One-pot Synthesis and Antitumor Activity of Unsymmetrical Terphenyls.
In this paper a simple and efficient method for the unsymmetrical terphenyls via sequential one-pot Suzuki coupling reactions using Pd(OAc)2without isolation of the intermediate is described. The prepared terphenyls were found to possess potent anticancer properties against a panel of cancer cells which includes A549, HeLa, MCF7, DU145, HT29 and BxPC-3. Structural similarity with combretastatin A4, these terphenyls disrupted the tubulin polymerization in vitro and destabilized the microtubules in cells. Flow cytometry studies indicated growth arrest of cells in the G2/M phase of the cell cycle corresponding to antimitotic action. Furthermore, compound4cshowed potent anti-mitotic activity even in zebrafish model and could likely be a potential therapeutic compound as it is active both inin vitroandin vivo.
Sadhvi Pharma, Kukatpally IE, Hyderabad, India.
S R
SR
Punganuru
Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University Health Sciences Center, Amarillo, TX, USA.
R
R
Samala
Department of Biomedical Sciences and Cancer Biology Center, School of Pharmacy, Texas Tech University Health Sciences Center, 1406S. Coulter Dr., Amarillo, TX, USA.
K S
KS
Srivenugopal
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000494:pharmacology; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008870:Microtubules / Q000187:drug effects; D058105:Polymerization / Q000187:drug effects; D013329:Structure-Activity Relationship; D013730:Terphenyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D014404:Tubulin / Q000378:metabolism; D015027:Zebrafish
D000972:Antineoplastic Agents, Phytogenic; D013730:Terphenyl Compounds; D014404:Tubulin