title: Synthesis, anticancer, and antibacterial activities of piplartine derivatives on cell cycle regulation and growth inhibition.
abstract: A series of piplartine derivatives were synthesized via Baylis-Hillman reaction and evaluated for anticancer and antibacterial activities. The cytotoxicity of these compounds was examined in two different human tumor cell lines, IMR-32 and HeLa. The antibacterial activity was examined in Staphylococcus aureus and Pseudomonas aeruginosa. The results showed that compounds 2b, 2e, and 2j were found to be the most active compounds, which displayed line no cytotoxicity, but G2-M cell cycle arrest in tumor cells, and showed cytostatic effects in bacteria.
authors.affiliation: Centre for Cellular and Molecular Biology, Hyderabad 500 007, India.
authors.forename: J Ujwal
authors.initials: JU
authors.lastname: Kumar
authors.forename: G
authors.initials: G
authors.lastname: Shankaraiah
authors.forename: R Sateesh Chandra
authors.initials: RS
authors.lastname: Kumar
authors.forename: V V
authors.initials: VV
authors.lastname: Pitke
authors.forename: G Tirupathi
authors.initials: GT
authors.lastname: Rao
authors.forename: B
authors.initials: B
authors.lastname: Poornima
authors.forename: K Suresh
authors.initials: KS
authors.lastname: Babu
authors.forename: A S
authors.initials: AS
authors.lastname: Sreedhar
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D031701:Piper / Q000737:chemistry; D010881:Piperidones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects
chemical_list: C583250:(E)-3-(hydroxy(4-nitrophenyl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one; C583249:(E)-3-(hydroxy(phenyl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one; C583248:(E)-3-(hydroxy(thiophen-2-yl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one; D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D010881:Piperidones; C498077:piperlongumine