@article{d4b208d5550840d7bddfe1f9ca4ae397,
title = "Design, synthesis and biological evaluation of dihydronaphthalene and benzosuberene analogs of the combretastatins as inhibitors of tubulin polymerization in cancer chemotherapy",
abstract = "A novel series of dihydronaphthalene and benzosuberene analogs bearing structural similarity to the combretastatins in terms of 1,2-diarylethene, trimethoxyphenyl, and biaryl functionality has been synthesized. The compounds have been evaluated in regard to their ability to inhibit tubulin assembly and for their cytotoxicity against selected human cancer cell lines. From this series of compounds, benzosuberene analogs 2 and 4 inhibited tubulin assembly at concentrations comparable to that of combretastatin A-4 (CA4) and combretastatin A-1 (CA1). Furthermore, analog 4 demonstrated remarkable cytotoxicity against the three human cancer cell lines evaluated (for example GI50 = 0.0000032 μM against DU-145 prostate carcinoma).",
keywords = "Benzosuberenes, Cancer Chemotherapy, Combretastatins, Dihydronaphthalenes, Tubulin, Vascular disrupting agents",
author = "Madhavi Sriram and Hall, {John J.} and Grohmann, {Nathan C.} and Strecker, {Tracy E.} and Taylor Wootton and Andreas Franken and Trawick, {Mary Lynn} and Pinney, {Kevin G.}",
note = "Funding Information: The authors are grateful to Oxigene Inc. (Waltham, MA, grants to K.G.P. and M.L.T.), the Welch Foundation (Grant No. AA-1278 to K.G.P.), and the National Science Foundation for funding both the Varian 500 MHz NMR spectrometer (Award CHE-0420802) and the Bruker X8 APEX diffractometer (Grant CHE-0321214). The authors are thankful to Dr. Benon E. Mugabe (former Baylor Graduate student) for performing the tubulin assay for compounds 1 and 2 . The authors would like to thank Dr. Alejandro Ramirez (Mass Spectrometry Core Facility, Baylor University) for HRMS analysis. The authors also thank H&B Packing (Waco, TX) for providing calf brain, and are grateful to Ms. Beverly Herrington (Undergraduate student, Baylor University, 2003) and Mr. Ankur Gupta [Baylor high school summer science research program (HSSSRP), 2003] for their valuable assistance with chemical synthesis. ",
year = "2008",
month = sep,
day = "1",
doi = "10.1016/j.bmc.2008.07.050",
language = "English (US)",
volume = "16",
pages = "8161--8171",
journal = "Bioorganic and Medicinal Chemistry",
issn = "0968-0896",
publisher = "Elsevier Limited",
number = "17",
}