Antitumor Agents. 192. Antitubulin Effect and Cytotoxicity of C(7)-Oxygenated Allocolchicinoids

1999 ◽  
Vol 64 (2) ◽  
pp. 217-228 ◽  
Author(s):  
Jian Guan ◽  
Xiao-Kang Zhu ◽  
Arnold Brossi ◽  
Yoko Tachibana ◽  
Kenneth F. Bastow ◽  
...  
Keyword(s):  
Cell Lines ◽  
Antitumor Agents ◽  
Human Tumor ◽  
Crystallographic Analysis ◽  
Antitumor Activities ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
X Ray ◽  
Tubulin Binding ◽  
Marked Resistance

Two allocolchicinoids 6 and 8, prepared from colchicine, together with allo compounds 9-11, made from 6 by reduction and regiodemethylation, were evaluated for antitubulin and antitumor activities. Structures of 6, 8, and 10 were confirmed by X-ray crystallographic analysis. Compounds 6, 8, and 9 have high tubulin binding affinity and display potent inhibitory activities against tubulin polymerization and solid human tumor cell lines. Particularly, drug-resistant KB cell lines, including KB-7d, KB-VCR, and KB-CPT, do not show marked resistance to these compounds.

Expression of ribosomal phosphoprotein PO is induced by antitumor agents and increased in Mer− human tumor cell lines

1992 ◽  
Vol 13 (2) ◽  
pp. 259-263 ◽  
Author(s):  
David T. Grabowski ◽  
Russell O. Pieper ◽  
Bernie W. Futscher ◽  
Walter A. Deutsch ◽  
Leonard C. Erickson ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Antitumor Agents ◽  
Human Tumor ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

scholarly journals Triterpenoids from Schisandra propinqua var. propinqua

2016 ◽  
Vol 11 (7) ◽  
pp. 1934578X1601100
Author(s):  
Miao Liu ◽  
Jun Wan ◽  
Yuan-Qing Luo ◽  
Xiao-Nian Li ◽  
Xue Du ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Tumor ◽  
Mass Spectrometric ◽  
Cytotoxic Activities ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
X Ray ◽  
Weak Activity ◽  
Stems And Leaves

Four new triterpenoids, propindilactone T (1), propindilactone U (2), changnanic acid 3-methyl ester (3) and schipropinic acid (4), together with five known ones (5-9), were isolated and identified from the stems and leaves of Schisandra propinqua var. propinqua; their structures were determined based on spectroscopic and mass spectrometric analyses. The absolute configuration of 1 was confirmed by X-ray analysis. Compounds 1, 2, and 4-9 were tested for their cytotoxic activities against five human tumor cell lines; all were inactive except for 8, which showed weak activity against some of the cell lines.

Plant Antitumor Agents. 31.1 The Calycopterones, a New Class of Biflavonoids with Novel Cytotoxicity in a Diverse Panel of Human Tumor Cell Lines

1994 ◽  
Vol 37 (10) ◽  
pp. 1465-1470 ◽  
Author(s):  
Monroe E. Wall ◽  
Mansukh C. Wani ◽  
Fekadu Fullas ◽  
John B. Oswald ◽  
Dan M. Brown ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Antitumor Agents ◽  
Human Tumor ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
New Class

Two New Cytotoxic Maytansinoids Targeting Tubulin from Trewia nudiflora

Planta Medica ◽  
2021 ◽  
Author(s):  
Chun Lei ◽  
Ya-Nan Li ◽  
Jia-Nan Li ◽  
Yu-Bo Zhou ◽  
Ming-Jun Cui ◽  
...  
Keyword(s):  
Human Tumor ◽  
Crystallographic Analysis ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
X Ray ◽  
Trewia Nudiflora ◽  
Ic50 Values ◽  
Mcf 7

AbstractTwo new maytansinoids, N-methyltreflorine (1) and methyltrewiasine (2), were isolated from the dried fruits of Trewia nudiflora, together with three known congeners (3 – 5). Their structures were elucidated by spectroscopic methods, and the absolute configuration of 1 and 2 was determined by X-ray crystallographic analysis. Compounds 1 – 5 exhibited strong cytotoxicity against human tumor cell lines, including HeLa, MV-4 – 11, and MCF-7, with IC50 values ranging from 0.12 to 11 nM. Compounds 1 and 4 also showed inhibitory activity against the MCF-7/ADR cell line with IC50 values of 13 and 28 nM, respectively. Compounds 1 and 2 significantly inhibited tubulin polymerization in vitro with IC50 values of 3.6 and 3.2 µM, respectively.

Bromoalkoxyxanthones as promising antitumor agents: Synthesis, crystal structure and effect on human tumor cell lines

2009 ◽  
Vol 44 (9) ◽  
pp. 3830-3835 ◽  
Author(s):  
Emília Sousa ◽  
Ana Paiva ◽  
Nair Nazareth ◽  
Luis Gales ◽  
Ana M. Damas ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Tumor Cell ◽  
Cell Lines ◽  
Antitumor Agents ◽  
Human Tumor ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

Design and Synthesis of 4(1H)-quinolone Derivatives as Autophagy Inducing Agents by Targeting ATG5 Protein

2020 ◽  
Vol 17 (7) ◽  
pp. 884-890
Author(s):  
Yifan Jia ◽  
Difei Yu ◽  
Qiuhua Huang ◽  
Xiaodong Zhang ◽  
Liqin Qiu ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Antitumor Agents ◽  
Human Tumor ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Design And Synthesis ◽  
Antiproliferative Agent ◽  
Quinolone Derivatives

Background: Quinolines have been characterized as a class of potential antitumor agents, and a large number of natural and synthetic quinolines acting as antitumor agents were reported. Methods: A series of 7-chloro-4(1H)-quinolone derivatives were synthesized. The antiproliferative effect of these compounds was evaluated by MTT assay against five human tumor cell lines. The mechanism of action of the selected compound 7h was also investigated. Results and Discussion: Most of the compounds had more potent antiproliferative activities than the lead compound 7-chloro-4(1H)-quinolone 6b. Compound 7h was found to be the most potent antiproliferative agent against human tumor cell lines. Further investigation demonstrated that compound 7h triggered ATG5-dependent autophagy of colorectal cancer cells by promoting the functions of LC3 proteins. Conclusion: These results were useful for designing and discovering more potent novel antitumor agents endowed with better pharmacological profiles.

Differential Increases in Glutathione S-Transferase Activities in a Range of Multidrug-Resistant Human Tumor Cell Lines

1989 ◽  
Vol 1 (6) ◽  
pp. 359-365 ◽  
Author(s):  
Richard D. H. Whelan ◽  
Louise K. Hosking ◽  
Alan J. Townsend ◽  
Kenneth H. Cowan ◽  
Bridget T. Hill
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Multidrug Resistant ◽  
Tumor Cell Lines ◽  
Glutathione S Transferase ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines
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