Synthesis and biological evaluation of the natural product komaroviquinone and related compounds aiming at a potential therapeutic lead compound for high-risk multiple myeloma

[Display omitted] Alternatives of treatments for multiple myeloma (MM) have become increasingly available with the advent of new drugs such as proteasome inhibitors, thalidomide derivatives, histone deacetylase inhibitors, and antibody drugs. However, high-risk MM cases that are refractory to novel...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2017-10, Vol.27 (19), p.4558-4563
Main Authors: Suto, Yutaka, Sato, Mariko, Fujimori, Kota, Kitabatake, Shotaro, Okayama, Mikio, Ichikawa, Daiju, Matsushita, Maiko, Yamagiwa, Noriyuki, Iwasaki, Genji, Kiuchi, Fumiyuki, Hattori, Yutaka
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents, Phytogenic - chemical synthesis
Antineoplastic Agents, Phytogenic - chemistry
Antineoplastic Agents, Phytogenic - pharmacology
Antitumor reagent
Biological Products - chemical synthesis
Biological Products - chemistry
Biological Products - pharmacology
Bone Marrow Cells - drug effects
Cell Line, Tumor
Cell Proliferation - drug effects
Cell Survival - drug effects
Diterpenes - chemical synthesis
Diterpenes - chemistry
Diterpenes - pharmacology
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Lamiaceae - chemistry
Mice
Molecular Structure
Multiple myeloma
Multiple Myeloma - drug therapy
Multiple Myeloma - pathology
Natural product
Quinones - chemical synthesis
Quinones - chemistry
Quinones - pharmacology
Structure-Activity Relationship
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Summary:[Display omitted] Alternatives of treatments for multiple myeloma (MM) have become increasingly available with the advent of new drugs such as proteasome inhibitors, thalidomide derivatives, histone deacetylase inhibitors, and antibody drugs. However, high-risk MM cases that are refractory to novel drugs remain, and further optimization of chemotherapeutics is urgently needed. We had achieved asymmetric total synthesis of komaroviquinone, which is a natural product from the plant Dracocephalum komarovi. Similar to several leading antitumor agents that have been developed from natural compounds, we describe the antitumor activity and cytotoxicity of komaroviquinone and related compounds in bone marrow cells. Our data suggested that komaroviquinone-related agents have potential as starting compounds for anticancer drug development.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2017.08.054