Chen, Lingfeng et al. published their research in European Journal of Medicinal Chemistry in 2017 | CAS: 4769-96-4

6-Nitro-1H-indole (cas: 4769-96-4) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Category: indole-building-block

Structure-based design and synthesis of 2,4-diaminopyrimidines as EGFR L858R/T790M selective inhibitors for NSCLC was written by Chen, Lingfeng;Fu, Weitao;Feng, Chen;Qu, Rong;Tong, Linjiang;Zheng, Lulu;Fang, Bo;Qiu, Yinda;Hu, Jie;Cai, Yuepiao;Feng, Jianpeng;Xie, Hua;Ding, Jian;Liu, Zhiguo;Liang, Guang. And the article was included in European Journal of Medicinal Chemistry in 2017.Category: indole-building-block This article mentions the following:

Mutated epidermal growth factor receptor (EGFR) is a major driver of non-small cell lung cancer (NSCLC). The EGFRT790M secondary mutation has become a leading cause of clin.-acquired resistance to gefitinib and erlotinib. Herein, structure-based design approach to increase the potency and selectivity of the previously reported reversible EGFR inhibitor I, at the kinase and cellular levels has been reported. Three-step structure-activity relationship exploration led to promising compounds II (R1 = Br; R2 = 1-methyl-1H-indol-6-yl, 2,3-dihydro-1H-inden-5-yl; R3 = OMe; R4 = 4-methyl-1-piperazinyl) with unique chem. structure and binding mode from the other third-generation tyrosine kinase inhibitors. In a human NSCLC xenograft model, the above compounds exhibited dose-dependent tumor growth suppression without toxicity. These selective inhibitors are promising drug candidates for EGFRT790M-driven NSCLC. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Category: indole-building-block).

6-Nitro-1H-indole (cas: 4769-96-4) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Category: indole-building-block

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles