title: Synthesis and anticancer activity of quinopimaric and maleopimaric  acids’ derivatives.
abstract: 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.
authors.forename: Elena V
authors.initials: EV
authors.lastname: Tretyakova
authors.forename: Irina E
authors.initials: IE
authors.lastname: Smirnova
authors.forename: Oxana B
authors.initials: OB
authors.lastname: Kazakova
authors.forename: Genrikh A
authors.initials: GA
authors.lastname: Tolstikov
authors.forename: Nadejda P
authors.initials: NP
authors.lastname: Yavorskaya
authors.forename: Irina S
authors.initials: IS
authors.lastname: Golubeva
authors.forename: Rujena B
authors.initials: RB
authors.lastname: Pugacheva
authors.forename: Galina N
authors.initials: GN
authors.lastname: Apryshko
authors.forename: Vladimir V
authors.initials: VV
authors.lastname: Poroikov
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004224:Diterpenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051379:Mice; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity
chemical_list: D000970:Antineoplastic Agents; D004224:Diterpenes; D014315:Triterpenes; C027815:maleopimaric acid; C008911:pimaric acid