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2Â¥2011-05-04 20:12:46
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Ï´ÍѼÁ(½ð±Ò+1): 2011-05-04 20:34:50
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cfm877

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Ï´ÍѼÁ(½ð±Ò+1): ÕªÒªÎÒϵ½ÁË£¬Ã»ÓÐÈ«Îİ¡£¡²»¹ÜÔõÑù£¬Ð»Ð»£¡ 2011-05-05 18:00:48
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Synthesis, SAR and biological evaluation of racemic abyssinone II and analogs as potential aromatase inhibitors for prevention of breast cancer.     Maiti, Arup; Cuendet, Muriel; Croy, Vicki L.; Endringer, Denise C.; Pezzuto, John M.; Cushman, Mark.    Department of Medicinal Chemistry and Molecular Pharmacology and The Purdue Cancer Center,  Purdue University,  West Lafayette,  IN,  USA.    Abstracts of Papers, 233rd ACS National Meeting, Chicago, IL, United States, March 25-29, 2007  (2007),     MEDI-093.  Publisher: American Chemical Society,  Washington, D. C  CODEN: 69JAUY  Conference; Meeting Abstract; Computer Optical Disk  written in English.    AN 2007:295526    CAPLUS  

Abstract

Aromatase, which converts androgens to estrogens and catalyzes the transformation of pro-carcinogens to carcinogenic metabolites, is an attractive target for the chemoprevention of breast cancer.  Inhibitors of aromatase show an overall superior efficacy over selective estrogen receptor modulators (SERMs), a std. therapy used in the treatment of estrogen-receptor-pos. breast cancer in postmenopausal women.  Previous studies showed that (S)-abyssinone, isolated from Broussonetia papyrifera L., is a potent aromatase inhibitor.  An efficient approach to the synthesis of racemic abyssinone II and a series of its analogs as well as their biol. evaluation as potential selective aromatase inhibitors are described.  Racemic abyssinone II showed an IC50 value of 28.0 .mu.M by fluorimetric assay.  Several novel racemic analogs displayed increased aromatase inhibitory activity relative to abyssinone II, with IC50 values starting from as low as 1.9 .mu.M.  A structure-activity (SAR) model was established to search for new potent chemopreventive agents.  This research was supported by program project grant P01 CA48112 funded by the NCI.
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6Â¥2011-05-04 20:35:41
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cfm877

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Multi-gram total syntheses of Zapotin and ()-Abyssinone II, cancer chemopreventive natural products.     Maiti, Arup; Pezzuto, John M.; Cuendet, Muriel; Kondratyuk, Tamara; Croy, Vicki L.; Cushman, Mark.    Department of Medicinal Chemistry and Molecular Pharmacology and The Purdue Cancer Center,  Purdue University,  West Lafayette,  IN,  USA.    Abstracts of Papers, 232nd ACS National Meeting, San Francisco, CA, United States, Sept. 10-14, 2006  (2006),     MEDI-172.  Publisher: American Chemical Society,  Washington, D. C  CODEN: 69IHRD  Conference; Meeting Abstract; Computer Optical Disk  written in English.    AN 2006:861627    CAPLUS  

Abstract

Zapotin (1) and abyssinone II (2) are two natural products found in the edible plants Casimiroa edulis and Broussonetia papirifera, resp.  Very recently zapotin was evaluated in HL-60 cell differentiation (ED50 = 0.5 .mu.M) and mouse mammary organ culture model (MMOC) assays and abyssinone II was evaluated in the aromatase assay (IC50 = 0.4 .mu.M).  Both of these natural products were found to be very active as cancer chemopreventive and chemotherapeutic agents.  Based on these results, novel LiHMDS-mediated, cost efficient, multi-gram total syntheses of both natural products were carried out.  The synthetic zapotin was active in TPA-induced ornithine decarboxylase (ODC, IC50 = 1.9 .mu.M) and inhibition of NF-.kappa.B (IC50 = 16.4 .mu.M) screening assays.  Several structurally modified analogs of abyssinone II were synthesized and a structure-activity (SAR) model was established to search for new potent chemopreventive agents.  (Supported by program project grant P01 CA48112 funded by the NCI).
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7Â¥2011-05-04 20:37:52
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yxqiang119

Ìú¸Ëľ³æ (Ö°Òµ×÷¼Ò)

medal of honor

Ï´ÍѼÁ(½ð±Ò+1): 2011-05-05 18:00:56
Ï´ÍѼÁ(½ð±Ò+1): 2011-05-06 11:10:43
Ï´ÍѼÁ(½ð±Ò+1): 2011-05-08 08:52:59
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what hurts more,the painof hard work orthe pain of regrets?
8Â¥2011-05-04 21:24:41
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