title: Synthesis and anticancer activity of 2-benzylidene indanones through inhibiting tubulin polymerization.
abstract: In an attempt to discover a potent and selective anticancer agent, gallic acid has been modified to benzylidene indanones as tubulin polymerization inhibitors. These compounds were evaluated against several human cancer cell lines and also evaluated for inhibition of tubulin polymerase in in vitro assays. Three of the analogues exhibited strong cytotoxicity against human cancer cell lines IC(50)=10-880 nM and also showed tubulin polymerization inhibition (IC(50)=0.62-2.04 μM). Compound 9j, the best candidate of the series was found to be non-toxic in acute oral toxicity in Swiss-albino mice up to 1000 mg/kg dose.
authors.affiliation: CSIR, Central Institute of Medicinal and Aromatic Plants, Kukrail Picnic Spot Road, Lucknow 226 015, UP, India.
authors.forename: A P
authors.initials: AP
authors.lastname: Prakasham
authors.forename: A K
authors.initials: AK
authors.lastname: Saxena
authors.forename: Suaib
authors.initials: S
authors.lastname: Luqman
authors.forename: Debabrata
authors.initials: D
authors.lastname: Chanda
authors.forename: Tandeep
authors.initials: T
authors.lastname: Kaur
authors.forename: Atul
authors.initials: A
authors.lastname: Gupta
authors.forename: D K
authors.initials: DK
authors.lastname: Yadav
authors.forename: C S
authors.initials: CS
authors.lastname: Chanotiya
authors.forename: Karuna
authors.initials: K
authors.lastname: Shanker
authors.forename: F
authors.initials: F
authors.lastname: Khan
authors.forename: Arvind S
authors.initials: AS
authors.lastname: Negi
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D052117:Benzodioxoles; D001597:Benzylidene Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001665:Binding Sites; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003198:Computer Simulation; D006801:Humans; D007189:Indans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D017434:Protein Structure, Tertiary; D014404:Tubulin / Q000737:chemistry* / Q000378:metabolism; D050257:Tubulin Modulators / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: C000605628:3-(3',4',5'-trimethoxyphenyl)-4,5,6-trimethoxy,2-(3',4'-methylenedioxybenzylidene)indan-1-one; D000970:Antineoplastic Agents; D052117:Benzodioxoles; D001597:Benzylidene Compounds; D007189:Indans; D014404:Tubulin; D050257:Tubulin Modulators