TY - JOUR
T1 - Antineoplastic Agents. 606. the Betulastatins
AU - Pettit, George
AU - Melody, Noeleen
AU - Chapuis, Jean
N1 - Funding Information:
We acknowledge with special thanks the financial support from the Arizona Biomedical Research Commission, grant no. R01 CA90441 from the Division of Cancer Treatment and Diagnosis, NCI, NIH, the J.W. Kiecknefer Foundation, and the Margaret T. Morris Foundation. We are grateful to Dr. J. C. Knight and N. Zolotova, Arizona State University, for the HRMS data.
Publisher Copyright:
© 2018 American Chemical Society and American Society of Pharmacognosy.
PY - 2018/3/23
Y1 - 2018/3/23
N2 - The medicinal potential of the plant pentacyclic triterpene betulin has generated long-term interest focused on various SAR research avenues. The present approach was based on producing further analogues (chimeras) arising from a studied modification of betulin bonded to the Dov-Val-Dil-Dap unit of the powerful anticancer drug dolastatin 10, which provided betulastatins 1 (7b), 2 (11b), 3 (16b), and 4 (18b). Betulastatin 1, 2, and 4 exhibited modest levels of cancer cell growth inhibition against six cancer cell lines. Betulastatin 3 proved to be the most potent cancer cell growth inhibitor (GI 50 0.01 μg/mL) and seems worthy of further development, as the presumed mixture of anticancer mechanisms of action may prove to be useful.
AB - The medicinal potential of the plant pentacyclic triterpene betulin has generated long-term interest focused on various SAR research avenues. The present approach was based on producing further analogues (chimeras) arising from a studied modification of betulin bonded to the Dov-Val-Dil-Dap unit of the powerful anticancer drug dolastatin 10, which provided betulastatins 1 (7b), 2 (11b), 3 (16b), and 4 (18b). Betulastatin 1, 2, and 4 exhibited modest levels of cancer cell growth inhibition against six cancer cell lines. Betulastatin 3 proved to be the most potent cancer cell growth inhibitor (GI 50 0.01 μg/mL) and seems worthy of further development, as the presumed mixture of anticancer mechanisms of action may prove to be useful.
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U2 - 10.1021/acs.jnatprod.7b00536
DO - 10.1021/acs.jnatprod.7b00536
M3 - Article
C2 - 29303263
AN - SCOPUS:85044547023
SN - 0163-3864
VL - 81
SP - 458
EP - 464
JO - Journal of Natural Products
JF - Journal of Natural Products
IS - 3
ER -