An article Design, Synthesis, and Anticancer Screening for Repurposed Pyrazolo[3,4-d]pyrimidine Derivatives on Four Mammalian Cancer Cell Lines WOS:000655074500001 published article about SERUM; INHIBITION; MECHANISMS; CELECOXIB; ANTITUMOR in [Othman, Eman M.; Dandekar, Thomas] Univ Wurzburg, Bioctr, Dept Bioinformat, D-97074 Wurzburg, Germany; [Othman, Eman M.; Bekhit, Amany A.] Minia Univ, Fac Pharm, Dept Biochem, Al Minya 61519, Egypt; [Anany, Mohamed A.] Univ Hosp Wuerzburg, Dept Internal Med 2, Div Mol Internal Med, D-97080 Wurzburg, Germany; [Anany, Mohamed A.] Natl Res Ctr, Dept Microbial Biotechnol, Div Genet Engn & Biotechnol, Giza 12622, Egypt; [Ragab, Hanan M.] Alexandria Univ, Fac Pharm, Dept Pharmaceut Chem, Alexandria 21500, Egypt; [Wahid, Ahmed] Alexandria Univ, Fac Pharm, Dept Pharmaceut Biochem, Alexandria 21500, Egypt in 2021.0, Cited 44.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9. Name: 3,4-Dimethoxybenzaldehyde
The present study reports the synthesis of new purine bioisosteres comprising a pyrazolo[3,4-d]pyrimidine scaffold linked to mono-, di-, and trimethoxy benzylidene moieties through hydrazine linkages. First, in silico docking experiments of the synthesized compounds against Bax, Bcl-2, Caspase-3, Ki67, p21, and p53 were performed in a trial to rationalize the observed cytotoxic activity for the tested compounds. The anticancer activity of these compounds was evaluated in vitro against Caco-2, A549, HT1080, and Hela cell lines. Results revealed that two (5 and 7) of the three synthesized compounds (5, 6, and 7) showed high cytotoxic activity against all tested cell lines with IC50 values in the micro molar concentration. Our in vitro results show that there is no significant apoptotic effect for the treatment with the experimental compounds on the viability of cells against A549 cells. Ki67 expression was found to decrease significantly following the treatment of cells with the most promising candidate: drug 7. The overall results indicate that these pyrazolopyrimidine derivatives possess anticancer activity at varying doses. The suggested mechanism of action involves the inhibition of the proliferation of cancer cells.
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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