103791-08-8Relevant academic research and scientific papers
Polymer-supported N-heterocyclic carbene-rhodium complex catalyst for the addition of arylboronic acids to aldehydes
Yan, Chun,Zeng, Xiaoming,Zhang, Weifeng,Luo, Meiming
, p. 3391 - 3396 (2006)
A novel polymer-supported N-heterocylic carbene (NHC)-rhodium complex was prepared from chloromethyl polystyrene (CM PS) resin using a simple procedure. This polymer-supported NHC-rhodium complex was used as a catalyst for the addition of arylboronic acids to aldehydes affording arylmethanols in excellent yields.
Synthesis and biological evaluation of 1‐(Diarylmethyl)‐1h‐1,2,4‐triazoles and 1‐(diarylmethyl)‐1h‐imidazoles as a novel class of anti‐mitotic agent for activity in breast cancer
Ana, Gloria,Kelly, Patrick M.,Malebari, Azizah M.,Noorani, Sara,Nathwani, Seema M.,Twamley, Brendan,Fayne, Darren,O’boyle, Niamh M.,Zisterer, Daniela M.,Pimentel, Elisangela Flavia,Endringer, Denise Coutinho,Meegan, Mary J.
, p. 1 - 59 (2021/03/16)
We report the synthesis and biochemical evaluation of compounds that are designed as hybrids of the microtubule targeting benzophenone phenstatin and the aromatase inhibitor letrozole. A preliminary screening in estrogen receptor (ER)‐positive MCF‐7 breast cancer cells identified 5‐((2H‐1,2,3‐triazol‐1‐yl)(3,4,5‐trimethoxyphenyl)methyl)‐2‐methoxyphenol 24 as a potent antiproliferative compound with an IC50 value of 52 nM in MCF‐7 breast cancer cells (ER+/PR+) and 74 nM in triple‐negative MDA‐MB‐231 breast cancer cells. The compounds demonstrated significant G2/M phase cell cycle arrest and induction of apoptosis in the MCF‐7 cell line, inhibited tubulin polymerisation, and were selective for cancer cells when evaluated in non-tumorigenic MCF‐10A breast cells. The immunofluorescence staining of MCF‐7 cells confirmed that the compounds targeted tubulin and induced multinucleation, which is a recognised sign of mitotic catastrophe. Computational docking studies of compounds 19e, 21l, and 24 in the colchicine binding site of tubulin indicated potential binding conformations for the compounds. Compounds 19e and 21l were also shown to selectively inhibit aromatase. These compounds are promising candidates for development as antiproliferative, aromatase inhibitory, and microtubule‐disrupting agents for breast cancer.
PREPARATION OF ALKYLARYLCARBINOLS BY MONO-OXIDATION AT THE BENZYLIC POSITION USING 2,3-DICHLORO-5,6-DICYANOBENZOQUINONE (D.D.Q.)
Bouquet, M.,Guy, A.,Lemaire, M.,Guette, J. P.
, p. 1153 - 1158 (2007/10/02)
A new and convenient method for the preparation of alkylarylacetates and alkylarylcarbinols is described.Monooxidation at the benzylic position was performed using 2,3-dichloro-5,6-dicyanobenzoquinone (D.D.Q.) in acetic acid.Good yields of arylcarbinols were obtained under mild conditions.
