Novel compounds having antitumor activity: process for their preparation and pharmaceutical compositions containing them
Inactive Publication Date: 2002-03-14
DR REDDYS LAB LTD
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0025] Still another objective of the present invention is to provide a process for the preparation of Andrographolide derivatives of the formula (I) as defined above, their stereoisomers, their polymorphs, their pharma
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Increased activity or temporarily abnormal activation of these kinases has been shown to result in development of tumors and other proliferative disorders such as restenosis.
Although severa
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EXAMPLE 2
Preparation of 3,14,19-Triacetyl 8,17-Epoxy Andrographolide
[0087] 14
Example
[0088] 8,17-epoxy andrographolide (100 mg) obtained in Example 1 above was taken in 2 ml of acetic anhydride and refluxed for 5 minutes. The reaction was monitored by TLC. After completion of the reaction, the reaction mixture was diluted with solvent ether, washed with water and dried over Na.sub.2SO.sub.4 and concentrated. The residue obtained was chromatographed over a column of silicagel (60-120 mesh) with light petrol:ethyl acetate (65:35) as the solvent system to afford the title compound as a colourless solid (90 mg, 67%). mp: 195.degree. C.
Preparation of 3,14,19-Tripropionyl 8,17-Epoxyandrographolide
[0090] 15
[0091] 8,17-epoxyandrographolide (200 mg) obtained in Example 1 was taken in propionic anhydride (3 ml) and the mixture was refluxed for 5 minutes. The reaction was monitored by TLC. After completion of the reaction, the reaction mixture was poured into water (50 ml) and extracted with dichloromethane. The organic layer was dried over Na.sub.2SO.sub.4 and concentrated. The concentrated residue was recrystallised with ethanol to yield the title compound as colourless solid (115 mg, 39%) m.p. 119.degree. C.
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Abstract
The present invention relates to novel derivatives of Andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of Andrographolide have the general formula (I) The andrographolide derivatives represented by general formula (I) are useful for treating cancer, HSV, HIV, psoriasis, restonosis, atherosclerosis, other cardiovascular disorders, and can be used as antiviral, antimalarial, antibacterial, hepatoprotective, and immunomodulating agents and for treatment of other metabolic disorders.
Description
[0001] The present invention relates to novel anticancer agents, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The present invention more particularly relates to novel derivatives of Andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of Andrographolide have the general formula (I), 2[0002] where R.sup.1, R.sup.2 and R.sup.3 may be same or different and independently represent hydrogen or substituted or unsubstituted groups selected from alkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, alkanoyl, alkenoyl, aroyl, heteroaroyl, sulfonyl group or a group --(CO)--W--R.sup.4 where W represents O, S, or NR.sup.5, wherein R.sup.5 represents hydrogen or (C.sub.1-C.sub.6)alkyl group, R.sup.4 represents substituted or unsubstituted groups selected from alkyl, aryl, aroyl, or aralkyl or R.sup.2 and R....
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