The invention provides a 10-methoxyl camptothecin derivative which is sown in a formula (1), wherein in the formula, R is selected from hydrogen, C1-6 alkyl groups and aryl substituted C1-6 alkyl groups, and R1 is selected from hydrogen and tert-butoxycarbonyl substituted amino group. The invention also provides a preparation method of the derivative and application of the derivative to anti-tumor medicaments.

10-methoxyl camptothecin derivative, preparation method and application

The invention relates to a camptothecin derivative shown as a formula (I) and a medicament thereof, a method for preparing a compound of the invention and application of the compound serving as the medicament for treating tumors. In the formula (I), R1 is hydrogen or ethyl, R2 is hydrogen or nitro group, R3 and R4 are hydrogen, hydroxyl or carbonyl, and R5 is hydroxyl or carbonyl.

Novel camptothecin derivative coupled with cholic acid at position 10

The invention discloses a camptothecin derivative shown as a formula (I). The synthetic method of the derivative comprises the following steps: carrying out a radical substitution reaction on a compound (II) to produce a compound (III) under light conditions; carrying out a coupled reaction on the compound (III) and a boronic acid derivative R-B(OH)2 (IV) to produce a compound (V); carrying out areduction reaction on the compound (V) to produce a compound (VI) under the effect of a catalyst palladium on carbon; and carrying out a Friedlander condensation reaction on the compound (VI) and tricyclic ketolide (VII), thereby obtaining the camptothecin derivative (I). The synthetic method disclosed by the invention is mild in reaction conditions, high in reaction efficiency, low in cost, highin yield and excellent in product quality, has less three-waste pollution in the reaction and is suitable for industrial production. The prepared camptothecin derivative can be applied to preparing antitumor drugs. The structural formula is as shown in the description.

Camptothecin derivative as well as preparation method and application thereof

本発明は医薬化学物質の分野に関し、そして式Ｉのラパマイシン誘導体、及びその調製方法、医薬組成物及び使用に関する。本発明の化合物は、水溶性及び代謝特性に関するラパマイシンの欠点を克服する。幾つかの化合物は、インビトロにおいてラパマイシンよりも優れた抗腫瘍活性を有し、正常細胞に対してラパマイシンよりも低い毒性を有し、そして極めて良好なドラッガビリティを有する。

ラパマイシン誘導体、並びにその調製方法、医薬組成物及び使用

The invention relates to camptothecin derivates in formulas of (I), (II) and (III) as well as acceptable salt in medicine, relating to a method for preparing the compounds as well as applications thereof in tumor therapy particularly by using the compounds as medicines In the formulas of (I), (II) and (III), R1 is hydrogen and ethyl; R2 is hydrogen and nitryl; R3 is oxhydryl, amido, an amine compound, and a compound containing one or a plurality of five-membered or six-membered nitrogen heterocyclic rings as well as derivates thereof; R4 is hydrogen and oxhydryl; and n can be 2, 3 and 4

Camptothecin derivative and its preparation

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Camptothecin derivative and its preparation