Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 22, Pages 6481-6489Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.09.030
Keywords
Synthesis; Diterpenes; Levopimaric acid; Quinopimaric acid; Maleopimaric acid; Anticancer activity
Funding
- Russian Foundation for Basic Research [11-03-12144]
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A series of quinopimaric and maleopimaric acids' derivatives modified in the E-ring, at the carbonyl-and carboxyl-groups were synthesized and their in vitro cytotoxic activity was evaluated at the National Cancer Institute, USA. Methyl esters of dihydroquinopimaric, 1a,4a-dehydroquinopimaric, 2,3-epoxyquinopimaric, 1-ethylenketal-dihydroquinopimaric, 1-ethylenketal-4-hydroxyiminodihydroquinopimaric acids displayed an activity on renal cancer, leukemia, colon cancer and breast cancer cell lines in concentration 10 (5) M. Methyl 1,4-dihydroxyiminodihydroquinopimarate showed both a potent and broad spectrum of cytotoxic activity against NSC lung cancer, colon cancer, breast cancer, renal cancer and leukemia and revealed in vivo antineoplastic activity towards mouse solid transplantable mammary carcinoma Ca755 and colon adenocarcinoma AKATOL. The information about antineoplastic activity of the studied quinopimaric and maleopimaric acids' derivatives will be used for hit to lead optimization in these chemical series. (C) 2014 Elsevier Ltd. All rights reserved.
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