Detail of "116057-75-1"

Reference

Pyrrolidino-4-iodotamoxifen and 4-iodotamoxifen, new analogs of the antiestrogen tamoxifen for the treatment of breast cancer

Pyrrolidino-4-iodotamoxifen and 4-iodotamoxifen, new analogs of the antiestrogen tamoxifen for the treatment of breast cancer. Chander, S.Some chemicals with cas registry numbers like 116057-75-1 and 116057-66-0 are also used. K.; McCague, R.; Luqmani, Y.; Newton, C.; Dowsett, M.; Jarman, M.; Coombes, R. C. (Med. Sch., St. George's Hosp., London SW17 0RE, UK). Cancer Res., 51(21), 5851-8 (English) 1991. CODEN: CNREA8. ISSN: 0008-5472. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) New tamoxifen analogs were tested for their antiproliferative activity both in vitro and in vivo. Binding studies showed that both 4-iodotamoxifen and pyrrolidino-4-iodotamoxifen and 2.5-fold higher affinities for the estrogen receptor compared with tamoxifen. Pyrrolidino-4-iodotamoxifen was also 1.5-fold more effective in causing inhibition of estrogen-induced growth of MCF-7 cells compared with tamoxifen at 10-6 M. The 4-iodotamoxifen analog was similar to tamoxifen in its inhibitory action at 10-6 M. Antiproliferative activities of these drugs were tested using the nitrosomethylurea-induced rat mammary tumor model. Pyrrolidino-4-iodotamoxifen caused regression in 92% of rats, whereas tamoxifen caused regression in 75% of rats. The agonist activity of the analogs was detd. using the immature rat and mouse uterotrophic assays. Both tamoxifen and 4-iodotamoxifen had similar partial agonist activity, and this was greater than that seen with pyrrolidino-4-iodotamoxifen. Furthermore, pyrrolidino-4-iodotamoxifen caused a dose-dependent inhibition of estrogen-induced vaginal cornification, whereas tamoxifen and 4-iodotamoxifen did not. These studies demonstrate that pyrrolidino-4-iodotamoxifen is more effective than tamoxifen in inhibiting tumor regression and that its reduced uterotropic activity and increased estrogen receptor binding may give it significant clin. advantages over the parent compd. .

Prevention and treatment of cardiovascular pathologies with tamoxifen analogs

Prevention and treatment of cardiovascular pathologies with tamoxifen analogs. Grainger, David J.; Metcalfe, James C.; Kunz, Lawrence L.; Kemp, Paul R.; Schroff, Robert W.; Weissberg, Peter L. (Neorx Corporation; Grainger, David J.; Metcalfe, James C.; Kunz, Lawrence L.; Kemp, Paul R. 84449-90-1 and 116057-75-1 are cas registry numbers. These chemicals are also mentioned in this article.; Schroff, Robert W.; Weissberg, Peter L., USA). PCT Int. Appl. WO 9640098 A2 19 Dec 1996, 130 pp. DESIGNATED STATES: W: AL, AM, AT, AU, AZ, BB, BG, BR, BY, CA, CH, CN, CZ, DE, DK, EE, ES, FI, GB, GE, HU, IL, IS, JP, KE, KG, KP, KR, KZ, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, NL, PT, SE. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: A61K031-135. APPLICATION: WO 1996-US10211 7 Jun 1996. PRIORITY: US 1995-478936 7 Jun 1995; US 1995-476735 7 Jun 1995; US 1995-477393 7 Jun 1995; US 1995-486334 7 Jun 1995. DOCUMENT TYPE: Patent CA Section: 1 (Pharmacology) Section cross-reference(s): 63 A method for treating or preventing cardiovascular pathologies comprises administering a compd. I (Z = C:O, covalent bond; Y = H, O(C1-4)alkyl; R1, R2 = (C1-4)alkyl, together with N satd. heterocyclic group; R3 = Et, chloroethyl; R4 = H; R5 = I, O(C1-4)alkyl, H; R6 = I, O(C1-C4)alkyl, H, with the proviso that when R4, R5, and R6 are H, R3 is not ethyl) or a pharmaceutically acceptable salt thereof, effective to elevate the level of TGF-b to treat and/or prevent conditions such as atherosclerosis, thrombosis, myocardial infarction, and stroke is provided. Useful compds. include idoxifene, raloxifene, toremifene, droloxifene or salts thereof. A method for identifying an agent that elevates the level of TGF-beta and an assay or kit to det. TGF-b based on anti-TGF-b-antibodies are also provided. Tamoxifen (1.1 mg/kg/day) strongly inhibited the formation of lipid lesions induced by a high fat diet in mice. The major effect of tamoxifen in mice was to elevate TGF-b in aortic wall and in circulation. .