Susan L. Morris‐Natschke

New eremophilane sesquiterpenes, 6β-sarracinoyloxy-1β,10β-epoxy-furanoeremophilane (1), 6α-angeloyloxy-10βH-furanoeremophil-1-one (2), 1α-hydroxy-9-deoxycacalol (3), and 1β-hydroxy-11(R,S)-8-oxoeremophil-6,9-dien-12-al (4a+4b), together with five known sesquiterpenes (5−9) were isolated from the roots and rhizomes of Ligularia macrophylla. The structures were elucidated by spectroscopic methods including 2D NMR techniques, and the structure of 1 was confirmed by a single-crystal X-ray diffraction experiment. The compounds were also evaluated for cytotoxic activity against human lung carcinoma (A-549) and human breast adenocarcinoma (MCF-7) and were found to show only very weak cytotoxicity.

Terpene

10.1021/np070113x

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Ochrocephalamine A, a new quinolizidine alkaloid from Oxytropis ochrocephala Bunge

Tetrahedron Letters (2016)

Li-Na Liu Jian-Qiang Ran Li-Jun Li Yu Zhao Masuo Goto

Quinolizidine

10.1016/j.tetlet.2016.10.009

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Citations (16)

ChemInform Abstract: Design and Synthesis of Gambogic Acid Analogues as Potent Cytotoxic and Antiinflammatory Agents.

ChemInform (2012)

Chiao‐Ting Yen Kyoko Nakagawa‐Goto Tsong‐Long Hwang Susan L. Morris‐Natschke Kenneth F. Bastow

Abstract Prenyl‐ and pyrano‐xanthones derived from xanthenone (III), a basic backbone of gambogic acid, are synthesized and screened for in vitro cytotoxic effects against four human cancer cell lines and anti‐inflammatory activity.

Gambogic acid

10.1002/chin.201246213

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Citations (0)

Plant-derived triterpenoids and analogues as antitumor and anti-HIV agents

Natural Product Reports (2009)

Reen-Yen Kuo Keduo Qian Susan L. Morris‐Natschke Kuo‐Hsiung Lee

Covering: January 2006 to December 2008

10.1039/b810774m

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Citations (163)

Lead Optimization: Synthesis and Biological Evaluation of PBT-1 Derivatives as Novel Antitumor Agents

ACS Medicinal Chemistry Letters (2021)

Lan Xie Masuo Goto Xiaoyan Chen Susan L. Morris‐Natschke Kuo‐Hsiung Lee

Phenanthrene-based tylophorine-1 (PBT-1) was identified previously as a lead compound in an anticancer drug discovery effort based on natural Tylophora alkaloids. An expanded structural optimization using a new more efficient synthetic route provided 14 PBT-derivatives. Eleven compounds displayed obvious antiproliferative activities in cellular assays (GI50 0.55-9.32 μM). The most potent compounds 9c, 9g, and 9h (GI50 < 1 μM) contained a 7-hydroxy group on the phenanthrene B-ring in addition to a pendant piperidine E-ring with different 4-substituents. Compound 9h with NH2 as the piperidine substituent was at least 4-fold more potent against triple-negative breast cancer MDA-MB-231 than estrogen-responsible breast cancer MCF-7 cell growth. In further biological evaluations, the new active compounds induced cell cycle accumulation in the late S and G2/M phase without interfering with microtubule formation or cell morphology. These results on the optimization of the B- and E-rings of PBT-1 should benefit further development of novel antitumor agents.

Piperidine

Lead compound

10.1021/acsmedchemlett.1c00505

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Citations (4)

Design and synthesis of novel spin-labeled camptothecin derivatives as potent cytotoxic agents

Bioorganic & Medicinal Chemistry (2014)

Xiao-Bo Zhao Dan Wu Mei-Juan Wang Masuo Goto Susan L. Morris‐Natschke

Camptothecin

10.1016/j.bmc.2014.09.035

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Citations (16)