estradiol-3-o-sulfamate and Carcinoma--Lewis-Lung

estradiol-3-o-sulfamate has been researched along with Carcinoma--Lewis-Lung* in 1 studies

Other Studies

1 other study(ies) available for estradiol-3-o-sulfamate and Carcinoma--Lewis-Lung

Article	Year
2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity. Journal of medicinal chemistry, 2006, Dec-28, Volume: 49, Issue:26 The anticancer activities and SARs of estradiol-17-O-sulfamates and estradiol 3,17-O,O-bis-sulfamates (E2bisMATEs) as steroid sulfatase (STS) inhibitors and antiproliferative agents are discussed. Estradiol 3,17-O,O-bis-sulfamates 20 and 21, in contrast to the 17-O-monosulfamate 11, proved to be excellent STS inhibitors. 2-Substituted E2bisMATEs 21 and 23 additionally exhibited potent antiproliferative activity with mean graph midpoint values of 18-87 nM in the NCI 60-cell-line panel. 21 Exhibited antiangiogenic in vitro and in vivo activity in an early-stage Lewis lung model, and 23 dosed p.o. caused marked growth inhibition in a nude mouse xenograft tumor model. Modeling studies suggest that the E2bisMATEs and 2-MeOE2 share a common mode of binding to tubulin, though COMPARE analysis of activity profiles was negative. 21 was cocrystallized with carbonic anhydrase II, and X-ray crystallography revealed unexpected coordination of the 17-O-sulfamate of 21 to the active site zinc and a probable additional lower affinity binding site. 2-Substituted E2bisMATEs are attractive candidates for further development as multitargeted anticancer agents. Topics: Animals; Antineoplastic Agents; Binding Sites; Breast Neoplasms; Carbonic Anhydrase II; Carcinoma, Lewis Lung; Cell Proliferation; Crystallography, X-Ray; Estradiol; Female; Humans; Mice; Mice, Nude; Models, Molecular; Neovascularization, Pathologic; Steryl-Sulfatase; Structure-Activity Relationship; Sulfonic Acids; Survival Rate; Tumor Cells, Cultured; Xenograft Model Antitumor Assays; Zinc	2006

Article

Year

2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity.

Journal of medicinal chemistry, 2006, Dec-28, Volume: 49, Issue:26

The anticancer activities and SARs of estradiol-17-O-sulfamates and estradiol 3,17-O,O-bis-sulfamates (E2bisMATEs) as steroid sulfatase (STS) inhibitors and antiproliferative agents are discussed. Estradiol 3,17-O,O-bis-sulfamates 20 and 21, in contrast to the 17-O-monosulfamate 11, proved to be excellent STS inhibitors. 2-Substituted E2bisMATEs 21 and 23 additionally exhibited potent antiproliferative activity with mean graph midpoint values of 18-87 nM in the NCI 60-cell-line panel. 21 Exhibited antiangiogenic in vitro and in vivo activity in an early-stage Lewis lung model, and 23 dosed p.o. caused marked growth inhibition in a nude mouse xenograft tumor model. Modeling studies suggest that the E2bisMATEs and 2-MeOE2 share a common mode of binding to tubulin, though COMPARE analysis of activity profiles was negative. 21 was cocrystallized with carbonic anhydrase II, and X-ray crystallography revealed unexpected coordination of the 17-O-sulfamate of 21 to the active site zinc and a probable additional lower affinity binding site. 2-Substituted E2bisMATEs are attractive candidates for further development as multitargeted anticancer agents.

Topics: Animals; Antineoplastic Agents; Binding Sites; Breast Neoplasms; Carbonic Anhydrase II; Carcinoma, Lewis Lung; Cell Proliferation; Crystallography, X-Ray; Estradiol; Female; Humans; Mice; Mice, Nude; Models, Molecular; Neovascularization, Pathologic; Steryl-Sulfatase; Structure-Activity Relationship; Sulfonic Acids; Survival Rate; Tumor Cells, Cultured; Xenograft Model Antitumor Assays; Zinc

2006