5145-71-1Relevant articles and documents
An expeditious synthesis of n-substituted pyrroles via microwave-induced iodine-catalyzed reactions under solventless conditions
Bandyopadhyay, Debasish,Mukherjee, Sanghamitra,Banik, Bimal K.
, p. 2520 - 2525 (2010)
An expeditious synthesis of N-substituted pyrroles has been developed by reacting 2,5-dimethoxy tetrahydrofuran and several amines using a microwave-induced molecular iodine-catalyzed reaction under solventless conditions. Copyright
A facile synthesis of diaryl pyrroles led to the discovery of potent colchicine site antimitotic agents
Romagnoli, Romeo,Oliva, Paola,Salvador, Maria Kimatrai,Manfredini, Stefano,Padroni, Chiara,Brancale, Andrea,Ferla, Salvatore,Hamel, Ernest,Ronca, Roberto,Maccarinelli, Federica,Rruga, Fatlum,Mariotto, Elena,Viola, Giampietro,Bortolozzi, Roberta
, (2021/02/09)
Three different series of cis-restricted analogues of combretastatin A-4 (CA-4), corresponding to thirty-nine molecules that contained a pyrrole nucleus interposed between the two aryl rings, were prepared by a palladium-mediated coupling approach and evaluated for their antiproliferative activity against six human cancer cell lines. In the two series of 1,2-diaryl pyrrole derivatives, results suggested that the presence of the 3′,4′,5′-trimethoxyphenyl moiety at the N-1 position of the pyrrole ring was more favorable for antiproliferative activity. In the series of 3,4-diarylpyrrole analogues, three compounds (11i-k) exhibited maximal antiproliferative activity, showing excellent antiproliferative activity against the CA-4 resistant HT-29 cells. Inhibition of tubulin polymerization of selected 1,2 pyrrole derivatives (9a, 9c, 9o and 10a) was similar to that observed with CA-4, while the isomeric 3,4-pyrrole analogues 11i-k were generally from 1.5- to 2-fold more active than CA-4. Compounds 11j and 11k were the only compounds that showed activity as inhibitors of colchicine binding comparable to that CA-4. Compound 11j had biological properties consistent with its intracellular target being tubulin. This compound was able to block the cell cycle in metaphase and to induce significant apoptosis at a concentration of 25 nM, following the mitochondrial pathway, with low toxicity for normal cells. More importantly, compound 11j exerted activity in vivo superior to that of CA-4P, being able to significantly reduce tumor growth in a syngeneic murine tumor model even at the lower dose tested (5.0 mg/kg).
The remarkable selectivity of the 2-arylquinoline-based acyl hydrazones toward copper salts: Exploration of their catalytic applications in the copper catalysed: N -arylation of indole derivatives and C1-alkynylation of tetrahydroisoquinolines via the A
Echeverry-Gonzalez, Carlos A.,Ortiz Villamizar, Marlyn Catalina,Kouznetsov, Vladimir V.
supporting information, p. 243 - 250 (2021/01/11)
Ligands promoting copper-catalysed coupling reactions have received increasing attention because of their ability to enhance the catalytic activity of copper, making these reactions applicable in different fields such as drugs, pharmaceutically interestin
Echeverry-Gonzalez, Carlos A.,Ortiz Villamizar, Marlyn Catalina,Kouznetsov, Vladimir V.
supporting information, p. 243 - 250 (2021/01/11)
Ligands promoting copper-catalysed coupling reactions have received increasing attention because of their ability to enhance the catalytic activity of copper, making these reactions applicable in different fields such as drugs, pharmaceutically interestin
