propyl-caffeate and ferulic-acid

We developed two efficient protocols for the synthesis of feruloyl and caffeoyl derivatives from commercial vanillin and veratraldehyde. Pharmacological activities were assessed against a panel of human cancer cell lines in vitro. Most synthesized compounds demonstrated attractive cytotoxicity. Several new compounds demonstrated significant antiproliferative and cytotoxic activities against HeLa and Bewo tumor cell lines. In particular, 5-nitro caffeic adamantyl ester showed broad spectrum of tumor inhibition in 10 cell lines, and reduced tumor weight by 36.7% in vivo when administered at a dose of 40 mg kg(-1).

Topics: Antineoplastic Agents, Phytogenic; Apoptosis; Caffeic Acids; Cell Line, Tumor; Cell Proliferation; Coumaric Acids; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; HeLa Cells; Hep G2 Cells; HL-60 Cells; Humans; Molecular Structure; Structure-Activity Relationship

The anticancer activities of alkyl esters and NO-donors of ferulic acid (FA) and caffeic acid (CA) were assessed by a high-throughout screening (HTS) method, and the structure-activity relationships were described. CA alkyl esters had better anticancer activities than FA alkyl esters with the same alkyl substituent. Mono-nitrates and phenylfuroxan nitrates were more potent than the dual nitrates. Phenylsulfonylfuroxan nitrates of FA, especially compounds 8b-8d, exhibited more potent activities in anticancer.

Topics: Antineoplastic Agents; Caffeic Acids; Cell Line, Tumor; Cell Proliferation; Coumaric Acids; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; HeLa Cells; High-Throughput Screening Assays; Humans; Molecular Structure; Stereoisomerism; Structure-Activity Relationship