tamoxifen and Ovarian-Neoplasms

tamoxifen has been researched along with Ovarian-Neoplasms* in 2 studies

Other Studies

2 other study(ies) available for tamoxifen and Ovarian-Neoplasms

Article	Year
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101). Journal of medicinal chemistry, 2018, 09-13, Volume: 61, Issue:17 The glucocorticoid receptor (GR) has been linked to therapy resistance across a wide range of cancer types. Preclinical data suggest that antagonists of this nuclear receptor may enhance the activity of anticancer therapy. The first-generation GR antagonist mifepristone is currently undergoing clinical evaluation in various oncology settings. Structure-based modification of mifepristone led to the discovery of ORIC-101 (28), a highly potent steroidal GR antagonist with reduced androgen receptor (AR) agonistic activity amenable for dosing in androgen receptor positive tumors and with improved CYP2C8 and CYP2C9 inhibition profile to minimize drug-drug interaction potential. Unlike mifepristone, 28 could be codosed with chemotherapeutic agents readily metabolized by CYP2C8 such as paclitaxel. Furthermore, 28 demonstrated in vivo antitumor activity by enhancing response to chemotherapy in the GR Topics: Animals; Drug Discovery; Female; Hormone Antagonists; Humans; Mice; Ovarian Neoplasms; Rats; Receptors, Glucocorticoid; Swine; Swine, Miniature; Tissue Distribution; Tumor Cells, Cultured; Xenograft Model Antitumor Assays	2018
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I. Journal of medicinal chemistry, 2011, May-26, Volume: 54, Issue:10 A 14-step biomimetic synthetic route to glyceollin I (1.5% overall yield) was developed and deployed to produce the natural enantiomeric form in soy, its unnatural stereoisomer, and a racemic mixture. Enantiomeric excess was assessed by asymmetric NMR shift reagents and chiral HPLC. Antiproliferative effects were measured in human breast, ovarian, and prostate cancer cell lines, with all three chiral forms exhibiting growth inhibition (GI) in the low to mid μM range for all cells. The natural enantiomer, and in some cases the racemate, gave significantly greater GI than the unnatural stereoisomer for estrogen receptor positive (ER(+)) versus ER(-) breast/ovarian cell lines as well as for androgen receptor positive (AR(+)) versus AR(-) prostate cancer cells. Surprisingly, differences between ER(+) and ER(-) cell lines were not altered by media estrogen conditions. These results suggest the antiproliferative mechanism of glyceollin I stereoisomers may be more complicated than strictly ER interactions. Topics: Antineoplastic Agents; Biomimetics; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Chromatography, High Pressure Liquid; Drug Screening Assays, Antitumor; Female; Humans; Magnetic Resonance Spectroscopy; Male; Models, Chemical; Ovarian Neoplasms; Prostatic Neoplasms; Pterocarpans; Receptors, Estrogen; Stereoisomerism	2011

Article

Year

Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).

Journal of medicinal chemistry, 2018, 09-13, Volume: 61, Issue:17

The glucocorticoid receptor (GR) has been linked to therapy resistance across a wide range of cancer types. Preclinical data suggest that antagonists of this nuclear receptor may enhance the activity of anticancer therapy. The first-generation GR antagonist mifepristone is currently undergoing clinical evaluation in various oncology settings. Structure-based modification of mifepristone led to the discovery of ORIC-101 (28), a highly potent steroidal GR antagonist with reduced androgen receptor (AR) agonistic activity amenable for dosing in androgen receptor positive tumors and with improved CYP2C8 and CYP2C9 inhibition profile to minimize drug-drug interaction potential. Unlike mifepristone, 28 could be codosed with chemotherapeutic agents readily metabolized by CYP2C8 such as paclitaxel. Furthermore, 28 demonstrated in vivo antitumor activity by enhancing response to chemotherapy in the GR

Topics: Animals; Drug Discovery; Female; Hormone Antagonists; Humans; Mice; Ovarian Neoplasms; Rats; Receptors, Glucocorticoid; Swine; Swine, Miniature; Tissue Distribution; Tumor Cells, Cultured; Xenograft Model Antitumor Assays

2018

Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.

Journal of medicinal chemistry, 2011, May-26, Volume: 54, Issue:10

A 14-step biomimetic synthetic route to glyceollin I (1.5% overall yield) was developed and deployed to produce the natural enantiomeric form in soy, its unnatural stereoisomer, and a racemic mixture. Enantiomeric excess was assessed by asymmetric NMR shift reagents and chiral HPLC. Antiproliferative effects were measured in human breast, ovarian, and prostate cancer cell lines, with all three chiral forms exhibiting growth inhibition (GI) in the low to mid μM range for all cells. The natural enantiomer, and in some cases the racemate, gave significantly greater GI than the unnatural stereoisomer for estrogen receptor positive (ER(+)) versus ER(-) breast/ovarian cell lines as well as for androgen receptor positive (AR(+)) versus AR(-) prostate cancer cells. Surprisingly, differences between ER(+) and ER(-) cell lines were not altered by media estrogen conditions. These results suggest the antiproliferative mechanism of glyceollin I stereoisomers may be more complicated than strictly ER interactions.

Topics: Antineoplastic Agents; Biomimetics; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Chromatography, High Pressure Liquid; Drug Screening Assays, Antitumor; Female; Humans; Magnetic Resonance Spectroscopy; Male; Models, Chemical; Ovarian Neoplasms; Prostatic Neoplasms; Pterocarpans; Receptors, Estrogen; Stereoisomerism

2011