3781-69-9Relevant articles and documents
4-Hydroxy-3-methylbenzofuran-2-carbohydrazones as novel LSD1 inhibitors
Gao, Yuan,He, Xingrui,Hui, Zi,Shen, Guodong,Wang, Shuo,Xie, Tian,Ye, Xiang-Yang
, (2020/03/31)
Histone lysine specific demethylase 1 (LSD1 or KDM1A) is a potential therapeutic target in oncology due to its overexpression in various human tumors. We report herein a new class of benzofuran acylhydrazones as potent LSD1 inhibitors. Among the 31 compounds prepared, 14 compounds exhibited excellent LSD1 inhibitory activity with IC50 values ranging from 7.2 to 68.8 nM. In cellular assays, several compounds inhibited the proliferations of various cancer cell lines, including PC-3, MCG-803, U87 MG, PANC-1, HT-29 and MCF-7. This opens up the opportunity for further optimization and investigation of this class compounds for potential cancer treatment.
Preparation and application of substituted benzofuran 2-formylhydrazone LSD1 inhibitor
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, (2020/05/08)
The invention discloses a substituted benzofuran 2-formylhydrazone LSD1 inhibitor and a preparation method and an application thereof in tumor resistance. Specifically disclosed is a compound of formula (I) or a pharmaceutically acceptable salt thereof which has a good inhibitory effect on LSD1 enzyme. The invention further provides application of the compound shown in the formula (I) or the pharmaceutically acceptable salt thereof to treatment of diseases related to the expression quantity of the LSD1 enzyme, including but not limited to treatment of various cancers. The compound or the pharmaceutically acceptable salt thereof can be combined with other drugs (including but not limited to targeted drugs, various immunomodulators, anti-tumor antibodies and the like) to obtain a better cancer treatment effect.
NOVEL COMPOUNDS AND THEIR USE IN THERAPY
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Page/Page column 65-66, (2013/06/27)
The invention provides compounds which inhibit N-myristoyltransferase and are selective for protozoal N-myristoyltransferase and, consequently suitable to treat microbial infections, including viral and fungal infections, and protozoan infections such as malaria, leishmaniasis and sleeping sickness.
Design, synthesis, and biological evaluation of benzofuran derivatives as et receptor antagonists
Cai, Jin,Chen, Junqing,Cao, Meng,Wang, Peng,Feng, Chengliang,Ji, Min
, p. 5472 - 5480 (2013/12/04)
A series of novel benzofuran carboxylic acid derivatives have been designed and synthesized, with their antagonism effect screened on ET-1-induced contraction in the rat thoracic aortic ring. Some target compounds demonstrated significant inhibitory activ
Syntheses of [1,2,3]selenadiazolo[4,5-e]benzofuran or benzothiophene, [1,2,3]thiadiazolo[4,5-e]benzofuran or benzothiophene, and 2-benzofuranyl-1,3,4-oxodiazole derivatives
Shekarchi,Ellahiyan,Akbarzadeh,Shafiee
, p. 427 - 433 (2007/10/03)
Dehydrogenation of ethyl 3-methyl-4-oxo-4,5,6,7-tetrahydrobenzofuran-2-carboxylate 1 with 2,2′-azobisisobutyronitrile and N-bromosuccinimide gave ethyl 4-hydroxy-3-methylbenzofuran-2-carboxylate 3. Reaction of compounds 3-4 with hydrazine hydrate afforded
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1
Masubuchi, Miyako,Kawasaki, Ken-ichi,Ebiike, Hirosato,Ikeda, Yoshihiko,Tsujii, Shinji,Sogabe, Satoshi,Fujii, Toshihiko,Sakata, Kiyoaki,Shiratori, Yasuhiko,Aoki, Yuko,Ohtsuka, Tatsuo,Shimma, Nobuo
, p. 1833 - 1837 (2007/10/03)
Potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitors have been identified through optimization of a lead compound 1 discovered by random screening. The inhibitor design is based on the crystal structure of the CaNmt complex with compound (S)-3 and structure-activity relationships (SARs) have been clarified. Modification of the C-4 side chain of 1 has led to the discovery of a potent and selective CaNmt inhibitor 11 (RO-09-4609), which exhibits antifungal activity against C. albicans in vitro.