Jammikuntla N. Rosaiah

Rare dipeptide and urea derivatives from roots of Moringa oleifera as potential anti-inflammatory and antinociceptive agents.

In the course of our studies on the isolation of bioactive compounds from the roots of Moringa oleifera, a traditional herb in southeast Asia, rare aurantiamide acetate 4 and 1,3-dibenzyl urea 5 have been isolated and characterized. And also, this is the first report of isolation from this genus. Isolated compound inhibited the production of TNF-alpha and IL-2; further compound 5 showed significant analgesic activities in a dose dependant manner. These findings may help in understanding the mechanism of action of this traditional plant leading to control of activated mast cells on inflammatory conditions like arthritis, for which the crude extract has been used.

Neo-tanshinlactone inspired synthesis, in vitro evaluation of novel substituted benzocoumarin derivatives as potent anti-breast cancer agents.

A small library of novel benzocoumarin derivatives based on naturally occurring neo-tanshinlactone scaffold was constructed and their antiproliferative activities against breast cancer cells MCF-7 and MDA-MB-231 were evaluated. A number of derivatives showed good anti-breast cancer activity, in some cases higher to that of the reference compound tamoxifen. In particular, benzocoumarins Bc-5, Bc-8 and Bc-9 strongly inhibited the proliferation of MCF-7 cancer cell line with the IC(50) values of 3.8, 7.9 and 6.5 μM, respectively. The compounds were capable of inducing nuclear fragmentation, cell cycle arrest and caspase dependent apoptosis in MCF-7 cell lines. In addition, these derivatives were devoid of cytotoxic effect against normal osteoblast cells. These synthetic benzocoumarins hold promises for developing safer alternative to the existing anti-breast cancer agents.

Synthesis of novel benzocoumarin derivatives as lipid lowering agents

A series of novel benzocoumarin derivatives were synthesized and evaluated for their in vivo anti-dyslipidemic and in vitro antioxidant activities. Preliminary screening indicates compound 4 as potential lead with significant lipid lowering and antioxidant activities. The study revealed that such attempts on benzocoumarin-based pharmacophores which is a biologically important scaffold might result in identification of new lead for anti-dyslipidemia.

Iodine-Catalyzed Mild and Efficient Method for the Synthesis of Chalcones

Abstract Molecular iodine is found to catalyze the condensation of acetophenones with various aromatic aldehydes to prepare chalcones.

Unusual Reaction of 6-Formyl-2-oxo-2H-benzo[h]chromene-3-carboxylic Acid Ethyl Ester with Aliphatic Amines

The unusual reaction of coumarone systems when exposed to aliphatic amines is described. The stability and formation of these compounds is discussed with respect to its substituents at para position, and it was found that the para substituents have no role to play.

New Protocol for Masking and Unmasking Vicinal Hydroxyl and Formyl Groups in 6-Hydroxyarene-1,3-dicarboxaldehydes

Abstract A simple and efficient protocol is revealed for the masking and unmasking of an α-hydroxyl benzaldedyde group in aromatic dialdehydes by forming keto-enamine Schiff bases and subsequent unmasking using NaN3/DMF.