Article ID Journal Published Year Pages File Type
1366846 Bioorganic & Medicinal Chemistry Letters 2007 5 Pages PDF
Abstract

A series of 11 bis-indolylthiophenes of type 8–10 were obtained by cyclization of diketones 4 and 7 using Lawesson’s reagent. Derivatives 8c, 9c, 9d, and 10c were selected to be evaluated in the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity generally in the micromolar range. The most sensitive cell lines were: CCRF-CEM, MOLT-4, HL60 (TB), and RPMI-8226 of the leukemia subpanel, HT29 and HCC-2998 cell lines of the colon sub-panel, NCI-H522 of the non-small cell lung cancer sub-panel, LOX IMVI of the melanoma sub-panel, and UO-31 of the renal cancer sub-panel.

Graphical abstractThe synthesis and antitumor activity of novel 2,5-bis(3′-indolyl)thiophene derivatives are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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