitors: Design, Synthesis, and Antiproliferative Activity Evaluation

2018 ◽  
Vol 15 (11) ◽  
pp. e1800289 ◽  
Author(s):  
Hong-Wei Han ◽  
Hong-Yan Lin ◽  
De-Liu He ◽  
Yao Ren ◽  
Wen-Xue Sun ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Design Synthesis ◽  
Tubulin Inhibitors ◽  
Activity Evaluation ◽  
Podophyllotoxin Derivatives

Design, synthesis and antiproliferative activity evaluation of fluorine-containing chalcone derivatives

2020 ◽  
pp. 1-26
Author(s):  
Serdar Burmaoglu ◽  
Derya Aktas Anil ◽  
Arzu Gobek ◽  
Deryanur Kilic ◽  
Derya Yetkin ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Design Synthesis ◽  
Chalcone Derivatives ◽  
Activity Evaluation

scholarly journals Design, synthesis and biological evaluation of novel nitric oxide-donating podophyllotoxin derivatives as potential antiproliferative agents against multi-drug resistant leukemia cells

RSC Advances ◽  
2018 ◽  
Vol 8 (60) ◽  
pp. 34266-34274 ◽  
Author(s):  
Lei Zhang ◽  
Ying Rong ◽  
Jie Zheng ◽  
Chengli Yang ◽  
Yongzheng Chen ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Antiproliferative Activity ◽  
Biological Evaluation ◽  
Leukemia Cells ◽  
Drug Resistant ◽  
Design Synthesis ◽  
Antiproliferative Agents ◽  
Podophyllotoxin Derivatives ◽  
Synthesis And Biological Evaluation

Conjugate S1 exhibited potential antiproliferative activity against multi-drug resistant leukemia cells.

Design, Synthesis and Antiproliferative Activity Evaluation of New 5-Azaisoindigo Derivatives

Heterocycles ◽  
2014 ◽  
Vol 89 (8) ◽  
pp. 1923 ◽  
Author(s):  
Zhenmin Mao ◽  
Ping Zhao ◽  
Yun Yan ◽  
Yanzhong Li ◽  
Aiying Zhang ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Design Synthesis ◽  
Activity Evaluation

Tubulin Inhibitors Binding to Colchicine-Site: A Review from 2015 to 2019

2020 ◽  
Vol 27 (40) ◽  
pp. 6787-6814 ◽  
Author(s):  
Lin-Ying Xia ◽  
Ya-Liang Zhang ◽  
Rong Yang ◽  
Zhong-Chang Wang ◽  
Ya-Dong Lu ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Structural Features ◽  
Design Synthesis ◽  
Antiproliferative Effects ◽  
Tubulin Inhibitors ◽  
Relationship Of ◽  
Podophyllotoxin Derivatives

Due to the three domains of the colchicine-site which is conducive to the combination with small molecule compounds, colchicine-site on the tubulin has become a common target for antitumor drug development, and accordingly, a large number of tubulin inhibitors binding to the colchicine-site have been reported and evaluated over the past years. In this study, tubulin inhibitors targeting the colchicine-site and their application as antitumor agents were reviewed based on the literature from 2015 to 2019. Tubulin inhibitors were classified into ten categories according to the structural features, including colchicine derivatives, CA-4 analogs, chalcone analogs, coumarin analogs, indole hybrids, quinoline and quinazoline analogs, lignan and podophyllotoxin derivatives, phenothiazine analogs, N-heterocycle hybrids and others. Most of them displayed potent antitumor activity, including antiproliferative effects against Multi-Drug-Resistant (MDR) cell lines and antivascular properties, both in vitro and in vivo. In this review, the design, synthesis and the analysis of the structure-activity relationship of tubulin inhibitors targeting the colchicine-site were described in detail. In addition, multi-target inhibitors, anti-MDR compounds, and inhibitors bearing antitumor activity in vivo are further listed in tables to present a clear picture of potent tubulin inhibitors, which could be beneficial for medicinal chemistry researchers.

Design, synthesis and antiproliferative activity evaluation of m -(4-morpholinyl-1,3,5-triazin-2-yl)benzamides in vitro

2015 ◽  
Vol 25 (8) ◽  
pp. 1730-1735 ◽  
Author(s):  
Xiao-Meng Wang ◽  
Jing Xu ◽  
Min-Hang Xin ◽  
She-Min Lu ◽  
San-Qi Zhang
Keyword(s):  
Antiproliferative Activity ◽  
Design Synthesis ◽  
Activity Evaluation

Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives

2020 ◽  
Vol 30 (12) ◽  
pp. 127194 ◽  
Author(s):  
Hao-Yue Xiang ◽  
Yan-Hong Chen ◽  
Yi Wang ◽  
Xi Zhang ◽  
Jian Ding ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Design Synthesis ◽  
Activity Evaluation ◽  
Triazine Derivatives

Design, Synthesis, in vitro Antiproliferative Activity Evaluation of 2-Acylaminothiopene-3-carboxamide Derivatives

Heterocycles ◽  
2016 ◽  
Vol 92 (12) ◽  
pp. 2145
Author(s):  
Jie Tang ◽  
Jiefeng Zhang ◽  
Fengjie Guan ◽  
Jiakun Qiu ◽  
Yanfen Fang ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Design Synthesis ◽  
Activity Evaluation

Design, Synthesis, and In Vitro Evaluation of Tubulin‐targeting Dibenzothiazines with Antiproliferative Activity as Novel Heterocycle Building Block

ChemMedChem ◽  
2021 ◽  
Author(s):  
Walter Damián Guerra ◽  
Daniel Lucena-Agell ◽  
Rafael Hortigüela ◽  
Roberto Arturo Rossi ◽  
J. Fernando Díaz ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Building Block ◽  
Design Synthesis ◽  
In Vitro Evaluation

Semi-synthesis and anti-lung cancer activity evaluation of aryl dihydrothiazol acyl podophyllotoxin ester derivatives

RSC Advances ◽  
2015 ◽  
Vol 5 (35) ◽  
pp. 27775-27784 ◽  
Author(s):  
Hong-Yan Lin ◽  
Li-Fei Bai ◽  
Fang Wang ◽  
Xun Wu ◽  
Lu-Jing Han ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Anticancer Agent ◽  
Tubulin Polymerization ◽  
Inhibition Effect ◽  
Activity Evaluation ◽  
Podophyllotoxin Derivatives ◽  
Cancer Activity

S12, the best anticancer agent among the 17 podophyllotoxin derivatives, showed a proliferative inhibition effect via inhibiting tubulin polymerization.

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