Steroidal Dimer by001 Inhibits Proliferation and Migration of Esophageal Cancer Cells via Multiple Mechanisms

Sai-Qi Wang; Kai-Rui Zhou; Xiao-Li Shi; Li-Ming Chang; Yan-Bing Zhang; Bin Yu; Hongmin Liu

doi:10.20944/preprints201706.0128.v1

Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Version 1 : Received: 29 June 2017 / Approved: 30 June 2017 / Online: 30 June 2017 (07:43:06 CEST)

Following our previous success in identifying new steroid-based anticancer agents, we herein disclosed the structural requirements for retaining high potency against cancer cells and associated modes of action. The structurally novel steroidal dimer by001 inhibited growth of different esophageal cancer cells and colony formation at low micromolar levels, elevated cellular ROS levels and caused mitochondrial dysfunction. Mechanistic studies showed that by001 induced cell death through the mitochondria and death receptor-mediated apoptotic pathways and autophagy induction, as well as inhibited migration.

steroidal dimer; steroidal N-heterocycles; antiproliferative activity; esophageal cancer cells

Chemistry and Materials Science, Medicinal Chemistry

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Steroidal Dimer by001 Inhibits Proliferation and Migration of Esophageal Cancer Cells via Multiple Mechanisms

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