22367-82-4Relevant articles and documents
Benzofuran-Based Carboxylic Acids as Carbonic Anhydrase Inhibitors and Antiproliferative Agents against Breast Cancer
Abdel-Aziz, Hatem A.,Al-Sanea, Mohammad M.,Al-Warhi, Tarfah,Aljaeed, Nada,Alotaibi, Ohoud J.,Eldehna, Wagdy M.,Elsayed, Zainab M.,Nocentini, Alessio,Supuran, Claudiu T.
, p. 1022 - 1027 (2020)
Pursuing our effort for developing effective inhibitors of the cancer-related hCA IX isoform, here we describe the synthesis of novel benzofuran-based carboxylic acid derivatives, featuring the benzoic (9a-f) or hippuric (11a,b) acid moieties linked to 2-
Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors
Shaldam, Moataz,Eldehna, Wagdy M.,Nocentini, Alessio,Elsayed, Zainab M.,Ibrahim, Tamer M.,Salem, Rofaida,El-Domany, Ramadan A.,Capasso, Clemente,Abdel-Aziz, Hatem A.,Supuran, Claudiu T.
, (2021)
In the present study, we describe the design of different series of benzofuran-based derivatives as potential carbonic anhydrase inhibitors (CAIs). The adopted design is based on bioisosteric replacement for the p-fluorophenyl SLC-0111 tail with the lipop
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Wesson et al.
, p. 4265 (1977)
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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.
