title: Synthesis of terphenyl benzimidazoles as tubulin polymerization inhibitors.
abstract: A series of new terphenyl benzimidazoles (3a-z and 3aa-ad) were synthesized and evaluated for their anticancer activity. All the 30 compounds have shown moderate to good anticancer potency, however some of the compounds (3j, 3m-t and 3aa-ad) exhibited prominent anticancer potency with GI(50) values ranging from <0.1 to 9.72 μM. These compounds exhibit G2/M phase arrest and the analysis of tubulin by Western blot experiments in case of 3t and 3ad shows the disturbances that are caused in the ratio of soluble versus polymerized tubulin in cells. Compounds 3t and 3ad are the most promising candidates amongst the series and has the potential to be taken up for further detailed studies either alone or in combination with the existing therapies.
authors.affiliation: Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500607, India. ahmedkamal@iict.res.in
authors.forename: Ahmed
authors.initials: A
authors.lastname: Kamal
authors.forename: M Kashi
authors.initials: MK
authors.lastname: Reddy
authors.forename: Thokhir B
authors.initials: TB
authors.lastname: Shaik
authors.lastname: Rajender
authors.forename: Y V V
authors.initials: YV
authors.lastname: Srikanth
authors.forename: V Santhosh
authors.initials: VS
authors.lastname: Reddy
authors.forename: G Bharath
authors.initials: GB
authors.lastname: Kumar
authors.forename: Shasi V
authors.initials: SV
authors.lastname: Kalivendi
mesh_terms: D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D015153:Blotting, Western; D002453:Cell Cycle / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000378:metabolism*; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
chemical_list: D001562:Benzimidazoles; D014404:Tubulin; D050257:Tubulin Modulators