194423-79-5Relevant articles and documents
New quinoxaline derivatives as dual pim-1/2 kinase inhibitors: Design, synthesis and biological evaluation
Bach, Stéphane,Berthelot, Pascal,Brachet-Botineau, Marie,Croix, Cécile,Denevault-Sabourin, Caroline,Gouilleux, Fabrice,Guillon, Jean,Ibrahim, Sajida,Logé, Cédric,Oyallon, Bruno,Pinaud, No?l,Raoul, William,Robert, Thomas,Viaud-Massuard, Marie-Claude
, (2021/06/12)
Proviral integration site for Moloney murine leukemia virus (Pim)-1/2 kinase overexpression has been identified in a variety of hematologic (e.g., multiple myeloma or acute myeloid leukemia (AML)) and solid (e.g., colorectal carcinoma) tumors, playing a key role in cancer progression, metastasis, and drug resistance, and is linked to poor prognosis. These kinases are thus considered interesting targets in oncology. We report herein the design, synthesis, structure–activity relationships (SAR) and in vitro evaluations of new quinoxaline derivatives, acting as dual Pim1/2 inhibitors. Two lead compounds (5c and 5e) were then identified, as potent submicromolar Pim-1 and Pim-2 inhibitors. These molecules were also able to inhibit the growth of the two human cell lines, MV4-11 (AML) and HCT-116 (colorectal carcinoma), expressing high endogenous levels of Pim-1/2 kinases.
Quinoxaline chemistry. Part 7. 2-[aminobenzoates]- and 2- [aminobenzoylglutamate]-quinoxalines as classical antifolate agents. Synthesis and evaluation of in vitro anticancer, anti-HIV and antifungal activity
Loriga,Piras,Sanna,Paglietti
, p. 157 - 166 (2007/10/03)
Thirty-three quinoxalines bearing an aminobenxoyl or aminobenzoylglutammate group on position 2 and various substituents on position 3,6,7 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI showed that most derivatives exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10-5 and 10-4 molar concentrations. Interesting selectivities were also recorded between 10-8 and 10-6. Among the series examined one compound (29) which was the most active also exhibited both in vitro anti-HIV protection and antifungal activity while in other two (31.37) the antifungal activity was prevailing.
