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Design, synthesis and biological studies of tetrazole fused imidazopyridines
Reddy Banoth,Taneja Amit Kumar,Tej Mandava Bhuvan,Navya Sri Komati,Tej Mandava Bhagya,Vijayavardhini Suryadevara,Srilaxmi Dandamudi,Tiruveedhula Somasekhar,Penumutchu Srinivasa Rao,Rao Mandava V. Basa 한국탄소학회 2024 Carbon Letters Vol.34 No.1
New tetrazole fused imidazopyridine derivatives (12a–j) were developed to exploit their cytotoxic activity towards cancer cell lines-MCF7, A549, and MDA-MB-231, utilizing MTT reduction assay with doxorubicin as standard drug. The compounds 12 h and 12j demonstrated strong anticancer activity bearing IC50 values 1.44 µM and 1.33 µM against A549 cell line.
Mandava Mohana Rao,M Joy Thomas,B.P. Singh 대한전기학회 2007 Journal of Electrical Engineering & Technology Vol.2 No.3
The transient fields generated during switching operations in a Gas Insulated Substation(GIS) are associated with high frequency components in the order of few tens of MHz. These transient fields leak into the external ennearby electronics. Measurements of the transient fields are thus required to characterise the interference caused by switching phenomena in such substations. In view of the above, E-field emission measurement during a switching operation has been carried out for a 245 kV GIS model, using a resonant dipole antenna and D-dot sensor. The characteristics of the E-fields i.e., frequency spectra and their levels have been analysed and are reported in the paper. Suitability of the measurements has been confirmed by comparing frequency spectra of the measured and computed transient fields.
Synthesis and Structure Revision of Dimeric Tadalafil Analogue Adulterants in Dietary Supplements
Mandava, S.,Ganganna, B.,Hwang, Ju.,Jang, Y.,Hwang, Ji.,Samala, M.,Kim, K.-B.,Park, H.,Lee, J. H.,Baek, S. Y. Pharmaceutical Society of Japan 2017 Chemical & pharmaceutical bulletin Vol. No.
<P>A number of phosphodiesterase 5 (PDE5) inhibitors approved by authorities have been used successfully in the treatment of erectile dysfunction. These medicines must be prescribed carefully due to their adverse effects, but they and their analogues are being illegally added to dietary supplements. These illegal dietary supplements pose a significant risk to public health. Several dimeric tadalafil analogues have been synthesized for use as reference standards in the inspection of functional foods that are mainly advertised as sexual enhancement products. During the course of this synthesis, 1-Ibis(dimethylamino)methylenek1H-1,2,3triazolo14,5-blpyridinium 3-oxid hexafluorophosphate (HATU) was proven to be the reagent of choice for amide coupling to produce these dimeric tadalafil analogues. Moreover, the trans-isomer structures tentatively assigned for the isolated dimeric tadalafil analogues (bisprehomotadalafil and bisprecyclopentyltadalafil) found in dietary supplements are now revised to cis-isomer structures.</P>
Anitha Mandava,Veeraiah Koppula,Meghana Kandati,K. V. V. N. Raju 대한방사선종양학회 2023 Radiation Oncology Journal Vol.41 No.4
Radiation-induced fistulas (RIF) are uncommon therapeutic complications of radiotherapy in patients treated for carcinoma of the uterine cervix. Synchronous occurrence of enterocervical and enterovesical fistulas secondary to radiation is extremely rare and previously unreported in the literature. We report a case of synchronous enterovesical and enterocervical fistulas in a patient with carcinoma of the cervix treated using chemotherapy and radiation along with a brief overview of etiopathogenesis of RIF.
