ChemInform Abstract: Medical Chemistry of Polyoxometalates. Part 1. Potent Antitumor Activity of Polyoxomolybdates on Animal Transplantable Tumors and Human Cancer Xenograft.

ChemInform ◽  
1988 ◽  
Vol 19 (12) ◽  
Author(s):  
T. YAMASE ◽  
H. FUJITA ◽  
K. FUKUSHIMA
Keyword(s):  
Antitumor Activity ◽  
Human Cancer ◽  
Transplantable Tumors ◽  
Medical Chemistry

scholarly journals Design, synthesis and biological evaluation of imidazopyridine–propenone conjugates as potent tubulin inhibitors

MedChemComm ◽  
2017 ◽  
Vol 8 (5) ◽  
pp. 1000-1006 ◽  
Author(s):  
Ibrahim Bin Sayeed ◽  
V. Lakshma Nayak ◽  
Mohd Adil Shareef ◽  
Neeraj Kumar Chouhan ◽  
Ahmed Kamal
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Tubulin Inhibitors ◽  
Synthesis And Biological Evaluation

A library of imidazopyridine–propenone conjugates (8a–8u) were synthesized and evaluated for their antitumor activity against four human cancer cell lines.

scholarly journals SYNTHESIS AND ANTITUMOR ACTIVITY OF NEW MULTIFUNCTIONAL COUMARINS

2020 ◽  
Vol 17 (36) ◽  
pp. 871-883
Author(s):  
Moath Kahtan BASHIR ◽  
Yasser Fakri MUSTAFA ◽  
Mahmood Khudhayer OGLAH
Keyword(s):  
Schiff Base ◽  
Antitumor Activity ◽  
Human Cancer ◽  
Biological Activities ◽  
Cell Viability Assay ◽  
Chemical Structures ◽  
Viability Assay ◽  
Schiff Base Formation ◽  
Mcf 7

Cancer constitutes one of the most severe public health menaces worldwide. It is imperative to synthesize new compounds and explore their antitumor activity to find a potential resolution to this health problem. Synthesis of new scaffolds and evaluating their antitumor activity is a relevant approach for combating cancer development. Coumarins can exhibit diverse biological activities, and one of these is the antitumor activity. This study aimed to synthesize new coumarins by grafting their precursors to the aromatic amines via Schiff base formation and evaluating their introductory antitumor activity. New multifunctional coumarins (MC1-MC9) were prepared by integrating a functionalized coumarin with different toluidine derivatives via a Schiff-base linkage. Spectral characterization inspired by FTIR, 1H- and 13C- NMR spectroscopies has established the chemical structures of the synthesized products. The antitumor activity was explored in vitro versus four dominant human cancer lines, including HeLa, SKG, MCF-7, and AMN3. The outcomes acquired from the cell viability assay inspected by applying MTT dye have revealed that the synthesized multifunctional coumarins, particularly MC3, have a hopeful activity. It can be concluded that a similar trend of activity against the test cell lines was observed for the synthesized coumarins, with the best action being versus MCF-7 and the least one versus AMN3. This study not only affords a new scaffold of a significant antitumor activity but also provides some insights into its structureactivity relationship.

scholarly journals Chloroquine Urea Derivatives: Synthesis and Antitumor Activity in Vitro

2018 ◽  
Vol 68 (4) ◽  
pp. 471-483 ◽  
Author(s):  
Kristina Pavić ◽  
Zrinka Rajić ◽  
Zvonimir Mlinarić ◽  
Lidija Uzelac ◽  
Marijeta Kralj ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Urea Derivatives ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Lead Compounds ◽  
Insight Into

Abstract In the current paper, we describe the design, synthesis and antiproliferative screening of novel chloroquine derivatives with a quinoline core linked to a hydroxy or halogen amine through a flexible aminobutyl chain and urea spacer. Synthetic pathway leading to chloroquine urea derivatives 4-10 includes two crucial steps: i) synthesis of chloroquine benzotriazolide 3 and ii) formation of urea derivatives through the reaction of compound 3 with the corresponding amine. Testing of antiproliferative activity against four human cancer cell lines revealed that chloroquine urea derivatives 9 and 10 with aromatic moieties show activity at micromolar concentrations. Therefore, these molecules represent interesting lead compounds that might provide an insight into the design of new anticancer agents.

Antitumor acridines with diaminoalkylo pharmacophoric group

2001 ◽  
Vol 73 (9) ◽  
pp. 1421-1428 ◽  
Author(s):  
Jerzy Konopa
Keyword(s):  
Clinical Trials ◽  
Biological Activity ◽  
Antitumor Activity ◽  
Clinical Evaluation ◽  
Wide Spectrum ◽  
Aromatic Rings ◽  
Transplantable Tumors

The substitution of acridine molecule in positions 1 and/or 4 with diaminoalkylo residue may result in obtaining derivatives displaying antitumor activity. The diaminoalkylo residue can be attached to acridine either directly or indirectly as a carboxamido moiety. In the former case, the presence of appropriate substituent in position para to diaminoalkylo residue is crucial for antitumor activity. Also, heterocyclic aromatic rings condensed with the acridine core can be considered as such substituents. Additional substituents introduced into the acridine core, especially those that may be transformed into quinoid systems, significantly increase antitumor activity of modified analogs. It is, however, of utmost importance that the presence of diaminoalkylo residue is the indispensable prerequisite for biological activity of acridines. Among several groups of synthesized diaminoalkyloacridines, the most potent antineoplastic properties toward a wide spectrum of transplantable tumors are exhibited by acridine-4-carboxamides, imidazo-, triazolo-, and pyrazoloacridinones. Two derivatives belonging to the above groups, acridine-4-carboxamide DACA and imidazoacridinone C-1311, are currently in clinical trials. Other derivatives exhibiting potent antitumor activity, that could be considered as close analogs of diaminolkyloacridines, are pyrazoloacridines, one of which is currently under clinical evaluation.

scholarly journals Molecular pharmacology and antitumor activity of Zalypsis® in several human cancer cell lines

2009 ◽  
Vol 78 (2) ◽  
pp. 162-170 ◽  
Author(s):  
Juan F.M. Leal ◽  
Verónica García-Hernández ◽  
Victoria Moneo ◽  
Alberto Domingo ◽  
Juan Antonio Bueren-Calabuig ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Molecular Pharmacology ◽  
Human Cancer Cell Lines
Sign in / Sign up

Export Citation Format

Share Document