Bakherad, Z; Safavi, M; Fassihi, A; Sadeghi-Aliabadi, H; Bakherad, M; Rastegar, H; Saeedi, M; Ghasemi, JB; Saghaie, L; Mahdavi, M in [Bakherad, Zohreh; Fassihi, Afshin; Sadeghi-Aliabadi, Hojjat; Saghaie, Lotfollah] Isfahan Univ Med Sci, Sch Pharm & Pharmaceut Sci, Dept Med Chem, Esfahan 8174673461, Iran; [Safavi, Maliheh] Iranian Res Org Sci & Technol, Dept Biotechnol, Tehran 33535111, Iran; [Bakherad, Mohammad] Shahrood Univ Technol, Sch Chem, Shahrood 3619995161, Iran; [Rastegar, Hossein] MOE, Food & Drug Lab Res Ctr, Food & Drug Control Labs, Tehran 1113615911, Iran; [Rastegar, Hossein] ME, Tehran 1113615911, Iran; [Saeedi, Mina] Univ Tehran Med Sci, Med Plants Res Ctr, Fac Pharm, Tehran 14176, Iran; [Saeedi, Mina] Univ Tehran Med Sci, Persian Med & Pharm Res Ctr, Tehran 14176, Iran; [Ghasemi, Jahan B.] Univ Tehran, Sch Sci, Fac Chem, Drug Design Silico Lab, Tehran 1417614418, Iran; [Mahdavi, Mohammad] Univ Tehran Med Sci, Endocrinol & Metab Res Inst, Endocrinol & Metab Res Ctr, Tehran 1417653761, Iran published Design and Synthesis of Novel Cytotoxic Indole-Thiosemicarbazone Derivatives: Biological Evaluation and Docking Study in 2019.0, Cited 50.0. Quality Control of 4′-Hydroxyacetophenone. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.
In this work, two novel series of indole-thiosemicarbazone derivatives were designed, synthesized, and evaluated for their cytotoxic activity against MCF-7, A-549, and Hep-G2cell lines in comparison to etoposide and colchicine as the reference drugs. Generally, the synthesized compounds showed better cytotoxicity towards A-549 and Hep-G2 than MCF-7. Among them, (2E)-2-{[2-(4-chlorophenyl)-1H-indol-3-yl]methylidene}-N-(4-methoxyphenyl)hydrazinecarbothioamide (8l) was found to be the most potent compound against A-549 and Hep-G2, at least three times more potent than etoposide. The morphological analysis by the acridine orange/ethidium bromide double staining test and flow cytometry analysis indicated that compound 8l induced apoptosis in A-549 cells. Moreover, molecular docking methodology was exploited to elucidate the details of molecular interactions of the studied compounds with putative targets.
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Reference:
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