154548-45-5Relevant articles and documents
Synthesis and antitumor evaluation of novel 4-anilino-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate derivatives as potential EGFR inhibitors
Zhang, Dajun,Yan, Yan,Jin, Ge,Liu, Bo,Ma, Xiaoliang,Han, Dan,Jia, Xiaojian
, (2018)
Novel series of 4-anilino-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylates (5a–p, 7, and 8a–e) were synthesized and evaluated for their antiproliferative activity against the A549, HT29, H460, and H1975 cancer cell lines in vitro. Nine compounds (5a–c, 5i, 5j, 7, 8a, 8b, 8i) demonstrated moderate to significant cytotoxic activity with IC50 values below 18 μM on A549 cells, which were comparable to that of the reference gefitinib (IC50 = 18.44 μM). Especially, the further enzymatic analysis on epidermal growth factor receptor (EGFR), HER2, and VEGFR identified compound 5a as a promising hit that exhibited considerable potency both in cellular (IC50 = 5.67, 17.04, 11.29, and 12.65 μM, respectively) and EGFR enzymatic assays (IC50 = 14.8 nM). Compound 5a was capable of down-regulating the expression of EGFR and inhibited EGFR phosphorylation in a dose-dependent manner, representing a potential EGFR candidate for further optimization.
6 SUBSTITUTED 2-HETEROCYCLYLAMINO PYRAZINE COMPOUNDS AS CHK-1 INHIBITORS
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Page/Page column 95-96, (2010/04/03)
The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, their synthesis, and their use as CHK-1 inhibitors.
Immunopotentiator agents
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Page column 10, (2010/02/05)
Novel compounds and methods for preparing same, immunopotentiating compositions, and a method for potentiating the immune system of a host animal. The method comprises administering to the animal an effective amount of an immunopotentiating compound of Formula I or Formula II, or a physiologically acceptable salt.