ethyl-2-amino-6-(3-5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4h-chromene-3-carboxylate and Neoplasms

ethyl-2-amino-6-(3-5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4h-chromene-3-carboxylate has been researched along with Neoplasms* in 2 studies

Reviews

1 review(s) available for ethyl-2-amino-6-(3-5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4h-chromene-3-carboxylate and Neoplasms

Article	Year
Sarco/Endoplasmic Reticulum Calcium ATPase Inhibitors: Beyond Anticancer Perspective. Journal of medicinal chemistry, 2020, 03-12, Volume: 63, Issue:5 Topics: Animals; Antineoplastic Agents; Enzyme Inhibitors; Gene Regulatory Networks; Humans; Neoplasms; Protein Structure, Secondary; Sarcoplasmic Reticulum Calcium-Transporting ATPases	2020

Other Studies

1 other study(ies) available for ethyl-2-amino-6-(3-5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4h-chromene-3-carboxylate and Neoplasms

Article	Year
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. Journal of medicinal chemistry, 2011, Aug-25, Volume: 54, Issue:16 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 IC(50) 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. Topics: Antineoplastic Agents; Benzopyrans; Cell Line, Tumor; Cell Survival; Daunorubicin; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Drug Synergism; HCT116 Cells; HL-60 Cells; HT29 Cells; Humans; Inhibitory Concentration 50; K562 Cells; Mitoxantrone; Molecular Structure; Neoplasms; Paclitaxel; Stereoisomerism; Structure-Activity Relationship; Vincristine	2011

Article

Year

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.

Journal of medicinal chemistry, 2011, Aug-25, Volume: 54, Issue:16

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 IC(50) 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.

Topics: Antineoplastic Agents; Benzopyrans; Cell Line, Tumor; Cell Survival; Daunorubicin; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Drug Synergism; HCT116 Cells; HL-60 Cells; HT29 Cells; Humans; Inhibitory Concentration 50; K562 Cells; Mitoxantrone; Molecular Structure; Neoplasms; Paclitaxel; Stereoisomerism; Structure-Activity Relationship; Vincristine

2011