2035-75-8Relevant articles and documents
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Hill
, p. 4110,4113 (1930)
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Preparation method 6 -hydroxy caproic acid
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Paragraph 0056-0060; 0093; 0095-0098; 0107; 0109-0112, (2021/11/10)
The invention provides a preparation method of 6 -hydroxycaproic acid. The method comprises the following steps: 1) subjecting 1 and 6 - adipic acid to intramolecular dehydration to obtain adipic anhydride. 2) The adipic acid anhydride is reacted with fatty alcohol to obtain the adipic acid monoester. 3) The adipic acid monoester was subjected to a reduction reaction under hydrogen pressure to give 6 - hydroxycaproic acid. 1-hydroxycaproic acid is prepared by taking 6 - and 6 - adipic acid cheap and easily available as raw materials through intramolecular dehydration, ring opening esterification, hydrogenation reduction and the like.
Evodiamine prodrug containing indole quinone unit as well as preparation method and application thereof
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Paragraph 0026, (2021/10/30)
The invention relates to an evodiamine prodrug containing an indole quinone unit as well as a preparation method and application thereof. The invention synthesizes a series of strong active evodiamine derivatives with indole quinine units, has strong anti-proliferative activity on non-small cell lung cancer (non-small cell lung cancer, NSCLC), and has dosage and time dependence. In-vitro experiments evaluate their biological activity, suggesting that the synthesized compounds have a strong inhibitory activity on lung cancer strains. Through molecular docking analysis, the binding affinity of the ligand to the active site of the target protein is predicted, and the interaction ability of the ligand and the protein is strong.
Synthesis, Antiproliferative Activity, and Effect on Carcinoma A549 Cell Microtubules of New Tubuloclustin Analogs
Zefirov,Evteeva, Yu. A.,Fatkulin,Schulz,Kuznetsov,Zefirova
, p. 423 - 428 (2019/09/16)
Combretastatin analogs of the antitumor agent tubuloclustin {N-[7-(adamant-2-yloxy)-7-oxoheptanoyl]-Ndeacetylcolchicine} were prepared via esterification of combretastatin by monoesters of pimelic or adipic acid with adamantan-2-ol or (adamantan-1-yl)methanol. These conjugates were stable and cytotoxic to human lung carcinoma A549 cells (EC50 ≈ 50 – 70 nM) and caused depolymerization of microtubules and slight clustering of tubulin. Tubuloclustin analogs with shortened linkers were prepared via amidation by N-deacetylcolchicine of monoesters of adipic or succinic acids with adamantan-1-ol or (adamantan-1-yl)methanol. The conjugate N-[6-(adamantyl)-6-oxohexanoyl]-N-deacetylcolchicine was more active (EC50 ≈ 4 nM) than tubuloclustin and promoted strong tubulin clusterization. All compounds induced apoptosis of A549 cells. Tests in vivo of N-[6-(adamantyl)-6-oxoheaxnoyl]-N-deacetylcolchicine on carcinoma A549 experimental models were concluded to be promising.