Synthesis and structure activity relationships of schweinfurthin indoles |
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| Affiliation: | 1. Department of Chemistry, University of Iowa, Iowa City, IA 52242-1294, United States;2. Molecular Targets Laboratory, Center for Cancer Research, NCI-Frederick, Frederick, MD 21702, United States;1. Department of Chemistry, Physical Chemistry Section, Visva Bharati University, Santiniketan, Birbhum 731 235, West Bengal, India;2. Department of Chemistry, Bishnupur Ramananda College, Bishnupur, Bankura 722122, West Bengal, India;3. Department of Chemistry, Brahmankhanda Basapara High School, Basapara, Birbhum 731215, West Bengal, India;1. Università degli Studi di Firenze, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino (Firenze), Italy;2. Istituto di Bioscienze e Biorisorse, CNR, Via Pietro Castellino 111, 80131 Napoli, Italy;3. Department of Chemistry, College of Science, King Saud University, PO Box 2455, Riyadh 11451, Saudi Arabia;4. Università degli Studi di Firenze, Neurofarba Department, Section of Pharmaceutical and Nutriceutical Sciences, Via U. Schiff 6, 50019 Sesto Fiorentino (Florence), Italy;1. Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China;2. Tsinghua-Peking Center for Life Sciences, China;3. Department of Pharmacology and Pharmaceutical Sciences, School of Medicine, Tsinghua University, Haidian Dist., Beijing 100084, China |
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| Abstract: | As part of a program to explore the biological activity of analogues of the natural schweinfurthins, a set of compounds has been prepared where an indole system can be viewed as a substitution for the resorcinol substructure of the schweinfurthin’s D-ring. Twelve of these schweinfurthin indoles have been prepared and evaluated in the 60 cell line screen of the National Cancer Institute. While a range of activity has been observed, it is now clear that schweinfurthin indoles can demonstrate the intriguing pattern of activity associated with the natural stilbenes. In the best cases, these indole analogues display both potency and differential activity across the various cell lines comparable to the best resorcinol analogues. |
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| Keywords: | Schweinfurthin Indole Stilbene analogues SAR |
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