Journal ArticleDOI
Synthesis, biological evaluation, and molecular docking studies of 1,3,4-oxadiazole derivatives possessing 1,4-benzodioxan moiety as potential anticancer agents
Xiao-Min Zhang,Min Qiu,Juan Sun,Zhang Yanbin,Yu-Shun Yang,Wang Xiaoliang,Tang Jianfeng,Hai-Liang Zhu +7 more
TLDR
A series of new 1,3, 4-oxadiazole derivatives containing 1,4-benzodioxan moiety (6a-6s) as potential telomerase inhibitors were synthesized and showed compound 6k possessed the most potent telomersase activity.About:
This article is published in Bioorganic & Medicinal Chemistry.The article was published on 2011-11-01. It has received 99 citations till now. The article focuses on the topics: Benzodioxan & Docking (molecular).read more
Citations
More filters
Journal ArticleDOI
Synthetic Approaches and Pharmacological Activity of 1,3,4-Oxadiazoles: A Review of the Literature from 2000–2012
Cledualdo Soares de Oliveira,Bruno Freitas Lira,José Maria Barbosa-Filho,Jorge Goncalo Fernandez Lorenzo,Petrônio Filgueiras de Athayde-Filho +4 more
TL;DR: This review provides readers with an overview of the main synthetic methodologies for 1,3,4-oxadiazole derivatives, and of their broad spectrum of pharmacological activities as reported over the past twelve years.
Journal ArticleDOI
1,3,4-Oxadiazoles: An emerging scaffold to target growth factors, enzymes and kinases as anticancer agents
TL;DR: The focused criteria of this review is to highlights the targeted inhibitory activity of 1,3,4-oxadiazole derivatives and their structure activity relationship to generate potential anticancer agents.
Journal ArticleDOI
Synthesis, molecular modeling and biological evaluation of 2-aminomethyl-5-(quinolin-2-yl)-1,3,4-oxadiazole-2(3H)-thione quinolone derivatives as novel anticancer agent.
TL;DR: A series of quinoline derivatives (4a-4o) have been synthesized and their biological activities were evaluated as potential telomerase inhibitors and compounds 4d and 4i with potent inhibitory activity in tumor growth inhibition may be potential anticancer agents.
Journal ArticleDOI
One-pot, four-component synthesis of novel cytotoxic agents 1-(5-aryl-1,3,4-oxadiazol-2-yl)-1-(1H-pyrrol-2-yl)methanamines.
Ali Ramazani,Mehdi Khoobi,Azar Torkaman,Fatemeh Zeinali Nasrabadi,Hamid Forootanfar,Mojtaba Shakibaie,Mandana Jafari,Alieh Ameri,Saeed Emami,Mohammad Ali Faramarzi,Alireza Foroumadi,Abbas Shafiee +11 more
TL;DR: The structure-activity relationship study revealed that the introduction of halogen atoms on both 5-phenyl ring and N-benzyl part improved the cytotoxic activity against all tested cell lines.
Journal ArticleDOI
Synthesis and Anti‐cancer Activity of 1,3,4‐Thiadiazole and 1,3‐Thiazole Derivatives Having 1,3,4‐Oxadiazole Moiety
Kamal M. Dawood,Sobhi M. Gomha +1 more
TL;DR: In this article, the anti-cancer activity of 1,3,4-oxadiazolyl-phenylthiourea 3 with hydrazonoyl halides was evaluated for the colon carcinoma cell line (HCT-116).
References
More filters
Journal ArticleDOI
Extension of life-span by introduction of telomerase into normal human cells
Andrea G. Bodnar,Michel M. Ouellette,Maria Frolkis,Shawn E. Holt,Choy-Pik Chiu,Gregg B. Morin,Calvin B. Harley,Jerry W. Shay,Serge Lichtsteiner,Woodring E. Wright +9 more
TL;DR: In this article, two telomerase-negative normal human cell types, retinal pigment epithelial cells and foreskin fibroblasts, were transfected with vectors encoding the human telomere catalytic subunit.
Journal ArticleDOI
Comparative Protein Structure Modeling Using MODELLER
Narayanan Eswar,Ben Webb,Marc A. Marti-Renom,Mallur S. Madhusudhan,David Eramian,Min-Yi Shen,Ursula Pieper,Andrej Sali +7 more
TL;DR: This unit describes how to calculate comparative models using the program MODELLER and discusses all four steps of comparative modeling, frequently observed errors, and some applications.
Journal ArticleDOI
Automated docking of substrates to proteins by simulated annealing.
TL;DR: The Metropolis technique of conformation searching is combined with rapid energy evaluation using molecular affinity potentials to give an efficient procedure for docking substrates to macromolecules of known structure.
Journal ArticleDOI
Cellular senescence as a tumor-protection mechanism: the essential role of counting.
Woodring E. Wright,Jerry W. Shay +1 more
TL;DR: Increasing understanding of the role of telomere shortening in the replicative aging of cultured fibroblasts now permits a re-examination of what may reasonably be called cellular senescence, and what most likely represents artifacts of the culture environment and/or specific cell-cycle control mechanisms.
Journal ArticleDOI
Synthesis of novel 1,3,4-trisubstituted pyrazole derivatives and their evaluation as antitumor and antiangiogenic agents.
TL;DR: Several 1,3,4-trisubstituted pyrazole derivatives were synthesized and screened for their cytotoxic effect in a primary 3 tumor cell line test at 10(-4) M drug concentration, and all the tested compounds interfered with the migratory function of HUVECs in response to vascular endothelium growth factor (VEGF) rather than the endothelial cells proliferation.