- Facile synthesis of acridines via Pd(0)-diphosphine complex-catalyzed tandem coupling/cyclization protocol
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A facile and efficient approach for the synthesis of a variety of acridines via the tandem coupling/cyclization of substituted 2-bromobenzaldehydes and anilines is described. The reaction can be accomplished with ease in the presence of a catalytic amount of Pd2(dba)3 and diphosphine ligand dppf, providing a broad range of substituted acridines in good to excellent yields (up to 99%). The Lewis acid, AlCl3, is required to promote the cyclization for less electron-rich anilines.
- Wang, Ting-Jun,Chen, Wen-Wen,Li, Yi,Xu, Ming-Hua
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p. 6580 - 6586
(2015/06/16)
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- Antiangiogenic combination therapy for the treatment of cancer
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The present invention provides combinations of a DNA topoisomerase I inhibiting agent and a selective COX-2 inhibiting agent for preventing, treating, and/or reducing the risk of developing a neoplasia disorder in a mammal.
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- Process for the preparation of N-[2-(dimethylamino)ethyl]acridine-4-carboxamide
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PCT No. PCT/GB97/02884 Sec. 371 Date Jun. 18, 1999 Sec. 102(e) Date Jun. 18, 1999 PCT Filed Oct. 17, 1997 PCT Pub. No. WO98/17649 PCT Pub. Date Apr. 30, 1998A process for producing an acridine carboxamide of formula (I): wherein each of R1, R2, R5 and R6,
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- A new synthesis of substituted acridine-4-carboxylic acids and the anticancer drug N-[2-dimethylamino)ethyl]acridine-4-carboxamide (DACA)
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A new synthesis of substituted acridine-4-carboxylic acids 2 from methyl 2-[N-(2-carboxyphenyl)amino]benzoates (4) is reported, via NaBH4 reduction of the corresponding imidazolides (5), oxidation of the resulting alcohols 6 to aldehyde 7, and cyclisation of these with trifluoroacetic acid to the methyl acridine-4-carboxylates (8), followed by base hydrolysis. Direct amidation of 8a provides a new route to the clinical anticancer drug DACA (3) which avoids use of the irritant acid 2a.
- Gamage, Swarna A.,Spicer, Julie A.,Rewcastle, Gordon W.,Denny, William A.
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p. 699 - 702
(2007/10/03)
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- Structure-activity relationships for acridine-substituted analogues of the mixed topoisomerase I/II inhibitor N-[2-(dimethylamino)ethyl] acridine- 4-carboxamide
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The mixed topoisomerase I/II inhibitor N-[2- (dimethylamino)ethyl]acridine-4-carboxamide (DACA) is currently in clinical trial as an anticancer drug. A series of acridine-substituted analogues were prepared, using a new synthetic route to substituted acri
- Spicer, Julie A.,Gamage, Swarna A.,Atwell, Graham J.,Finlay, Graeme J.,Baguley, Bruce C.,Denny, William A.
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p. 1919 - 1929
(2007/10/03)
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- Potential Antitumor Agents. 50. In Vivo Solid-Tumor Activity of Derivatives of N-acridine-4-carboxamide
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The synthesis, physicochemical properties, and antitumor activity of a series of N-acridine-4-carboxamides are reported.The compounds bind to DNA by intercalation, but exist under physiological conditions as monocations due to the w
- Atwell, Graham J.,Rewcastle, Gordon W.,Baguley, Bruce C.,Denny, William A.
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p. 664 - 669
(2007/10/02)
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