On October 13, 2021, there was a patent about antitumor agents.Name: 6-Fluoro-5-nitro-1H-indole The title of the patent was Preparation of (1H-indol-5-yl)acrylamide derivatives as inhibitors of TEAD proteins and the HIPPO-YAP1/TAZ signaling cascade for the treatment of cancer. And the patent contained the following:
The invention relates to 1H-indolyl-acrylamide derivatives I [n = 0-1; R1 = a single bond, alkenyl; R2 = (fluoro)alkyl, (fluoro)alkoxy, (un)substituted Ph, etc.; R4 = H, alkyl; R7 = H, CN, alkyl; R8 = H, (un)substituted alkyl] or pharmaceutically acceptable salts thereof, useful as inhibitors of the TEAD-dependent gene transcription and the HIPPO-YAP1/TAZ signaling cascade for use in methods of treatment of cancer, such as e.g. breast, ovarian, uterine, prostate, lung, gastric, colorectal, bladder, pancreatic and liver cancers, sarcomas, esophageal, head and neck cancers, uveal melanoma or glioma, and in particular in the treatment of patients who have exhibited resistance to prior anti-cancer therapy. E.g., a multi-step synthesis of II, starting from 5-nitroindole and 3-(trifluoromethyl)benzyl bromide, was disclosed. Exemplified compounds I underwent biochem. studies in order to determine their capacity to inhibit YAP1/TAZ-TEAD or TEAD-dependent gene transcription (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Name: 6-Fluoro-5-nitro-1H-indole
The Article related to indolylacrylamide preparation tead protein hippo yap1 taz signaling cascade, antitumor breast ovarian uterine prostate lung cancer indolylacrylamide preparation, gastric colorectal bladder pancreatic liver cancer treatment indolylacrylamide preparation, sarcoma esophageal head neck cancer glioma treatment indolylacrylamide preparation and other aspects.Name: 6-Fluoro-5-nitro-1H-indole
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles