1259294-16-0Relevant articles and documents
Coumarin Derivatives Exert Anti-Lung Cancer Activity by Inhibition of Epithelial–Mesenchymal Transition and Migration in A549 Cells
Barreto, Emiliano,Bourguignon, Jean-Jacques,Dos Santos Carmo, Julianderson de Oliveira,Filho, José Maria Barbosa,Mendon?a-Junior, Francisco Jaime Bezerra,Rodarte, Renato Santos,Schmitt, Martine,Silva, Simone Lara de Omena,Souza, Tayhana Priscila Medeiros,da Silva, Camila Radelley Azevedo Costa,de Aquino, Thiago Mendon?a,de Araújo, Rodrigo Santos Aquino,de Mélo, Natália Barbosa,de Moura, Ricardo Olímpio
, (2022/01/24)
A series of coumarin derivatives and isosteres were synthesized from the reaction of triflic intermediates with phenylboronic acids, terminal alkynes, and organozinc compounds through palladium-catalyzed cross-coupling reactions. The in vitro cytotoxic ef
Structure-activity relationship and molecular mechanisms of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H -chromene-3- carboxylate (CXL017) and its analogues
Das, Sonia G.,Srinivasan, Balasubramanian,Hermanson, David L.,Bleeker, Nicholas P.,Doshi, Jignesh M.,Tang, Ruoping,Beck, William T.,Xing, Chengguo
, p. 5937 - 5948 (2011/10/08)
Multidrug resistance (MDR) in cancer is a phenomenon in which administration of a single chemotherapeutic agent causes cross-resistance of cancer cells to a variety of therapies even with different mechanisms of action. Development of MDR against standard therapies is a major challenge in the treatment of cancer. Previously we have demonstrated a unique ability of CXL017 (5) to selectively target MDR cancer cells and synergize with mitoxantrone (MX) in HL60/MX2 MDR cells. Here we expand its scope and demonstrate that 5 can synergize with both vincristine and paclitaxel in three different MDR cell lines (HL60/DNR, K562/HHT300, and CCRF-CEM/VLB100). We also demonstrate that 5 has potent cytotoxicity in the NCI-60 panel of cell lines with an average IC 50 of 1.04 μM. In addition, 5 has a unique mechanism of action in comparison with standard agents in the NCI database based on COMPARE analysis. Further structure-activity relationship study led to the development of a more potent analogue, compound 7d, with an IC50 of 640 nM in HL60/MX2. Additionally, one enantiomer of 5 is 13-fold more active than the less active enantiomer. Taken together, our study has led to the discovery of a series of analogues that selectively target drug-resistant cancer cells with the potential for the treatment of drug-resistant cancers.
