Design, synthesis of 4-[2-(substituted phenyl) hydrazono]-3-(1-hydroxyethyl)-1-phenyl/methyl-3,4-dihydroquinolin-2(1H)-one derivatives and evaluation of their in vitro tyrosine kinase inhibitor activity

267-272The present investigation deals with molecular docking, synthesis, characterization, and evaluation of in vitro tyrosine kinase inhibitor activity of a series of 4-[2-(substituted phenyl) hydrazono]-3-(1-hydroxyethyl)-1-phenyl/methyl-3,4-dihydroquinolin-2(1H)-one derivatives {III-a(1-12)/III-b(1-12)}. Molecular docking studies of the title compounds were carried out using Molegro Virtual Docker (MVD-2013, 6.0) software. The MolDock scores of the derivatives ranged from (−66.508) to (−101.274); whereas the MolDock score of standard 4-anilinoquinazoline ligand was found to be (−105.219). Most of the synthesized qunolin-2-one derivatives showed better affinity towards EGFRK protein as compared to standard drug imatinib (−104.253). All the synthesized compounds were satisfactorily characterized by physical and spectral analysis (UV, IR, 1H NMR and 13C NMR and mass spectral data). Twelve derivatives were tested for their in vitro tyrosine kinase inhibitor activity using MDA-MB cell line. Compound 4-[2-(4-bromophenyl)hydrazono]-3-(1-hydroxyethyl)-1- methyl- 3,4-dihydroquinolin-2(1H)-one (III-b4) was found to be the most cytotoxic compound as compared to other synthesized derivatives, with IC50 value of 0.0515 μM against MDA- MB cell line

Design, synthesis of 4-[2-(substituted phenyl) hydrazono]-3-(1-hydroxyethyl)-1-phenyl/methyl-3,4-dihydroquinolin-2(1H)-one derivatives and evaluation of their in vitro tyrosine kinase inhibitor activity

The present investigation deals with molecular docking, synthesis, characterization, and evaluation of in vitro tyrosine kinase inhibitor activity of a series of 4-[2-(substituted phenyl) hydrazono]-3-(1-hydroxyethyl)-1-phenyl/methyl- 3,4-dihydroquinolin-2(1H)-one derivatives {III-a(1-12)/III-b(1-12)}. Molecular docking studies of the title compounds were carried out using Molegro Virtual Docker (MVD-2013, 6.0) software. The MolDock scores of the derivatives ranged from (−66.508) to (−101.274); whereas the MolDock score of standard 4-anilinoquinazoline ligand was found to be (−105.219). Most of the synthesized qunolin-2-one derivatives showed better affinity towards EGFRK protein as compared to standard drug imatinib (−104.253). All the synthesized compounds were satisfactorily characterized by physical and spectral analysis (UV, IR, 1H NMR and 13C NMR and mass spectral data). Twelve derivatives were tested for their in vitro tyrosine kinase inhibitor activity using MDA-MB cell line. Compound 4-[2-(4-bromophenyl)hydrazono]-3-(1-hydroxyethyl)-1- methyl- 3,4-dihydroquinolin-2(1H)-one (III-b4) was found to be the most cytotoxic compound as compared to other synthesized derivatives, with IC50 value of 0.0515 μM against MDA- MB cell line.

A Study of Marketing of Cashew Nut in South Goa District of Goa, India

A marketing of cashewnut was studied in South Goa district of Goa and have been presented in the form of tabular analysis. A multi-stage stratified sampling procedure was adopted to select marketing functionaries such as primary and secondary market. The study regarding market functionaries was considered to collect data regarding marketing cost and margins and to identify different marketing channels. With the help of this data price spread, producer share in consumer’s rupee and marketing efficiency was calculated. The three different channels were identified i.e., Channel I (Producer-Cooperative societies- Processor-Wholesaler-Retailer), Channel II (Producer-Village Trader-Processor-wholesaler-retailer) and Channel III (Producer-Processor-Wholesaler-Retailer). The Channel III was found to be most efficient marketing channel and the Channel II was found more popular in marketing of cashewnut