biostudies-literatureQin LNICHD NIH HHS657-670https://www.ebi.ac.uk/biostudies/studies/S-EPMC8404148biostudies-literatureUnknown28(10)Steroid receptor coactivators (SRCs) possess specific and distinct oncogenic roles in the initiation of cancer and in its progression to a more aggressive disease. These coactivators interact with nuclear receptors and other transcription factors to boost transcription of multiple genes, which potentiate cancer cell proliferation, migration, invasion, tumor angiogenesis and epithelial-mesenchymal transition (EMT). Targeting SRCs using small molecule inhibitors (SMIs) is a promising approach to control cancer progression and metastasis. By high-throughput screening analysis, we recently identified SI-2 as a potent SRC SMI. To develop therapeutic agents, SI-10 and SI-12, the SI-2 analogs are synthesized that incorporate the addition of F atoms to the SI-2 chemical structure. As a result, theEndocrine-related cancerDevelopment of improved SRC-3 inhibitors as breast cancer therapeutic agents.PMC8404148R01 HD007857R01 HD008188Peng XJain PQin LChen JO'Malley BWLu DLonard DMWang JCardenas DYu XXu JYu YfalseDevelopment of improved SRC-3 inhibitors as breast cancer therapeutic agents.Steroid receptor coactivators (SRCs) possess specific and distinct oncogenic roles in the initiation of cancer and in its progression to a more aggressive disease. These coactivators interact with nuclear receptors and other transcription factors to boost transcription of multiple genes, which potentiate cancer cell proliferation, migration, invasion, tumor angiogenesis and epithelial-mesenchymal transition (EMT). Targeting SRCs using small molecule inhibitors (SMIs) is a promising approach to control cancer progression and metastasis. By high-throughput screening analysis, we recently identified SI-2 as a potent SRC SMI. To develop therapeutic agents, SI-10 and SI-12, the SI-2 analogs are synthesized that incorporate the addition of F atoms to the SI-2 chemical structure. As a result, the2021-01-01T00:00:00Z2021 Aug2025-04-04T09:37:07.631Z2025-04-04T09:37:07.631ZS-EPMC84041483431034110.1530/erc-20-040210.1530/ERC-20-0402