Reshma Rani

Synthesis, anti-inflammatory and anticancer activity evaluation of some novel acridine derivatives

Condensation of 9-chloro-2,4-(un)substituted acridines (1a-c) with various amines (2a-e) and 9-isothiocyanato-2,4-(un)substituted acridines (4a,b) with different amines (2a,b,d,e) gave condensed products 3a-o and 5a-g respectively. Compounds 3a-o and 5a-g were screened for anti-inflammatory activity at a dose of 50mg/kg p.o. Compound 3e exhibited 41.17% anti-inflammatory activity which is better than most commonly used standard drug ibuprofen which showed 39% anti-inflammatory (at 50mg/kg p.o.) activity. Anticancer activity evaluation of compounds 3a-o and 5a-g was carried out against a small panel of human cancer cell lines and compounds 3g, 3m and 5g exhibited good anticancer activity against breast (MCF-7), liver (HEP-2), colon (COLO-205, 502713, HCT-15), lung (A-549) and neuroblastoma (IMR-32) cancer cell lines at a concentration of 1 x 10(-5)M.

Solvent free synthesis, anti-inflammatory and anticancer activity evaluation of tricyclic and tetracyclic benzimidazole derivatives.

Heterocyclic benzimidazole derivatives 3a-h, 5a-c and 7a-d have been synthesized by condensation of succinic acid (1) homophthalic acid (4) and 2,3-pyrazinedicarboxlic acid (6) with various substituted diamines under microwave irradiation in good yields. Structures assigned to 3a-h, 5a-c and 7a-d are fully supported by spectral data. All these compounds were screened for anti-inflammatory and anticancer activities. At a dose of 50 mg/kg p.o. compounds 3b (39.4%) and 3c (39.2%) exhibited anti-inflammatory activity, comparable to standard ibuprofen which showed 39% activity at 50 mg/kg p.o. and compound 7c exhibit good anticancer activity against ovary (IGR-OV-1), breast (MCF-7) and CNS(SF-295) human cancer cell lines.

Microwave-assisted synthesis of N-substituted cyclic imides and their evaluation for anticancer and anti-inflammatory activities

A number of N-substituted cyclic imides 3a-e, 5a-e, 7a-d, and 9a-e have been synthesized in very high yields, by condensation of various diacids 2, 4, 6, and 8 with different amines under microwave irradiation. These compounds were screened for anticancer and anti-inflammatory activities, and compounds 3c, 3e, 5c, 9c, and 9d exhibited anticancer activity against colon (COLO 205) cancer better than 5-fluorouracil and mitomycin-C, and compound 9b exhibited anti-inflammatory activity better than standard drug phenyl butazone.

Conventional and microwave assisted synthesis of small molecule based biologically active heterocyclic amidine derivatives

Heterocyclic amidine derivatives have been synthesized by condensation of 2-cyanopyrazine, 4-cyanopyridine and 2-cyanopyridine with furfurylamine, histamine, 1-(3-aminopropyl)imidazole, 4-picolylamine, 2-picolylamine, and tryptamine respectively, in the presence of sodium methoxide as well as via microwave irradiation in good yields. All these compounds were screened for anti-inflammatory and anticancer activities. At a dose of 50mg/kg p.o. compounds 3a (36.6%), 3d (32%), 4d (31.0%) and 4e (33.8%) exhibited good anti-inflammatory activity, comparable to standard drug ibuprofen which showed 39% activity at 50mg/kg p.o.

Microwave-mediated one step synthesis of tri- and tetracyclic heterocyclic molecules

Abstract Tricyclic and tetracyclic compounds related to vasicine and batracyclin, respectively, have been synthesized via condensation of dicarboxylic acids (aliphatic acid, homophthalic acid, and aromatic acid) with diamines (aliphatic, aminobenzyl amine, and aromatic amine) under solvent-free condition.

Synthesis, anti-inflammatory, and cytotoxicity evaluation of 9,10-dihydroanthracene-9,10-α,β-succinimide and bis-succinimide derivatives

Abstract9,10-Dihydroanthracene-9,10-α,β-succinimide derivatives 4a–e and bis-succinimide derivatives 6a–e have been synthesized by grinding 9,10-dihydroanthracene-9,10-α,β-succinic anhydride 2 with various mono 3a–e and diamines 5a–e in quantitative yields. All the target compounds were fully characterized by spectrometric and spectroscopic means. Compounds 4a–e, 6a–e and recently reported compounds 4f–p were screened for anti-inflammatory and for cytotoxicity against five human cancer cell lines: T47D, NCI H-522, HCT-15, PA1, and HepG-2. Compounds 4e, 4i, 4j, and 4p exhibited good anti-inflammatory activity and compounds with interesting cytotoxic profile were 4c, 6e (T47D); 4e, 4o (NCI H-522); 4n (HCT-15); 4e, 4h, 4o (PA1); and 4a, 4e, 4f, 4i, 4o (HepG-2).

Microwave-assisted conversion of aromatic heterocyclic nitriles to various heterocyclic molecules

Abstract Dihydroimidazole (3a-c), dihydrooxazole (3d-f), benzoxazole (5a-c), benzothiazole (5d-f) and oxazolopyridine (7a-c) derivatives have been synthesized by condensation of various heterocyclic aromatic nitriles with diamine, aminoalcohal, aminophenol, aminothiophenol, and 3-aminopyridine-2-ol, respectively, under microwave irradiation and under solvent free conditions. This catalyst free and solvent free approach provided heterocyclic compounds in quantitative yields. Time taken for the condensation to occur is < 20 min.

An expeditious, highly efficient, catalyst and solvent-free synthesis of 9,10-dihydro-anthracene-9,10-α,β-succiniimide derivatives

Abstract A simple, fast, and highly efficient protocol has been developed for the synthesis of 9,10-dihydro-anthracene-9,10-α,β-succinic imide derivatives by simple mixing and grinding of 9,10-dihydro-anthracene-9,10-α,β-succinic anhydride with various aliphatic, aromatic amines, and hydrazines. This catalyst and solvent-free green approach provided the condensation products within few minutes at room temperature in quantitative yield.