29096-59-1Relevant academic research and scientific papers
Method for synthesizing formyl-substituted imidazo[1,2a]pyridine compounds
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Paragraph 0040-0043, (2019/12/29)
The invention discloses a method for synthesizing formyl-substituted imidazo[1,2a]pyridine compounds. The method is carried out according to the following steps: taking a substituted pyridine allyl amine compound represented by the formula I as an initiat
Microwave-assisted synthesis of 3-formyl substituted imidazo[1,2-a]pyridines
Kusy, Damian,Maniukiewicz, Waldemar,B?a?ewska, Katarzyna M.
supporting information, (2019/10/16)
An efficient, metal-free method for the synthesis of 3-formyl imidazo[1,2-a]pyridines is reported. The method utilises commercially available substrates and features a broad substrate scope. The intermediate enamine was isolated and a plausible reaction mechanism proposed.
Identification of the Privileged Position in the Imidazo[1,2-a]pyridine Ring of Phosphonocarboxylates for Development of Rab Geranylgeranyl Transferase (RGGT) Inhibitors
Ka?mierczak, Aleksandra,Kusy, Damian,Niinivehmas, Sanna P.,Gmach, Joanna,Joachimiak, ?ukasz,Pentik?inen, Olli T.,Gendaszewska-Darmach, Edyta,B?azewska, Katarzyna M.
supporting information, p. 8781 - 8800 (2017/11/15)
Members of the Rab GTPase family are master regulators of vesicle trafficking. When disregulated, they are associated with a number of pathological states. The inhibition of RGGT, an enzyme responsible for post-translational geranylgeranylation of Rab GTPases represents one way to control the activity of these proteins. Because the number of molecules modulating RGGT is limited, we combined molecular modeling with biological assays to ascertain how modifications of phosphonocarboxylates, the first reported RGGT inhibitors, rationally improve understanding of their structure-activity relationship. We have identified the privileged position in the core scaffold of the imidazo[1,2-a]pyridine ring, which can be modified without compromising compounds' potency. Thus modified compounds are micromolar inhibitors of Rab11A prenylation, simultaneously being inactive against Rap1A/Rap1B modification, with the ability to inhibit proliferation of the HeLa cancer cell line. These findings were rationalized by molecular docking, which recognized interaction of phosphonic and carboxylic groups as decisive in phosphonocarboxylate localization in the RGGT binding site.
Design, synthesis and biological evaluation of acylhydrazone derivatives as PI3K inhibitors
Gao, Guo-Rui,Liu, Jia-Li,Mei, De-Sheng,Ding, Jian,Meng, Ling-Hua,Duan, Wen-Hu
, p. 118 - 120 (2015/01/30)
Since the PI3K signaling pathway is the most commonly activated in human cancers, inhibition of PI3K is a promising approach to cancer therapy. In this study, a series of 2-methyl-5-nitrobenzeneacylhydrazones were designed and synthesized. All the new der
Copper-catalyzed intramolecular dehydrogenative aminooxygenation: Direct access to formyl-substituted aromatic N-heterocycles
Wang, Honggen,Wang, Yong,Liang, Dongdong,Liu, Lanying,Zhang, Jiancun,Zhu, Qiang
supporting information; experimental part, p. 5678 - 5681 (2011/08/02)
A direct synthesis of carbaldehydes through intramolecular dehydrogenative aminooxygenation has been developed. The process uses a catalytic amount of copper(II) in DMF or DMA under oxygen and does not require additional oxidants (see scheme). Mechanistic studies suggest that the carbonyl oxygen atom of the aldehyde is derived from oxygen through a copper-mediated oxygen activation process via a peroxy-copper(III) intermediate. Copyright
Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110α inhibitors
Hayakawa, Masahiko,Kaizawa, Hiroyuki,Kawaguchi, Ken-ichi,Ishikawa, Noriko,Koizumi, Tomonobu,Ohishi, Takahide,Yamano, Mayumi,Okada, Minoru,Ohta, Mitsuaki,Tsukamoto, Shin-ichi,Raynaud, Florence I.,Waterfield, Michael D.,Parker, Peter,Workman, Paul
, p. 403 - 412 (2008/02/05)
3-{1-[(4-Fluorophenyl)sulfonyl]-1H-pyrazol-3-yl}-2-methylimidazo[1,2-a]pyridine, 2a, was discovered in our chemical library as a novel p110α inhibitor with an IC50 of 0.67 μM, through screening in a scintillation proximity assay. Optimization o
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110α inhibitors
Hayakawa, Masahiko,Kawaguchi, Ken-ichi,Kaizawa, Hiroyuki,Koizumi, Tomonobu,Ohishi, Takahide,Yamano, Mayumi,Okada, Minoru,Ohta, Mitsuaki,Tsukamoto, Shin-ichi,Raynaud, Florence I.,Parker, Peter,Workman, Paul,Waterfield, Michael D.
, p. 5837 - 5844 (2008/03/18)
We have previously reported the imidazo[1,2-a]pyridine derivative 4 as a novel p110α inhibitor; however, although 4 is a potent inhibitor of p110α enzymatic activity and tumor cell proliferation in vitro, it is unstable in solution and ineffective in vivo
