Synthesis and biological evaluation of indole-based UC-112 analogs as potent and selective survivin inhibitors was written by Wang, Qinghui;Arnst, Kinsie E.;Xue, Yi;Lei, Zi-Ning;Ma, Dejian;Chen, Zhe-Sheng;Miller, Duane D.;Li, Wei. And the article was included in European Journal of Medicinal Chemistry in 2018.Safety of 6-Nitro-1H-indole This article mentions the following:
The extensive structural modification of the recently discovered selective survivin inhibitor UC-112 and the synthesis of thirty-three new analogs I [R = (5-fluoro-1H-indazol-1-yl)methyl, 7-fluoro-indol-1-ylmethyl, 2-methyl-5-methoxy-indol-1-ylmethyl, etc.] have been reported. The structure-activity relationship (SAR) study indicated that replacement of the benzyloxy moiety in UC-112 with an indole moiety was preferred to other moieties. Among these UC-112 analogs, I (R = 5-fluoro-indol-1-ylmethyl, 5-nitro-indol-1-ylmethyl, 6-chloro-indol-1-ylmethyl, 6-methoxy-indol-1-ylmethyl) showed the most potent antiproliferative activities. Interestingly, they were more potent against the P-glycoprotein overexpressing cancer cell lines compared with the parental cancer cell lines. Mechanistic studies confirmed that new analogs maintained their unique selectivity against survivin among the IAP family members. In vivo study using I (R = 5-fluoro-indol-1-ylmethyl) in a human A375 melanoma xenograft model revealed that it effectively inhibited melanoma tumor growth without observable acute toxicity. Collectively, this study strongly supports the further preclin. development of selective survivin inhibitors based on the UC-112 scaffold. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Safety of 6-Nitro-1H-indole).
6-Nitro-1H-indole (cas: 4769-96-4) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Safety of 6-Nitro-1H-indole
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