Vijay Kumar Sethi

Acyl derivatives of boswellic acids as inhibitors of NF-κB and STATs

Boswellic acid acylates including their epimers were synthesized and screened against a panel of human cancer cell lines. They exhibited a range of cytotoxicity against various human cancer cell lines thereby leading to the development of a possible SAR. One of the identified lead compounds was found to be an inhibitor of the NF-κB and STAT proteins, warranting further investigations to be developed into a potential anticancer lead.

Saponins as novel TNF-α inhibitors: isolation of saponins and a nor-pseudoguaianolide from Parthenium hysterophorus

Two novel saponins and a 13-nor-pseudoguaianolide designated as hysterolactone were isolated from Parthenium hysterophorus. The two saponins were found to be potent inhibitors of TNF-alpha. Their mode of inhibition was studied through molecular modeling. The wet lab results were in concordance with the data obtained from docking experiments.

Structure–activity relationship (SAR) of parthenin analogues with pro-apoptotic activity: Development of novel anti-cancer leads

Analogues of parthenin were synthesized by substitutions at different reaction centres to establish a structure-activity relationship (SAR). Some of the molecules have displayed significant cytotoxicity in human cervical carcinoma (HeLa) and human myeloid leukemia (HL-60) cells. A few of the compounds also induced apoptosis in HL-60 cells measured in terms of sub-Go/G1 DNA fraction. Also one of the lead molecules has been shown to be the inhibitor of both telomerase and topoisomerase-II.

(−)-Epiafzelechin 5-O-βD-glucoside from crataeva religiosa

Abstract Epiafzelechin 5-glucoside was characterized from the bark of Crataeva religiosa together with other known compounds.

Rose Oxides: A Facile Chemo and Chemo‐Enzymatic Approach

Abstract Nonracemic rose oxides were synthesized from racemic or nonracemic monoterpene alcohol citronellol by a novel chemo and chemo‐enzymatic route. After the key step of bromomethoxylation of citronellol, the intermediate was dehydrobrominated by a base, followed by an acid catalyzed demethoxylation along with cyclization to furnish rose oxides in high yield. The racemic dehydrobrominated precursor was also kinetically resolved using various lipases to produce nonracemic rose oxides.

Minor sesquiterpenes of flowers of Parthenium hysterophorus

Abstract Three new ambrosanolides, 2β-hydroxycoronopilin, 8β-hydroxycoronopilin and 11-H,13-hydroxyparthenin, besides parthenin and coronopilin have been isolated and characterized from the defatted methanolic extract of flowers of Parthenium hysterophorus .

Psilostachyin, acetylated pseudoguaianolides and their analogues: Preparation and evaluation of their anti-inflammatory potential

Naturally occurring acetylated pseudoguaianolides and psilostachyin including their analogues were synthesized. The structure of semi-synthetic psilostachyin was also confirmed by X-ray crystallography. The anti-inflammatory potential of all the derivatives has been evaluated through in vitro expression of TNF-α, IL-1β and IL-6 in murine neutrophils.