30615-95-3Relevant academic research and scientific papers
Preparation method and application of compound containing zinc-bound and quinoline skeleton
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Paragraph 0150-0153, (2021/11/10)
The invention relates to the field of pharmaceutical chemistry, in particular to a novel zinc-containing binding group-containing quinoline compound. A geometric isomer, a pharmaceutically acceptable salt, solvate or prodrug thereof, a preparation method and thereof, and a pharmaceutical composition containing the compound. The invention also relates to an application of the compound in preparation of drugs for treating and/or preventing diseases mediated by c-Met tyrosine kinase and HDAC. The quinoline compounds, geometric isomers and pharmaceutically acceptable salts, solvates and prodrugs thereof are shown in the specification, and R. 1 , m, Q, X, As described in the claims and the description.
Novel 4-phenoxy pyridine derivative and application thereof
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Paragraph 0103-0107, (2021/06/02)
The invention relates to a novel 4-phenoxy pyridine derivative and application thereof. The 4-phenoxy pyridine derivative has a structure as shown in a general formula (I), and the pharmacological activity test result of the novel 4-phenoxy pyridine derivative shows that the 4-phenoxy pyridine derivative has a remarkable inhibition effect on human gastric cancer cells MKN45, human lung cancer cells A549, human lung cancer cells H460 and human colon cancer cells HT-29; and meanwhile, the invention relates to a strong c-Met kinase inhibition effect of the compounds, and also relates to application of the compounds and pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof in preparation of drugs for treating and/or preventing diseases caused by abnormal high expression of c-Met kinase, and application of the compounds and the pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof in preparation of drugs for treating and/or preventing diseases caused by abnormal high expression of c-Met kinase. particularly relates to application in preparation of medicines for treating and/or preventing cancers.
4-phenoxy pyridine derivative containing 3-pyridazinone structure, 4-pyridazinone structure and 1,2,4-triazinone structure, and applications thereof.
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Paragraph 0140-0143, (2020/02/04)
The invention relates to a 4-phenoxy pyridine derivative containing a 3-pyridazinone structure, a 4-pyridazinone structure and a 1,2,4-triazinone structure, and applications thereof. According to theinvention, the 4-phenoxy pyridine derivative has a struc
Design, synthesis and biological evaluation of novel N-[4-(2-fluorophenoxy)pyridin-2-yl]cyclopropanecarboxamide derivatives as potential c-Met kinase inhibitors
Chen, Ye,Ding, Shi,Gong, Yilin,Hao, Xuechen,Hou, Yunlei,Liu, Ju,Liu, Yajing,Shi, Jiantao,Wang, Yang,Zhou, Yunpeng
, (2020/03/31)
Three series of novel 4-phenoxypyridine derivatives containing 4-methyl-6-oxo-1,6-dihydropyridazine- 3-carboxamide, 5-methyl-4-oxo-1,4-dihydropyridazine-3-carboxamide and 4-methyl-3,5-dioxo-2,3,4,5- tetrahydro-1,2,4-triazine-6-carboxamide moieties were synthesized and evaluated for their in vitro inhibitory activitives against c-Met kinase and cytotoxic activitives against A549, H460, HT-29 cancer cell lines. The results indicated that most of the compounds showed moderate to good antitumor activitives. The most promising compound 26a (with c-Met IC50 value of 0.016 μM) showed remarkable cytotoxicity against A549, H460, and HT-29 cell lines with IC50 values of 1.59 μM, 0.72 μM and 0.56 μM, respectively. Their preliminary structure-activity relationships (SARs) studies indicate that 4-methyl-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carboxamide was more preferred as linker part, and electron-withdrawing groups on the terminal phenyl rings are beneficial for improving the antitumor activitives. Furthermore, the colony formation, acridine orange/ethidium bromide (AO/EB) staining, apoptosis, and wound-healing assay of 26a were performed on HT-29 and/or A549 cell lines.
Modification of 3,5-dioxo-2-phenyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile via mitsunobu and chan-lam coupling reaction
Ruil, Tom,Grepl, Martin,Canka, Petr
, p. 363 - 374 (2015/03/04)
Modification of 3,5-dioxo-2-phenyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile at position 4 is described. Alkylations were carried out under Mitsunobu reaction conditions in DCM or dioxane with alcohols containing tertiary amines, pyridine and imidazole heterocyclic systems, and Boc-protected amino groups. The scope of modifications was extended with arylations performed via Chan-Lam coupling reaction using copper(I) oxide as a catalyst in a DMF solution at room temperature. In order to further extend peripheral structural diversity the nitrile group at position 6 of several alkylated 1,2,4-triazines was transformed into the amidoxime functionality.
QUINOLINE COMPOUND COMPOSING 1,2,4-TRIAZINE-DIONE AND USE THEREOF
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Paragraph 0095-0096, (2013/10/07)
The present invention relates to a quinoline deravative represented by general formula (I) or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof, wherein Ar, R1, R2, R3, X, Y and n have the meanings given in the description. The present invention also relates to the comparatively strong effect of the compound represented by general formula (I) on inhibiting c-Met kinase. The present invention further relates to the use of this compound or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof in the manufacturing of a medicament for treating the disease caused by abnormally over-expressing c-Met kinase, in particular, for treating or preventing cancer.
