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المؤلفMalki, Ahmed
المؤلفAshour, Hayam M.A.
المؤلفElbayaa, Rasha Y.
المؤلفIssa, Doaa A. E.
المؤلفAziz, Hassan A.
المؤلفChen, Xiaozhuo
تاريخ الإتاحة2016-10-06T11:19:29Z
تاريخ النشر2015-12-18
اسم المنشورJournal of Enzyme Inhibition and Medicinal Chemistry
المعرّفhttp://dx.doi.org/10.3109/14756366.2015.1118686
الاقتباسAhmed Malki, Hayam M. A. Ashour, Rasha Y. Elbayaa, Doaa A. E. Issa, Hassan A. Aziz & Xiaozhuo Chen (2016) Novel 1,5-diphenyl-6-substituted 1H-pyrazolo[3,4- d]pyrimidin-4(5H)-ones induced apoptosis in RKO colon cancer cells, Journal of Enzyme Inhibition and Medicinal Chemistry, 31:6, 1286-1299.
الرقم المعياري الدولي للكتاب1475-6366
معرّف المصادر الموحدhttp://hdl.handle.net/10576/4833
الملخصNovel 1,5-diphenyl-6-substituted-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-ones were synthesized and characterized. All compounds were screened for their anti-proliferative activities in five different cancer cell lines. The results showed that compounds 7a and 7b comprising aminoguanidino or guanidino moiety at position 6 inhibited proliferation of RKO colon cancer cells with IC50 of 8 and 4 μM, respectively. Compounds 7a and 7b induced apoptosis in RKO cells, which was confirmed by TUNEL and annexin V-FITC assays. Flow cytometric analysis indicated that compounds 7a and 7b arrested RKO cells in the G1 phase and the most active compound 7b increased levels of p53, p21, Bax, ERK1/2 and reduced levels of Bcl2 and Akt. Compound 7b also activates release of cytochrome c, which is consistent with activation of caspase-9. Additionally, compound 7b increased caspase-3 activity and cleaved PARP-1 in RKO cells. Collectively, these findings could establish a molecular basis for the development of new anti-cancer agents.
اللغةen
الناشرTaylor & Francis
الموضوعApoptosis
caspase-3
PARP-1
pyrazolo[3,4- d]pyrimidin-4(5H)-ones
p53
RKO
العنوانNovel 1,5-diphenyl-6-substituted 1H-pyrazolo[3,4-d]pyrimidin-4(5H)-ones induced apoptosis in RKO colon cancer cells
النوعArticle
الصفحات1286-1299
رقم العدد6
رقم المجلد31
ESSN1475-6374
dc.accessType Abstract Only


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