Meirelles, MA; Braga, CB; Ornelas, C; Pilli, RA in [Meirelles, Matheus A.; Braga, Carolyne B.; Ornelas, Catia; Pilli, Ronaldo A.] Univ Estadual Campinas, UNICAMP, Inst Chem, Dept Organ Chem, BR-13083970 Campinas, SP, Brazil published Synthesis of Nitrogen-Containing Goniothalamin Analogues with Higher Cytotoxic Activity and Selectivity against Cancer Cells in 2019.0, Cited 41.0. Application In Synthesis of 4-Nitrobenzoic acid. The Name is 4-Nitrobenzoic acid. Through research, I have a further understanding and discovery of 62-23-7.
Two series of racemic goniothalamin analogues displaying nitrogen-containing groups were designed and synthesized. A total of 19 novel analogues were evaluated against a panel of four different cancer cell lines, along with the normal prostate cell line PNT2 to determine their selectivity. Among them, goniothalamin chloroacrylamide 13 e displayed the lowest IC50 values for both MCF-7 (0.5 mu m) and PC3 (0.3 mu m) cells, about 26-fold more potent than goniothalamin (1). Besides its higher potency, compound 13 e also displayed much higher selectivity than goniothalamin. In contrast, goniothalamin isobutyramide 13 c was the most potent analogue against Caco-2 cells (IC50=0.8 mu m), about 10-fold more potent and 17-fold more selective than 1. These results reveal the potential of compounds 13 c and 13 e for further in vivo studies, representing the first goniothalamin analogues with IC50 values in the low micromolar range and high selectivity against MCF-7, Caco-2, and PC3 cancer cell lines.
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Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem