کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373562 | 981903 | 2007 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110α inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and biological evaluation of pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110α inhibitors Synthesis and biological evaluation of pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110α inhibitors](/preview/png/1373562.png)
چکیده انگلیسی
4-Morpholin-4-ylpyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine 2a was discovered in our chemical library as a novel p110α inhibitor with an IC50 of 1.4 μM. By structural modification of 2a, the 2-aryl-4-morpholinopyrido[3′,2′:4,5]furo[3,2-d]pyrimidine derivative 10e was discovered as a p110α inhibitor with approximately 400-fold greater potency than 2a. Evaluation of isoform selectivity showed that 10e is a potent inhibitor of p110β. Furthermore, 10e showed anti-proliferative activity in various cell lines, including multi-drug resistant MCF7/ADR-res cells, and was effective against HeLa human cervical tumor xenografts in nude mice.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 9, 1 May 2007, Pages 2438–2442
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 9, 1 May 2007, Pages 2438–2442
نویسندگان
Masahiko Hayakawa, Hiroyuki Kaizawa, Hiroyuki Moritomo, Tomonobu Koizumi, Takahide Ohishi, Mayumi Yamano, Minoru Okada, Mitsuaki Ohta, Shin-ichi Tsukamoto, Florence I. Raynaud, Paul Workman, Michael D. Waterfield, Peter Parker,