Synthesis and Anticancer Activity of Di(3-thienyl)methanol and Di(3-thienyl)methane

@article{Kaushik2012SynthesisAA,
  title={Synthesis and Anticancer Activity of Di(3-thienyl)methanol and Di(3-thienyl)methane},
  author={Nagendra Kumar Kaushik and Hong Seon Kim and Young June Chae and Young Nam Lee and Gi-chung Kwon and Eun Ha Choi and In Tae Kim},
  journal={Molecules},
  year={2012},
  volume={17},
  pages={11456 - 11468}
}
Di(3-thienyl)methanol (2) and di(3-thienyl)methane (3) have been synthesized and screened against the T98G (brain cancer) cell line. Treatment induced cell death (MTT and macro-colony assay), growth inhibition, cytogenetic damage (micronuclei formation), were studied as cellular response parameters. Treatment with the compounds enhanced growth inhibition and cell death in a concentration dependent manner in both T98G and HEK (normal) cell lines. At higher concentrations (>20 µg/mL) the… 
Synthesis and Antiproliferative Activity of Ammonium and Imidazolium Ionic Liquids against T98G Brain Cancer Cells
TLDR
Four ammonium and imidazolium ionic liquids have been synthesized and screened against the T98G cell line (brain cancer) and HEK normal cells and exhibited less cytotoxicity against the normal human HEK cells at all effective concentrations.
Novel Methylselenoesters as Antiproliferative Agents
TLDR
A new series of methylselenoesters with different scaffolds aiming to modulate the release of CH3SeH, which follow Lipinski’s Rule of Five and with exception of compounds 1 and 14, present better drug-likeness values than the positive controlmethylseleninic acid.
Synthesis and Structure-Activity Relationship of Some New Thiophene-Based Heterocycles as Potential Antimicrobial Agents
TLDR
The results indicated that compounds 9, 12, and 19 were found to be more potent than the standard drug Amphotericin B against Aspergillus fumigates and Syncephalastrum racemosum.
Syntheses, characterization, and anti-cancer activities of pyridine-amide based compounds containing appended phenol or catechol groups
AbstractSeveral pyridine-amide compounds appended with phenol/catechol groups are synthesized. These compounds consist of protected or deprotected phenol/catechol groups and offer pyridine, amide,
Evaluation of cytotoxic activity of platinum nanoparticles against normal and cancer cells and its anticancer potential through induction of apoptosis
TLDR
It is proved that biosynthesized ptNPs could be potent anti-ovarian cancer drugs through green technology and had potent anticancer activities against PA-1 cell line via induction of apoptosis and cell cycle arrest.
Novel aminoalkylated azaphenothiazines as potential inhibitors of T98G, H460 and SNU80 cancer cell lines in vitro.
TLDR
In all, twenty-five molecules, including intermediates, were investigated for their in vitro anticancer activity, of which fourteen azaphenothiazines were found to decrease the metabolic viability and growth of the T98G, H460 and SNU80 cancer cells effectively in a dose-dependent manner.
Self-assembled supramolecular hetero-bimetallacycles for anticancer potency by intracellular release.
TLDR
The cytotoxicity of complexes 4 and 5 were found to be considerably more effective against cancer cells than reference drug cisplatin and to justify a significant level of apoptosis in complex-treated cells.
Heterocyclization of polarized system: synthesis, antioxidant and anti-inflammatory 4-(pyridin-3-yl)-6-(thiophen-2-yl) pyrimidine-2-thiol derivatives
TLDR
The newly synthesized compounds showed potent anti-inflammatory activities both in vitro and in vivo and exhibited promising antioxidant vitalities against α, α-diphenyl-β-picrylhydrazyl scavenging activity and lipid peroxidation.
Synthesis and Characterization of New Heterocyclic Compounds Containing Thienylbenzo[h]Quinoline Moiety
In this paper the reaction of 2-(2′-thienylmethylene)-3,4-dihydronaphthalen-2(1H)-one (1) with cyanothioacetamide gave a mixture of 3-cyano-5,6-dihydro-4-(2′-thienyl)-benzo[h]quinolin-2(1H)-thione
Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update
TLDR
A concise illustration explains the design strategy and anticancer potential of these five‐ and six‐ Membered sulfur‐containing heterocyclic molecules along with a brief outline on seven‐membered sulfur heterocycles.
...
1
2
...

References

SHOWING 1-10 OF 25 REFERENCES
Design, synthesis, and biological evaluation of thiophene analogues of chalcones.
TLDR
A series of chalcone-like agents, in which the double bond of the enone system is embedded within a thiophene ring, were synthesized and evaluated for antiproliferative activity and inhibition of tubulin assembly and colchicine binding to tubulin.
Synthesis and antitumor properties of 2,5-bis(3'-indolyl)thiophenes: analogues of marine alkaloid nortopsentin.
TLDR
A series of 11 bis-indolylthiophenes of type 8-10 were obtained by cyclization of diketones 4 and 7 using Lawesson's reagent and showed antiproliferative activity generally in the micromolar range.
Novel thiophene derivatives as PTP1B inhibitors with selectivity and cellular activity.
TLDR
The novel chemical entities reported in this study could be used for overcoming the poor selectivity and low cellular activity of PTP1B inhibitors and might represent a starting point for development of therapeutic PTP inhibitors.
Thiophenes and furans derivatives: a new class of potential pharmacological agents.
TLDR
A new class of potential pharmacological thiophenes and furans compounds has been prepared and all compounds displayed antioxidant activity however the anti-inflammatory activity is not related to antioxidant potential.
Synthesis, antimicrobial, antioxidant, anti-inflammatory, and analgesic activities of some new 3-(2′-thienyl)pyrazole-based heterocycles
Abstract1-Phenyl-3-(thiophen-2-yl)-1H-pyrazole-4-carbaldehyde was used as a synthon for the synthesis of new thiazole and pyrazoline heterocycles having 2-thienylpyrazole moiety. The antimicrobial,
Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes.
TLDR
Certain compounds show promising in vitro activity against Trypanosoma brucei rhodesiense and have superior in vivo activity against T. b.
Design, synthesis and anti-tubercular evaluation of new 2-acylated and 2-alkylated amino-5-(4-(benzyloxy)phenyl)thiophene-3-carboxylic acid derivatives. Part 1.
TLDR
It is suggested that the designed 2-amino-5-phenylthiophene-3-carboxylic acid scaffold may serve as new promising template for further elaboration as anti-TB drugs.
Inhibitors of the RET tyrosine kinase based on a 2-(alkylsulfanyl)-4-(3-thienyl)nicotinonitrile scaffold.
TLDR
Docking experiments suggest a binding mode of the new inhibitors in the ATP binding pocket of the target kinase, explaining the observed structure-activity relationships.
Synthesis, antitumor and antioxidant evaluation of some new thiazole and thiophene derivatives incorporated coumarin moiety
Abstract3-Acetylcoumarin (1) was utilized as a key intermediate for the synthesis of 2-aminothiazole derivative 3via bromination of 1 followed by treatment of the formed acetylbromide 2 with thiourea
Fabrication and growth mechanism of ZnO nanostructures and their cytotoxic effect on human brain tumor U87, cervical cancer HeLa, and normal HEK cells
TLDR
Screening results from anticancer studies of the effects on human brain tumor U87, cervical cancer HeLa, and normal HEK cells of ZnO nanostructures of diverse shape indicate promising activity that varies with changes in the structure and the size of the particles, and indicates that these structures may interfere with the rejoining of DNA strand breaks.
...
1
2
3
...