May 2024 in “Journal of molecular structure” This study found that a novel thiohydantoin derivative, 3a, effectively inhibited androgen receptor activity in LNCaP cells and showed promising in vivo results by reducing testosterone-induced prostate changes, outperforming finasteride in mitigating prostate index and histopathological alterations.
5 citations
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February 1997 in “Bioorganic & Medicinal Chemistry” This study found that among 17 beta-(N-ureylene-N,N'-disubstituted)-4-azasteroids, those with an N'-phenyl moiety were the most effective inhibitors of human type I 5 alpha-reductase.
7 citations
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August 2019 in “Bioorganic & medicinal chemistry” This study identified novel 4-Amino-2H-benzo[h]chromen-2-one analogs as potent androgen receptor antagonists that show strong antiproliferative activity against prostate cancer cells, suggesting them as potential lead compounds for therapy development.
451 citations
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March 2005 in “Endocrine Reviews” This paper discusses the role of steroid sulfatase in hormone-dependent tumors and highlights the development of potent inhibitors, noting the commencement of a phase I trial for one inhibitor in postmenopausal breast cancer patients.
45 citations
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August 2005 in “Bioorganic & medicinal chemistry” This study found that novel androgen antagonists incorporating a carborane moiety showed anti-androgenic activity comparable to flutamide in a laboratory setting.