Ontology highlight
ABSTRACT:
SUBMITTER: Cai CY
PROVIDER: S-EPMC6718313 | biostudies-literature | 2019 Oct
REPOSITORIES: biostudies-literature
Cai Chao-Yun CY Zhai Hong H Lei Zi-Ning ZN Tan Cai-Ping CP Chen Bao-Li BL Du Zhao-Yi ZY Wang Jing-Quan JQ Zhang Yun-Kai YK Wang Yi-Jun YJ Gupta Pranav P Wang Bo B Chen Zhe-Sheng ZS
European journal of medicinal chemistry 20190624
Ko143, a potent ABCG2 inhibitor that reverses multidrug resistance in cancer, cannot be used clinically due to its unsuitable metabolic stability. We identified benzoyl indoles as reversal agents that reversed ABCG2-mediated multidrug resistance (MDR), with synthetic tractability and enhanced metabolic stability compared to Ko143. Bisbenzoyl indole 2 and monobenzoyl indole 8 significantly increased the accumulation of mitoxantrone (MX) in ABCG2-overexpressing NCI-H460/MX20 cells, and sensitized ...[more]