کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1399179 1501153 2013 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and anticancer activity of novel 2-pyridyl hexahyrocyclooctathieno[2,3-d]pyrimidine derivatives
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and anticancer activity of novel 2-pyridyl hexahyrocyclooctathieno[2,3-d]pyrimidine derivatives
چکیده انگلیسی

A series of new 2-pyridyl hexahydrocycloocta [4,5]thieno[2,3-d]pyrimidines with different substituents as C-4 position was synthesized. The anticancer activity of the newly synthesized compounds was tested in vitro using a two-stage process utilizing 60 different human tumor cell lines representing leukemia, melanoma and cancers of lung, colon, central nervous system, ovary, kidney, prostate as well as breast. Compounds 4a, 6a, 7a, 7d and 7g showed potent anticancer activity at low concentrations against most of the used human tumor cell lines comparable with doxorubicin as standard potent anticancer drug (average log10 GI50 over all cell lines = −6.85). Also, compound 4b was selective against SNB-75 (CNS cancer) log10 GI50 = −5.57. Interestingly, compound 7e exhibited promising selectivity against 13 tumor cell lines showing growth inhibition percentages between 54.05 and 89.23.

Synthesis and anticancer activity of a series of new 2-pyridyl hexahydrocycloocta [4,5]thieno[2,3-d]pyrimidines with different substituents as C-4 position are presented.Figure optionsDownload as PowerPoint slideHighlights
► A series of new thieno[2,3-d]pyrimidines was synthesized.
► The anticancer activity of the new compounds was tested in vitro.
► Compounds 4a, 6a, 7a, 7d and 7g showed potent anticancer activity.
► Compounds 4b, 5a and 7e exhibited promising anticancer activity.
► Substitutions at positions 2 and 4 showed an effect on the anticancer activity.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 63, May 2013, Pages 224–230
نویسندگان
, ,