129047-38-7Relevant articles and documents
HETEROARYL COMPOUNDS AS KINASE INHIBITOR
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Page/Page column 78-79, (2019/10/04)
Provided herein are heteroaryl compounds of formula (I) having activity on a receptor protein tyrosine kinase, wherein R 1, R 2, R 3, A, Q, Z, X and W are set forth in the description, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof.
3-methyl pyridino-[1,2-a] pyrimidone derivative containing 1-((4-benzyl-substituted)oxygroup) and application
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Paragraph 0094; 0096, (2019/04/30)
The invention discloses a 3-methyl pyridino-[1,2-a] pyrimidone derivative containing 1-((4-benzyl-substituted)oxygroup) and application. The general formula of the derivative is shown in the description, wherein R1 is a methoxyl group or an oxyethyl group or halogen; R2 is hydroxyl or isobutyl or ethyl or propyl or chloroethyl or 2-methoxyl group benzyl or 2-methoxyl group benzy or 2-fluorine benzyl or 2-cyanogroup benzyl chloride or 4-cyanogroup benzyl2-methyl benzyl chloride or 3-methyl benzyl chloride or 4-methyl benzyl chloride. According to the derivative, the rice bacterial leaf blight and citrus canker can be prevented and treated. The general formula is shown in the description.
First Discovery of Novel Pyrido[1,2- a]pyrimidinone Mesoionic Compounds as Antibacterial Agents
Liu, Dengyue,Zhang, Jian,Zhao, Lei,He, Wengjing,Liu, Zhengjun,Gan, Xiuhai,Song, Baoan
, (2019/10/21)
Plant bacterial diseases cause tremendous decreases in crop yield and quality, and there is a lack of highly effective and low-risk antibacterial agents. A series of novel pyrido[1,2-a]pyrimidinone mesoionic compounds containing vanillin moieties were synthesized, and the application of these mesoionic compounds as plant antibacterial agents was reported here for the first time. The bioassay results revealed that the mesoionic compounds had good antibacterial activity. Of these compounds, compound 11 showed excellent in vitro activity against Xanthomonas oryzae pv. oryzae, with an EC50 value of 1.1 μg/mL, which was substantially better than that of bismerthiazol (92.7 μg/mL) and thiodiazole copper (105.4 μg/mL). Moreover, greenhouse condition trials indicated that the protective and curative activities of compound 11 against rice bacterial leaf blight were 75.12 and 72.04%, respectively, which were better than those of bismerthiazol (62.24 and 50.83%, respectively) and thiodiazole copper (53.35 and 65.04%, respectively). These results provide a basis for the application of mesoionic vanillin moieties as new antibacterial agents.
TRICYCLIC HETEROCYCLIC DERIVATIVES AND USES THEREOF
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Paragraph 89; 90, (2018/05/24)
Disclosed are tricyclic heterocyclic compounds having kinase inhibitory activity, pharmaceutical compositions and kits comprising the compounds, and use of the compounds in the treatment of or in medicaments for the treatment of various diseases and conditions. In particular, disclosed are tricyclic heterocyclic compounds of the formula (I) having CSF-1R (c-FMS kinase) inhibitory activity and their use in the treatment of various diseases and conditions, such as those mediated by CSF-1R, including proliferative or neoplastic diseases and conditions, including cancers, and bone, inflammatory, and autoimmune diseases and conditions.
Facile and selective deprotection of PMB ethers and esters using oxalyl chloride
Ilangovan, Andivelu,Anandhan, Karnambaram,Kaushik, Mahabir Prasad
supporting information, p. 1081 - 1084 (2015/02/19)
Oxalyl chloride, (0.5 equiv) was found to cleave the PMB group from alkyl, aryl PMB ethers, and esters to give corresponding alcohol and acid in good yields. This method offers simple and efficient protocol for the selective deprotection of PMB ether and ester in DCE at ambient temperature.
