ChemInform Abstract: Synthesis, Analgesic and Antiinflammatory Activities of Bis(indolyl)methanes.

Abstract

Indole derivatives R 0140Synthesis, Analgesic and Antiinflammatory Activities of Bis(indolyl)methanes.-All synthesized compounds (III) (no yields given) exhibit analgesic and antiinflammatory activity without ulcerogenic activity. Compounds (IIIb) and (IIIc) are found to be more active than ibuprofen. -(SUJATHA, K.; PERUMAL*, P. T.; MURALIDHARAN, D.; RAJENDRAN, M.; Indian J. Chem., Sect. B: Org. Chem.

Gold-Catalyzed Benzylic Azidation of Phthalans and Isochromans and Subsequent FeCl₃-Catalyzed Nucleophilic Substitutions

“…Consequently, the iron-catalyzed Friedel-Crafts arylation and allylation gave the 1-aryl/allyl phthalan and isochroman derivatives (3, 4) (Chart 2), while the use of highly nucleophilic indole derivatives effectively facilitated the double substitutions via elimination of the azido group and the subsequent ring opening of the cyclic ether to give the bisindolylarylmethane derivatives (5). [34][35][36][37][38][39] The obtained product (3) could also be converted into the corresponding bisarylindolylmethane derivatives (6) by the FeCl 3 -catalyzed ring-opening indolylation. [40][41][42] We now report the direct gold-catalyzed azidation of phthalan and isochroman derivatives (Chart 1) and the subsequent unique FeCl 3 -catalyzed nucleophilic substitutions (Chart 2) to produce the various pharmaceutically useful compounds.…”

Synthesis of bis(indolyl)methanes using molten N-butylpyridinium bromide

“…BIMs are effective towards estrogen-regulated events in human breast cancer cells, and are found as a promoter-specific activator of estrogen receptor even in the absence of 17β-estradiol [8]. In addition to that, these compounds exhibits a broad spectrum of anticancer activities by inducing cancer cell differentiation, growth inhibition, and apoptosis [9], as well as analgesic and antiinflammatory activities [10] are also reported.…”

A green protocol for the synthesis of bis(indolyl)methanes catalyzed by succinic acid under microwave irradiation

“…3 Bis(indolyl)methanes are known to promote beneficial estrogen metabolism and induce apoptosis in human cancer cell. 4a,b Other beneficial activities such as dietary supplements, 5 topoisomerase IIa inhibitors, 6 antibacterials, 7 antibiotics, 8 antifungal, 9 anti-inflammatory, 10 antimicrobialactivities, 11 agrochemicals, 12 and in material sciences as calorimetric sensors, particularly for various metals and fluorides. 13a, b Due to their broad range of biological applications, there is a great deal of interest in the synthesis of bis(indolyl)methane derivatives.…”