- Biomimetic Synthesis of Meroterpenoids by Dearomatization-Driven Polycyclization
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A biomimetic route to farnesyl pyrophosphate and dimethyl orsellinic acid (DMOA)-derived meroterpenoid scaffolds has yet to be reported despite great interest from the chemistry and biomedical research communities. A concise synthetic route with the poten
- Powers, Zachary,Scharf, Adam,Cheng, Andrea,Yang, Feng,Himmelbauer, Martin,Mitsuhashi, Takaaki,Barra, Lena,Taniguchi, Yoshimasa,Kikuchi, Takashi,Fujita, Makoto,Abe, Ikuro,Porco, John A.
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supporting information
p. 16141 - 16146
(2019/11/03)
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- Synthesis and biological evaluation of thielocin B1 analogues as protein-protein interaction inhibitors of PAC3 homodimer
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The synthesis and biological evaluation of thielocin B1 analogues have been demonstrated. Fourteen analogues modified in the central core and terminal carboxylic acid moiety were concisely synthesized by simple esterification or etherification reaction. The evaluation of synthetic analogues as inhibitors of proteasome assembling chaperone (PAC) complexes (the PAC3 homodimer and PAC1/PAC2) revealed that the natural product-like bending structure and terminal carboxylic acid groups were crucial for its biological activity. Moreover, SAR and in silico docking studies indicated that all methyl groups on the diphenyl ether moiety of thielocin B1 contribute to the potent and selective inhibition of the PAC3 homodimer via hydrophobic interactions.
- Ohsawa, Kosuke,Yoshida, Masahito,Izumikawa, Miho,Takagi, Motoki,Shin-ya, Kazuo,Goshima, Naoki,Hirokawa, Takatsugu,Natsume, Tohru,Doi, Takayuki
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supporting information
p. 6023 - 6034
(2018/11/23)
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- First total synthesis of the antitumor antibiotic (±)-resorthiomycin
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The first total synthesis of (±)-resorthiomycin, an antitumor antibiotic has been achieved.
- Ponde, Datta E.,Ramalingam,Patil, Mahesh L.,Borate, Hanumant B.,Deshpande, Vishnu H.
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p. 5399 - 5400
(2007/10/03)
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- 205. Synthese d'une nouvelle depsidone derivee de l'acide furfurique, le dimethoxy-3,8-(dimethoxy-2,4-methoxycarbonyl-5-dimethyl-3,6-benzyl)-9-trimethyl-1,4,6-oxo-11-11H-dibenzodioxepinnecarboxylate-7 de methyle
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The total synthesis of the title compound 1b is described.Starting from simple orcinol and β-orcinol units, the benzophenone 4 has been prepared.Using a biomimetic reaction, the intramolecular oxydative coupling, lead to the grisadienedione 25.By thermal interconversion and permethylation, the depsidone 1b has been obtained.
- Gunzinger, Jan,Tabacchi, Raffaele
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p. 1940 - 1947
(2007/10/02)
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- 206. Synthese des pseudocyphellarines A et B, deux depsides du lichen Pseudocyphellaria endochrysea
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The total synthesis of the depsides pseudocyphellarin A ( = 3-hydroxy-4-methoxycarbonyl-2,5,6-trimethylphenyl 3-formyl-2,4-dihydroxy-5,6-dimethylbenzoate; 11) and pseudocyphellarin B (3-hydroxy-4-methoxycarbonyl-2,5,6-trimethylphenyl 2,4-dihydroxy-3-hydro
- Pulgarin, Cesar,Gunzinger, Jan,Tabacchi, Raffaele
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p. 1948 - 1951
(2007/10/02)
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