38459-64-2Relevant academic research and scientific papers
Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C
Carpenter, Colleen,Sorenson, Roderick J.,Jin, Yafei,Klossowski, Szymon,Cierpicki, Tomasz,Gnegy, Margaret,Showalter, Hollis D.
, p. 5495 - 5504 (2016)
The clinical selective estrogen receptor modulator tamoxifen is also a modest inhibitor of protein kinase C, a target implicated in several untreatable brain diseases such as amphetamine abuse. This inhibition and tamoxifen's ability to cross the blood br
Synthesis and biological evaluation of novel tamoxifen-1,2,4-triazole conjugates
Murty,Katiki, Mohana Rao,Nanubolu, Jagadeesh Babu,Garimella, Srujana,Polepalli, Sowjanya,Jain, Nishant,Buddana, Sudheer Kumar,Prakasham
, p. 687 - 703 (2016)
Abstract: A new class of compounds, structurally related to the breast cancer drug tamoxifen, was designed and synthesized. The McMurry coupling reaction was used as the key synthetic step in the preparation of these analogs, and the structural assignment
A one-pot multicomponent ‘click’ approach to the synthesis of novel tamoxifen-triazole conjugates using nano iron oxide catalyst and their preliminary antiproliferative activity studies
Katiki, Mohana Rao,Kommula, Dileep,Polepalli, Sowjanya,Jain, Nishant,Murty, Madugula Sree Rama
, p. 846 - 860 (2019/10/28)
Background: In an effort to establish new drug candidates with improved antiproliferative activity, we report here a novel class of compounds designed rationally by the replacement of an ethyl group in tamoxifen with a methylene (1H-1,2,4-triazole) and th
A highly sensitive nucleic acid stain based on amino-modified tetraphenylethene: The influence of configuration
Xu, Li,Zhu, Zece,Zhou, Xiang,Qin, Jingui,Yang, Chuluo
supporting information, p. 6494 - 6497 (2014/06/09)
We designed and synthesized a new amino-functionalized tetraphenylethene (TPE) derivative as a highly sensitive dye for the detection of dsDNA and oligonucleotide in both solution and a gel matrix. We further revealed that the cis configuration dye showed
Conjugated polyelectrolytes with aggregation-enhanced emission characteristics: Synthesis and their biological applications
Hu, Rongrong,Ye, Ruquan,Lam, Jacky W.Y.,Li, Min,Leung, Chris W.T.,Tang, Ben Zhong
, p. 2436 - 2445 (2013/10/08)
Conjugated polyelectrolytes are promising candidates for the construction of fluorescent bioprobes. In this study, a series of water-soluble fluorescent polyelectrolytes have been designed and synthesized by means of the quaternization of their tetrapheny
1-[(Aryloxy)alkyl]-1H-imidazoles as inhibitors of neuronal nitric oxide synthase
Salerno,Sorrenti,Guerrera,Sarva,Siracusa,Di Giacomo,Vanella
, p. 491 - 494 (2007/10/03)
A series of 1-[(aryloxy)alkyl]-1 H-imidazoles were synthesized from imidazole and various (aryloxy)alkyl bromides and tested for inhibitory activity against the three isoforms of nitric oxide synthase. 1-[2-(4-Bromophenoxy)ethyl]-1 H-imidazole and 1-[2-[4-(trifluoromethyl)phenoxy]ethyl]-1H-imidazole showed inhibitory activity against the neuronal isoform but were less potent against the endothelial isoform. Thus they could be considered interesting for their selectivity. The remaining compounds had only modest activity.
Synthesis and chiral separation of some antitumor agents
Singh, Satendra,Meyer, Karen L.,Magarian, Robert A.
, p. 81 - 94 (2007/10/03)
Four Z-isomers of 1,1-dichloro-2,2,3-triarylcyclopropane (DTACs), designed as potent antitumor agents, were synthesized from their appropriately substituted ethenes, which were prepared from the Grignard reaction followed by the dehydration of their inter
Magnetic Field Effects on the Dynamics of Biradicals Generated from Benzophenone and Diphenylamine Bifunctional Chain Molecules
Tanimoto, Yoshifumi,Okada, Natsuo,Takamatsu, Shinji,Itoh, Michiya
, p. 1342 - 1348 (2007/10/02)
The magnetic field effects (MFE) on the lifetimes of triplet biradicals generated from the intramolecular photoreaction of bifunctional chain molecules, α-(4-benzoylphenoxy)-ω-alkanes (BP-O-n-O-DPA, n=2-16) were studied by laser fl
Crossed Coupling of Functionalised Ketones by Low Valent Titanium (The McMurry Reaction): A New Stereoselective Synthesis of Tamoxifen
Coe, Paul L.,Scriven, Clare E.
, p. 475 - 478 (2007/10/02)
Low valent titanium-mediated crossed coupling of substitued benzophenones of the 4-XPhCOPh, where X = MeO, ClCH2CH2O, BrCH2CH2O, CF3C6H4O, HO, and Me2NCH2CH2O, with propiophenone affords the corresponding but-1-enes in high yield with a marked preponderance of the Z-isomer in most cases.Remarkably, when X = OH the E:Z ratio is 9:1.The value of this method is illustrated by simple syntheses of (Z)-1-phenyl>-1,2-diphenylbut-1-ene (Tamoxifen) a drug widely used in the treatment of eostrogen-dependent breast tumors.
Ellipticine Derivatives with an Affinity to the Estrogen Receptor, an Approach to Develop Intercalating Drugs with a Specific Effect on the Hormone-Dependent Breast Cancer
Delbarre, Alain,Oberlin, Robert,Roques, Bernard P.,Borgna, Jean-Louis,Rochefort, Henri,et al.
, p. 752 - 761 (2007/10/02)
In order to obtain breast tumor directed agents, we have prepared mixed compounds using estradiol or (E)-clomiphene as specific vectors for the breast tissue and a DNA intercalator from the ellipticine series as cytotoxic agent.Among the newly synthesized
