MAHBOOBI, S and GROTHUS, G and VONANGERER, E (1994) 3-SUBSTITUTED 2-PHENYLINDOLES - SYNTHESIS AND BIOLOGICAL PROPERTIES. ARCHIV DER PHARMAZIE, 327 (8). pp. 481-492. ISSN 0365-6233,
Full text not available from this repository.Abstract
Knoevenagel-reaction of indol-3-carbaldehydes 5a,b and 7a,b with nitromethane leads to the nitroethenes 12 and 14, the analogous reaction with malodinitrile to the methylidenemalonic acid dinitriles 16.- Michael-addition of nitromethane at 12 and 14 affords the 1,3-dinitropropanes 13 and 15, reduction of 16 the methylmalonic acid dinitriles 17.- Reaction of indoles 3 with n-BuLi/phenylsulfonylchloride leads to the 3-chloroindoles 18, reaction with NaH/ethyliodide, ether cleavage and acylation to derivatives 19.- Compounds 7-11, 14-17, and 19 show affinity to the estrogen receptor. Compounds 7b, 9-11, 17b, and 19b inhibit the growth of MCF-7-and MDA-MB-231-cells. IC50-values are determined and structure-activity relationships are discussed.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | ESTROGEN-RECEPTOR AFFINITY; CYTOSTATIC ACTIVITY; HUMAN-BREAST; SECTIONS; CANCER; |
| Depositing User: | Dr. Gernot Deinzer |
| Last Modified: | 19 Oct 2022 08:40 |
| URI: | https://pred.uni-regensburg.de/id/eprint/53150 |
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