A series of indazol-2-yl(pyridin-4-yl)methanones, 4 were acquired from 2,6-bisbenzylidene cyclohexanones, 3 and anti-tubercular drug (isoniazid), and their anti-tubercular impacts were screened. Among the test compounds used against Mycobacterium tuberculosis H37 Ra cell line in the microplate alamar blue assay, the compounds 4g-j revealed moderate anti-tubercular activity with MIC 12.5 μg/mL, comparable to standard drugs (streptomycin, MIC, 6.25 μg/mL, pyrazinamide, isoniazid and ciprofloxacin with MICs of 3.125 μg/mL). © 2015 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.

Napoleon A-A

Department of Chemistry

School of Advanced Sciences

Vellore Campus

Nawaz Khan F

Jeong E.D

Chung E.H.

Vellore Institute of Technology (VIT) is a private university located in&nbsp;Tamil Nadu, India. Founded in 1984, as Vellore Engineering College, the institution offers 20 undergraduate, 34 postgraduate, four integrated and four research programs. It has campuses in Vellore, Amravati, Bhopal and Chennai.

VIT is one of the top ranked private universities in India according to NIRF, THE and QS Rankings.&nbsp;Govt. of India has recognized&nbsp;VIT, Vellore as an&nbsp;Institution of Eminence. This has allowed VIT to take independent quality initiatives and move up in world ranking.

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VIT University

Chinese Chemical Letters

Methoxy-substituted chalcones, 3 were obtained using simple, efficient method from 2-naphtylethanone, 1 and aromatic aldehydes, 2. The in vitro cytotoxicity activities of the chalcones against a panel of three human cancer cell lines were explored. The tested compounds were found to possess significant cytotoxic activity. The DNA strand break and damage was quantified through alkaline comet assay, flow cytometric analysis, and chromatin condensation studies, which revealed the apoptotic nature of the compounds. Compound 3c, (3-(3,4,5-trimethoxyphenyl)-1-(2-naphthyl) prop-2-en-1-one) showed highest cytotoxicity of 0.019 μm against HeLa, 0.020 μm against HCT15 and 0.022 μm against A549. Compound 3e, (3-(3,5-dimethoxyphenyl)-1-(2-naphthyl) prop-2-en-1-one) showed better IC50 values against all the three cell lines employed for the study.

Chemical Biology & Drug Design

Synthesis of Methoxy-substituted Chalcones andin vitroEvaluation of their Anticancer Potential

The role of methoxy group substitution in various positions in both the rings of chalcones on cytotoxicity profile was studied using various synthesized chalcones. The fluorine containing acetophenones when reacted with various methoxy-substituted benzaldehydes in the presence of 10&nbsp;% sodium hydroxide solution gave the functionalized chalcones. All the synthesized chalcones were confirmed by spectral techniques like FTIR, 1H NMR, 13C NMR, and HRMS studies. All the synthesized compounds were screened for their cytotoxicity against various cell lines. The promising compounds were analyzed for cell cycle analysis.

Medicinal Chemistry Research

Potential cytotoxic and apoptosis inducing agents: synthesis and evaluation of methoxy-substituted chalcones against human lung and cervical cancers

2-Acetyl naphthalene reacts with various methoxy substituted benzaldehyde in the presence of 10&nbsp;% sodium hydroxide solution giving functionalized chalcones. The synthesized chalcones when further reacted with hydrazine hydrate in the presence of acetic acid afforded N-acetyl pyrazolines. All the synthesized products were confirmed by various spectral data such as FTIR, 1H NMR, 13C NMR, and HRMS studies. All the synthesized compounds were screened for cytotoxicity against various cell lines.

Research on Chemical Intermediates

Synthesis and cytotoxicity study of pyrazoline derivatives of methoxy substituted naphthyl chalcones

The ethyl-2-chloroquinoline-3-carboxylates, 4, were achieved fromo-aminobenzophenones in two steps. i.e. initially, the ethyl-2-oxoquinoline- 3-carboxylates, 3, were obtained by base-catalyzed Friedlander condensations of o-aminobenzophenones, 1, and diethylmalonate, 2. The 2-chloroquinoline-3- carboxylates, 4, were then obtained by the reaction with POCl3 in good yields. The chemical structures were confirmed by FTIR, mass and 1H-NMR spectroscopic techniques. All the synthesized compounds were tested for their in vitro antibacterial activity against Bacillus subtilis and Vibrio cholera and found to possess moderate activity. © Springer Science+Business Media B.V. 2012.

Quinoline-3-carboxylates as potential antibacterial agents

An efficient, copper-free Sonogashira coupling reaction of 1-chloroisoquinolines and terminal alkynes, catalyzed by Pd(OAc) 2/Ruphos, in the presence of Et3N and tetrahydrofuran leads to the formation of 1-alkynyl-3-substituted isoquinolines in good yields. © 2011 Elsevier Ltd. All rights reserved.

Tetrahedron Letters

An efficient copper-free Pd(OAc)2/Ruphos-catalyzed Sonogashira coupling of 1-chloroisoquinolines in the formation of 1-alkynyl-3-substituted isoquinolines

Potential anti-tubercular agents: Hexahydro-3-phenyl indazol-2-yl(pyridin-4-yl)methanones from anti-tubercular drug isoniazid and bis(substituted-benzylidene)cycloalkanones

Journal	Data powered by TypesetChinese Chemical Letters
Publisher	Data powered by TypesetElsevier BV
ISSN	1001-8417
Open Access	0