517894-64-3

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• 86770-31-2 2-tert-butyl 4-ethyl 3,5-dimethyl-1H-pyrrole-2,4-dicarboxylate 

Relevant academic research and scientific papers

Synthesis and evaluation of novel 2-pyrrolidone-fused (2-oxoindolin-3-ylidene)methylpyrrole derivatives as potential multi-target tyrosine kinase receptor inhibitors

Signaling pathways of VEGFs and PDGFs are crucial in tumor angiogenesis, which is essential in solid tumor progression and metastasis. This study reports our strategy for designing and synthesizing a series of novel 2-pyrrolidone-fused (2-oxoindolin-3-ylidene)methylpyrrole derivatives as potential multi-target tyrosine kinase receptor inhibitors. The target compounds were obtained by condensation of 5-substituted oxindoles with N-substituted 2-pyrrolidone aldehyde 7 in satisfactory yields. Of these, 11 and 12 had the highest potency and, compared to sunitinib, showed: (1) significant increase in anti-proliferation of various cancer cells with a favorable selective index (SI); (2) higher inhibitory potency against both VEGFR-2 and PDGFRβ. The molecular modeling results showed that, in terms of VEGFR-2 binding, the synthesized products had a similar binding mode to sunitinib but with tighter interaction.

Readily synthesized novel fluorescent dipyrrinones

(Chemical Equation Presented) A new, highly fluorescent (φF up to 0.85) rigid anti-Z-dipyrrinone chromophore has been synthesized in high yield in a one-pot reaction by condensing two monopyrroles in the presence of DBU to form the pyrrolo[3,2-f]indolizine-4,6-dione nucleus.

Synthesis method of henatinib intermediate and obtained henatinib intermediate

The invention discloses a synthesis method of a henatinib intermediate and the obtained henatinib intermediate. The preparation method comprises the following steps of: (1) adding 3, 5-dimethyl-1H-pyrrole-2, 4-dicarboxylic acid-2-tert-butyl-4-ethyl ester into an organic solvent, then adding ceric ammonium nitrate, and reacting at room temperature to obtain an intermediate 1; (2) under the protection of inert gas, adding the intermediate 1 into an organic solvent, then adding (benzyloxyethyl) phenylphosphine, and reacting at room temperature to obtain an intermediate 2; and (3) adding the intermediate 2 into methanol, then adding a palladium-carbon catalyst, introducing hydrogen, and fully reacting at 30-35 DEG C to obtain the henatinib intermediate. The method has few reaction steps, only comprises three steps of oxidation, Wittig reaction and hydrogenation, does not have a hydrolysis process, avoids the phenomenon of environmental unfriendliness caused by a large amount of acid water, does not have a reduction reaction process of an expensive reducing agent, and is simple to operate, high in yield, few in impurities and high in purity.

COMPOUNDS FOR TREATING OR PREVENTING CANCER

The present invention provides a compound Formula I or a pharmaceutically acceptable salt or a physiologically functional derivative thereof:. In addition, the prevent invention provides a pharmaceutical composition comprising the compound, and a method for treating or preventing receptor tyrosine kinases (RTKs)-related cancer with the compound.

PHARMACEUTICALLY ACCEPTABLE SALTS OF PYRROLO-NITROGENOUS HETEROCYCLIC DERIVATIVES, PREPARATION METHOD AND MEDICAL USE THEREOF

Pharmaceutically acceptable salts of pyrrolo-nitrogenous heterocyclic derivatives, preparation method and medical use thereof are disclosed. More specifically, pharmaceutically acceptable salts of (R,Z)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-methylene)-5-(2-hydroxy-3-morpholinyl-4-yl-propyl)-3-methyl-5,6,7,8-tetrahydro-1H-pyrrolo[3,2-c]azepin-4-one presented by formula (I), the preparation method and the use thereof as therapeutic agents, especially as protein kinase inhibitors, are disclosed.

PYRROLO-NITROGENOUS HETEROCYCLIC DERIVATIES,THE PREPARATION AND THE PHARMCETICAL USE THEEOF

The invention provides new pyrrolo-nitrogenous heterocyclic derivatives represented by formula (I) or their salts, the preparation thereof, pharmaceutical compositions containing such derivatives and the use of such derivatives as therapeutic agents, especially as protein kinase inhibitors, wherein each substituent in formula (I) is same as defined in the description.

PYRROLO-NITROGENOUS HETEROCYCLIC DERIVATIVES, THE PREPARATION AND THE PHARMACEUTICAL USE THEREOF

The invention provides new pyrrolo-nitrogenous heterocyclic derivatives represented by formula (I) or their salts, the preparation thereof, pharmaceutical compositions containing such derivatives and the use of such derivatives as therapeutic agents, espe

Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: Synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives

The inhibition of receptor tyrosine kinases (RTKs) has become a successful approach in the development of anticancer agents. Many potent small-molecule kinase inhibitors have been discovered. We report herein a series of pyrrolo-fused-heterocycle-2-indolinone analogues as inhibitors of vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), and c-Kit. Among them, some pyrrolo-fused six- and seven-membered-heterocycle derivatives such as 9, 15, 23, and 25 are potent inhibitors of VEGFR, PDGFR, and c-Kit both enzymatically (50 nM) and cellularly (50 nM). Furthermore, compounds 9 and 25 possess favorable pharmacokinetic profiles and demonstrate good efficacies against human HT-29 cell colon tumor xenografts in nude mice. Further evaluations are in progress.