title: Selenium analogues of raloxifene as promising antiproliferative agents in treatment of breast cancer.
abstract: Synthetic protocols for the preparation of selenium analogues of raloxifene were elaborated. General aim of the current research is to improve the positive impact of selenium atom introduction in drug design. Antiproliferative activity on CCL-8 (mouse sarcoma), MDA-MB-435s (human melanoma), MES-SA (human uterus sarcoma), MCF-7 (human breast adenocarcinoma), HT-1080 (human fibrosarcoma), MG-22A (mouse hepatoma) tumor cell lines, and normal cell line NIH 3T3 (mouse fibroblasts) was studied. Influence of aminoethoxy "tail" and benzoyl group position on SAR was discussed. Results of in vivo studies on BALB/c female mice with 4T1 cell induced breast cancer model showed that selenium analogue of raloxifene is able to suppress estrogen-depending tumor growth.
authors.affiliation: Department of Medicinal Chemistry, Latvian Institute of Organic Synthesis, Aizkraukles 21, LV-1006 Riga, Latvia. Electronic address: pavel.arsenyan@lycos.com.
authors.forename: Pavel
authors.initials: P
authors.lastname: Arsenyan
authors.affiliation: Department of Medicinal Chemistry, Latvian Institute of Organic Synthesis, Aizkraukles 21, LV-1006 Riga, Latvia.
authors.forename: Edgars
authors.initials: E
authors.lastname: Paegle
authors.affiliation: Department of Medicinal Chemistry, Latvian Institute of Organic Synthesis, Aizkraukles 21, LV-1006 Riga, Latvia.
authors.forename: Ilona
authors.initials: I
authors.lastname: Domracheva
authors.affiliation: Department of Medicinal Chemistry, Latvian Institute of Organic Synthesis, Aizkraukles 21, LV-1006 Riga, Latvia.
authors.forename: Anita
authors.initials: A
authors.lastname: Gulbe
authors.affiliation: Department of Medicinal Chemistry, Latvian Institute of Organic Synthesis, Aizkraukles 21, LV-1006 Riga, Latvia.
authors.forename: Iveta
authors.initials: I
authors.lastname: Kanepe-Lapsa
authors.affiliation: Department of Medicinal Chemistry, Latvian Institute of Organic Synthesis, Aizkraukles 21, LV-1006 Riga, Latvia.
authors.forename: Irina
authors.initials: I
authors.lastname: Shestakova
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000627:therapeutic use*; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D005260:Female; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008807:Mice, Inbred BALB C; D041681:NIH 3T3 Cells; D020849:Raloxifene Hydrochloride / Q000031:analogs & derivatives* / Q000494:pharmacology; D012643:Selenium / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D000970:Antineoplastic Agents; D020849:Raloxifene Hydrochloride; D012643:Selenium
keywords: Breast; Cancer; Cytotoxic activity; Raloxifene; Selenium; Selenophene