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Investigation of chemical reactivity of 2-alkoxy-1,4-naphthoquinones and their anticancer activity
Manickam, Manoj,Boggu, Pulla Reddy,Cho, Jungsuk,Nam, Yeo Jin,Lee, Seung Jin,Jung, Sang-Hun Elsevier 2018 Bioorganic & medicinal chemistry letters Vol.28 No.11
<P><B>Abstract</B></P> <P>To establish the structure-activity relationship of 5-hydroxy-1,4-naphthoquinones toward anticancer activity, a series of its derivatives were prepared and tested for the activity (IC<SUB>50</SUB> in µM) against three cell lines; colo205 (colon adenocarcinoma), T47D (breast ductal carcinoma) and K562 (chronic myelogenous leukemia). Among them <B>2</B> (IC<SUB>50</SUB>: 2.3; 2.0; 1.4 µM), <B>6</B> (IC<SUB>50</SUB>: 1.9; 2.2; 1.3 µM), <B>9</B> (IC<SUB>50</SUB>: 0.7; 1.7; 0.9 µM) and <B>10</B> (IC<SUB>50</SUB>:1.7; 1.0; 1.2 µM) showed moderate to excellent activity. Our perception toward the DNA substitution of alkoxy groups at the C2 position of these naphthoquinones for the anticancer activity led us to investigate their reactivity of substitution toward dimethylamine as a nucleophile. The ease of the substitution of alkoxy groups at the C2 position with dimethylamine is strongly accelerated by hydroxyl group at C5 position and is well correlated with the found anticancer activity results.</P> <P><B>Highlights</B></P> <P> <UL> <LI> SAR of 1,4-naphthoquinones toward anticancer activity was established. </LI> <LI> C2-Alkoxy and C5-hydroxyl is crucial for activity. </LI> <LI> The substitution of alkoxyl at the C2 with amine is accelerated by hydroxyl at C5. </LI> <LI> The chemical reactivity of these analogs is correlated with their anticancer activity. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Manickam Kalappan Vanitha,Kalpana Deepa Priya,Kuppusamy Baskaran,Kuppusamy Periyasamy,Dhravidamani Saravanan,Ramachandran Venkateswari,Balasundaram Revathi Mani,Aruldass Ilakkia,Sundaramoorthy Selvara 대한약침학회 2015 Journal of pharmacopuncture Vol.18 No.3
Objectives: The present study was undertaken to determine the modulatory effect of taurine on the liver mitochondrial enzyme system with reference to mitochondrial lipid peroxidation (LPO), antioxidants, major tricarboxylic acid cycle enzymes, and electron transport chain enzymes during 7,12-dimethyl benz[a]anthracene (DMBA) induced breast cancer in Sprague-Dawley rats. Methods: Animals in which breast cancer had been induced by using DMBA (25 mg/kg body weight) showed an increase in mitochondrial LPO together with decreases in enzymic antioxidants (superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), glutathione reductase (GR) and glutathione-S-transferase (GST)), non-enzymic antioxidants (reduced glutathione (GSH), vitamin C, and vitamin E), in citric acid cycle enzymes (isocitrate dehydrogenase (ICDH), alpha ketoglutarate dehydrogenase (alpha KDH), succinate dehydrogenase (SDH) and malate dehydrogenase (MDH)), and in electron transport chain (ETC) complexes. Results: Taurine (100 mg/kg body weight) treatment decreased liver mitochondrial LPO and augmented the activities/levels of enzymic, and non-enzymic antioxidants, tricarboxylic acid cycle enzymes and ETC complexes. Conclusion: The results of our present study demonstrated the chemotherapeutic efficacy of taurine treatment for DMBA-induced breast carcinomas.
A new ultrasonic cavitation approach for the synthesis of zinc ferrite nanocrystals
Manickam Sivakumar,Atsuya Towata,Kyuichi Yasui,Toru Tuziuti and Yasuo Iida,Yasuo Iida 한국물리학회 2006 Current Applied Physics Vol.6 No.3
An ultrasound mediated simple emulsion process has been demonstrated for the synthesis of zinc ferrite nanocrystals using the pre-cursors of zinc and iron acetates and rapeseed oil. Following this technique avoids many of the outstanding problems that normally existin conventional emulsion synthesis. Due to the simplicity of this process, it could also become a valuable starting point for the generationof other mixed and complex ferrites.
Manickam Sundaram,Balasubramanian Visvalingam 대한용접·접합학회 2016 대한용접·접합학회지 Vol.34 No.3
This paper discusses the optimization of friction stir spot welding (FSSW) process parameters for joining Aluminum alloy (AA6061-T6) with Magnesium alloy (AZ31B) sheets. Prior to optimization an empirical relationship was developed to predict the Tensile Shear Fracture Load (TSFL) incorporating the four most important FSSW parameters, i.e., tool rotational speed, plunge rate, dwell time and tool diameter ratio, using response surface methodology (RSM). The experiments were conducted based on four factor, five levels central composite rotatable design (CCD) matrix. The maximum TSFL obtained was 3.61kN, with the tool rotation of 1000 rpm, plunge rate of 16 mm/min, dwell time of 5 sec and tool diameter ratio of 2.5.
Manickam Matheswaran,Subramanian Balaji,Sang Joon Chung,문일식 대한화학회 2007 Bulletin of the Korean Chemical Society Vol.28 No.8
The electrochemical oxidation of cerium(III) was carried out using divided and undivided electrochemical cells in nitric acid medium. It was found that divided cell with Nafion 324 as the separator gave good conversion yield with high current efficiency compared to the undivided cell. The efficiency of the divided electrochemical cell was further optimized in terms of cell voltage, temperature, flow rate of solution recirculation, concentrations of Ce(III) and nitric acid. The better conditions for 1 M Ce(III) in 3 M nitric acid were found to be 2.5 V, 363 K and 100 mL/min recirculation flow rate based on the current efficiency under the experimental conditions investigated. The Ce(IV) oxidant produced was used as a mediator for the mineralization of phenol. The mineralization efficiency of the cerium mediated electrochemical oxidation was found rapid and higher compared to the direct electrochemical oxidation based on CO2 evolution under the same conditions.
Design and synthesis of sulfonamidophenylethylureas as novel cardiac myosin activator
Manickam, Manoj,Jalani, Hitesh B.,Pillaiyar, Thanigaimalai,Boggu, Pulla Reddy,Sharma, Niti,Venkateswararao, Eeda,Lee, You-Jung,Jeon, Eun-Seok,Son, Min-Jeong,Woo, Sun-Hee,Jung, Sang-Hun Elsevier 2018 European Journal of Medicinal Chemistry Vol.143 No.-
<P><B>Abstract</B></P> <P>To optimize the lead urea scaffold <B>1</B> and <B>2</B> as selective cardiac myosin ATPase activator, a series of urea derivatives have been synthesized to explore its structure activity relationship. Among them <I>N,N</I>-dimethyl-4-(2-(3-(3-phenylpropyl)ureido)ethyl)benzenesulfonamide (<B>13</B>, CMA = 91.6%, FS = 17.62%; EF = 11.55%), <I>N,N</I>-dimethyl-4-(2-(1-methyl-3-(3-phenylpropyl)ureido)ethyl)benzene sulfonamide (<B>40</B>, CMA = 52.3%, FS = 38.96%; EF = 24.19%) and <I>N,N</I>-dimethyl-4-(2-(3-methyl-3-(3-phenylpropyl)ureido)ethyl)benzenesulfonamide (<B>41</B>, CMA = 47.6%, FS = 23.19%; EF = 15.47%) proved to be efficient to activate the cardiac myosin <I>in vitro</I> and <I>in vivo</I>. Further the % change in ventricular cell contractility at 5 μM of <B>13</B> (47.9 ± 3.2), <B>40</B> (45.5 ± 2.4) and <B>41</B> (63.5 ± 2.2) showed positive inotropic effect in isolated rat ventricular myocytes. The potent compounds <B>13, 40, 41</B> were highly selective for cardiac myosin over skeletal and smooth muscle myosin, thus proving them these new urea derivatives is a novel scaffold for discovery of cardiac myosin activators for the treatment of systolic heart failure.