Vanillin-derived antiproliferative compounds influence Plk1 activity
Carrasco-Gomez, Roberto,Keppner-Witter, Sarah,Hieke, Martina,Lange, Lisa,Schneider, Gisbert,Schubert-Zsilavecz, Manfred,Proschak, Ewgenij,Sp?nkuch, Birgit
supporting information, p. 5063 - 5069 (2014/12/11)
We synthesized a series of vanillin-derived compounds and analyzed them in HeLa cells for their effects on the proliferation of cancer cells. The molecules are derivatives of the lead compound SBE13, a potent inhibitor of the inactive conformation of huma
A convenient approach for the deprotection and scavenging of the PMB group using POCl3
Ilangovan, Andivelu,Saravanakumar, Shanmugasundar,Malayappasamy, Subramani,Manickam, Govindaswamy
, p. 14814 - 14828 (2013/09/02)
A convenient and high yielding approach for the deprotection and scavenging of the p-methoxybenzyl (PMB) group in PMB ethers and PMB esters was developed using POCl3 as the reagent. 4-Methoxybenzyl chloride, a starting material used for the preparation of PMB ethers and esters was regenerated in the deprotection step. This mild and selective procedure tolerates several acid sensitive functional groups. The Royal Society of Chemistry 2013.
PROPHYLACTIC OR THERAPEUTIC AGENT FOR CANCER
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Page/Page column 70, (2012/05/20)
A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has a superior activity as an estrogen-related receptor-α modulator, and is useful as a prophylactic or therapeutic agent for cancer.
Small molecules that protect against β-amyloid-induced cytotoxicity by inhibiting aggregation of β-amyloid
Lee, Yun Suk,Kim, Hye Yun,Kim, Youngsoo,Seo, Jae Hong,Roh, Eun Joo,Han, Hogyu,Shin, Kye Jung
experimental part, p. 4921 - 4935 (2012/10/08)
Aggregated β-amyloid (Aβ) plays crucial roles in Alzheimer's disease (AD) pathogenesis, therefore blockade of Aβ aggregation is considered as a potential therapeutic target. We designed and synthesized small molecules to reduce Aβ-induced cytotoxicity by inhibiting Aβ aggregation. The small molecules were screened via ThT, MTT, and cell-based cytotoxicity assay (Aβ burden assay). Selected compounds 1c, 1d, 1e, and 1f were then investigated by evaluating their effects on cognitive impairment of acute AD mice model. Learning and memory dysfunction by injection of Aβ(1-42) was recovered by administration of these molecules. Especially, 1d showed the best recovery activity in Y-maze task, object recognition task, and passive avoidance task with dose dependent manner. These results suggest that 1d has high potential as a therapeutic agent for AD.
Identification, synthesis, and biological evaluation of metabolites of the experimental cancer treatment drugs indotecan (LMP400) and indimitecan (LMP776) and investigation of isomerically hydroxylated indenoisoquinoline analogues as topoisomerase i poisons
Cinelli, Maris A.,Reddy, P. V. Narasimha,Lv, Peng-Cheng,Liang, Jian-Hua,Chen, Lian,Agama, Keli,Pommier, Yves,Van Breemen, Richard B.,Cushman, Mark
, p. 10844 - 10862 (2013/02/25)
Hydroxylated analogues of the anticancer topoisomerase I (Top1) inhibitors indotecan (LMP400) and indimitecan (LMP776) have been prepared because (1) a variety of potent Top1 poisons are known that contain strategically placed hydroxyl groups, which provides a clear rationale for incorporating them in the present case, and (2) the hydroxylated compounds could conceivably serve as synthetic standards for the identification of metabolites. Indeed, incubating LMP400 and LMP776 with human liver microsomes resulted in two major metabolites of each drug, which had HPLC retention times and mass fragmentation patterns identical to those of the synthetic standards. The hydroxylated indotecan and indimitecan metabolites and analogues were tested as Top1 poisons and for antiproliferative activity in a variety of human cancer cell cultures and in general were found to be very potent. Differences in activity resulting from the placement of the hydroxyl group are explained by molecular modeling analyses.