852443-61-9Relevant articles and documents
Synthesis, anticancer activity and molecular modeling studies of 1,2,4-triazole derivatives as EGFR inhibitors
El-Sherief, Hany A.M.,Youssif, Bahaa G.M.,Abbas Bukhari, Syed Nasir,Abdelazeem, Ahmed H.,Abdel-Aziz, Mohamed,Abdel-Rahman, Hamdy M.
, p. 774 - 789 (2018/07/29)
A series of novel compounds carrying 1,2,4-triazole scaffold were prepared and evaluated for their antiproliferative activities against NCI 60 cell line. Compounds 10 (a, c), 11 (a-d), and 14 (a-e) were selected for evaluation at single concentration of 10 μM towards panel of sixty cancer cell lines. Some of nitric oxide (NO) donating triazole/oxime hybrids 11a-d showed antiproliferative activity better than their corresponding ketones. On the other hand, the thiazolo [3,2-b][1,2,4]-triazoles 14a-e showed remarkable antiproliferative activities against the same cell lines. Compound 14d was selected for five dose testing against the full panel of 60 human tumor cell lines. Compound 14d showed high selectivity against renal subpanel with selectivity ratio of 6.99 at GI50 level. Compounds 11a-d, 10a-d and 14a-e were tested against four cell lines using MTT assay then compounds of the least IC50 were evaluated against three known anticancer targets including EGFR, BRAF and Tubulin. The results revealed that compound 14d showed promising EGFR inhibitory activity of cancer cell proliferation and were also observed to be moderate BRAF and tubulin inhibitors. Moreover, cell cycle analysis and apoptosis assay were finished for compounds 14d and 14f. Finally molecular modeling studies were performed to explore the binding mode of the most active compounds to the target enzymes.
THIAZOLE CARBOXAMIDE DERIVATIVE AND METHOD FOR USE THEREOF
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Paragraph 0072-0074, (2017/10/31)
PROBLEM TO BE SOLVED: To provide a plant disease control agent having excellent performance as compared to the conventional art, particularly a compound useful as a blast control agent by box treatment and seed treatment. SOLUTION: The present invention provides a thiazole carboxamide derivative represented by formula (I) (where R is a hydrogen atom or a formyl group) or a salt thereof, and a plant disease control agent comprising the derivative as an active ingredient. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPO&INPIT
INHIBITORS OF AKT ACTIVITY
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Page/Page column 136, (2010/10/03)
The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.