</P> <P><B>Highlights</B></P> <P> <UL> <LI> SAR study of sulfonamidophenylethylureas discovered highly potent inotrope. </LI> <LI> These urea analogs are selective cardiac myosin ATPase activators. </LI> <LI> Compound <B>13</B>, <B>40</B>, <B>41</B> shows 17.6, 38.9, 23.2% fractional shortening in the echocardiographic study with rat. </LI> <LI> The cell contractility of <B>13</B>, <B>40</B>, <B>41</B> shows 47.9, 45.5, 63.5% at 5 µM in rat ventricle cells. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Manickam Matheswaran,문일식 한국공업화학회 2009 Journal of Industrial and Engineering Chemistry Vol.15 No.3
The ozonation of phenol wastewater treatment system has been investigated with effective mass transfer between gas and liquid phase in a bubble column reactor. The designed bubble column reactor was investigated for increasing the rate of mass transfer of ozone, the rate of oxidation of phenol in the solution, the solubility and decomposition rate of ozone in the distilled water were also studied at different flow rates. The decomposition rate constants were calculated based on pseudo first order kinetics. The oxidation of phenol was investigated in order to provide the overall reaction rate constant for the reaction between ozone and phenol at 25℃. The influence of the operating parameters like initial phenol concentration, ozone flow rate and pH for the destruction of phenol by ozonation were studied. The pseudo first order rate constant was depending on the initial concentration of phenol solution. A comparison of TOC removal percentage between bubble column reactor and bubble diffuser using ozonation were reported.
Exploration of diphenylalkyloxadiazoles as novel cardiac myosin activator
Manickam, Manoj,Boggu, Pulla Reddy,Pillaiyar, Thanigaimalai,Sharma, Niti,Jalani, Hitesh B.,Venkateswararao, Eeda,Jung, Sang-Hun Elsevier 2018 Bioorganic & medicinal chemistry letters Vol.28 No.14
<P><B>Abstract</B></P> <P>To explore novel cardiac myosin activator, a series of diphenylalkyl substituted 1,3,4-oxadiazoles and 1,2,4-oxadiazoles have been prepared and tested for cardiac myosin ATPase activation <I>in vitro</I>. In all cases, three carbon spacer between the oxadiazole core and one of the phenyl ring was considered crucial. In case of 1,3,4-oxadiazole, zero to two carbon spacer between oxadiazole core and other phenyl ring are favorable. Phenyl ring can be replaced by cyclohexyl moiety. In case of 1,2,4-oxadiazole, zero or one carbon spacer between the oxadiazole and other phenyl ring are favorable. Introduction of hydrogen bonding donor (NH) group at the 2<SUP>nd</SUP> position of the 1,3,4-oxadiazole enhances the activity. Substitutions on either of the phenyl rings or change of phenyl ring to other heterocycle are not tolerated for both the oxadiazoles. The prepared oxadiazoles showed selective activation for cardiac muscle over smooth and skeleton muscles.</P> <P><B>Highlights</B></P> <P> <UL> <LI> The diphenylalkyl oxadiazoles were identified as novel cardiac myosin ATPase activator. </LI> <LI> Three carbon spacer between oxadiazole core and one of the phenyl ring is crucial. </LI> <LI> Introduction of NH group at the 2nd position of the 1,3,4-oxadiazole is favored. </LI> <LI> These oxadiazoles are selective activators for cardiac myosin. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>