Saravanakumar, Kandasamy,Mandava, Suresh,Chellia, Ramachandran,Jeevithan, Elango,Babu Yelamanchi, Ravi Shankar,Mandava, Deepthi,Wen-Hui, Wu,Lee, Jongkook,Oh, Deog-Hwan,Kathiresan, Kandasamy,Wang, Myeo Elsevier 2019 Microbial pathogenesis Vol.126 No.-
<P><B>Abstract</B></P> <P>The present study aimed to purify and identify the metabolites from <I>T. atroviride</I> using high-performance liquid chromatography (HPLC) and <SUP>1</SUP>H and <SUP>13</SUP>C nuclear magnetic resonance spectrometer (NMR) followed by analyzing their toxicological, antibacterial and anticancer properties. This work identified two metabolites - TM1 and TM2. TM1 was in two forms: (i) 1, 3-dione-5, 5-dimethylcyclohexane; and, (ii) 2-enone-3hydroxy −5,5-dimethylcylohex, while TM2 was 4H-1,3-dioxin-4-one-2,3,6-trimethyl. These metabolites did not exhibit any irritant or allergic reaction as revealed by HET- CAM test. TM2 significantly inhibited the growth of <I>H. pylori</I> and Shigella toxin producing <I>Escherichia coli</I> (STEC) as evident by <I>in vitro</I> and microscopic observations of bacterial cell death. TM2 also induced the cell death and cytotoxicity, as revealed by cell viability test and western blot analysis. According to microscopic, flow cytometer and western blot analysis, TM2 treated cells displayed higher ROS, cell death, and apoptosis-related protein expression than TM1 and control. This study concluded that TM2 derived from <I>T. atroviride</I> was a potential therapeutic agent for anti-prostate cancer and antibiotic agent against MDR- <I>H. pylori</I> and STEC and it is also recommended to carry out further <I>in vivo</I> animal model experiments with improved stability of the metabolites for future pharmaceutical trails.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Fungal metabolites against <I>H. pylori</I> and Shigella toxin producing <I>Escherichia coli</I> (STEC). </LI> <LI> <I>Trichoderma</I> derived metabolites exhibited the antibacterial, and anticancer activity. </LI> <LI> TM2 reported as the potential therapeutic agent against - <I>H. pylori</I>, STEC, and anti-prostate cancer. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Potential Moracin M Prodrugs Strongly Attenuate Airway Inflammation In Vivo
( Jongkook Lee ),( Suresh Mandava ),( Sung-hoon Ahn ),( Myung-ae Bae ),( Kyung Soo So ),( Ki Sun Kwon ),( Hyun Pyo Kim ) 한국응용약물학회 2020 Biomolecules & Therapeutics(구 응용약물학회지) Vol.28 No.4
This study aims to develop new potential therapeutic moracin M prodrugs acting on lung inflammatory disorders. Potential moracin M prodrugs (KW01-KW07) were chemically synthesized to obtain potent orally active derivatives, and their pharmacological activities against lung inflammation were, for the first time, examined in vivo using lipopolysaccharide (LPS)-induced acute lung injury model. In addition, the metabolism of KW02 was also investigated using microsomal stability test and pharmacokinetic study in rats. When orally administered, some of these compounds (30 mg/kg) showed higher inhibitory action against LPSinduced lung inflammation in mice compared to moracin M. Of them, 2-(3,5-bis((dimethylcarbamoyl)oxy)phenyl)benzofuran-6-yl acetate (KW02) showed potent and dose-dependent inhibitory effect on the same animal model of lung inflammation at 1, 3, and 10 mg/kg. This compound at 10 mg/kg also significantly reduced IL-1β concentration in the bronchoalveolar lavage fluid of the inflamed-lungs. KW02 was rapidly metabolized to 5-(6-hydroxybenzofuran-2-yl)-1,3-phenylene bis(dimethylcarbamate) (KW06) and moracin M when it was incubated with rat serum and liver microsome as expected. When KW02 was administered to rats via intravenous or oral route, KW06 was detected in the serum as a metabolite. Thus, it is concluded that KW02 has potent inhibitory action against LPS-induced lung inflammation. It could behave as a potential prodrug of moracin M to effectively treat lung inflammatory disorders.
Bhandari, Prerana,Ahmad, Firoz,Mandava, Swarna,Das, Bibhu Ranjan Asian Pacific Journal of Cancer Prevention 2016 Asian Pacific journal of cancer prevention Vol.17 No.8
Background: Childhood acute lymphoblastic leukemia (ALL) is a heterogeneous genetic disease and its etiology remains poorly understood. Recent genome wide association and replication studies have highlighted specific polymorphisms contributing to childhood ALL predispositions mostly in European populations. It is unclear if these observations generalize to other populations with a lower incidence of ALL. The current case-control study evaluated variants in ARID5B (rs7089424, rs10821936), IKZF1 (rs4132601) and CEBPE (rs2239633) genes, which appear most significantly associated with risk of developing childhood B-lineage ALL. Materials and Methods: Using TaqMan assays, genotyping was conducted for 162 de novo B-lineage ALL cases and 150 unrelated healthy controls in India. Appropriate statistical methods were applied. Results: Genotypic and allelic frequencies differed significantly between cases and controls at IKZF1-rs4132601 (p=0.039, p=0.015) and ARID5B-rs10821936 (p=0.028, p=0.026). Both rs10821936 (p=0.019; OR 0.67; 95% CI=0.47-0.94) and rs4132601 (p=0.018; OR 0.67; 95%CI 0.48-0.94) were associated with reduced disease risk. Moreover, gender-analysis revealed male-specific risk associations for rs10821936 (p=0.041 CT+CC) and rs4132601 (p=0.005 G allele). Further, ARID5B-rs7089424 and CEBPE-rs2239633 showed a trend towards decreased disease risk but without significance (p=0.073; p=0.73). Conclusions: Our findings provide the first evidence that SNPs ARID5B-rs10821936 and IKZF1-rs4132601 are associated with decreased B-lineage ALL susceptibility in Indian children. Understanding the effects of these variants in different ethnic groups is crucial as they may confer different risk of ALL within different populations.
Samala, Mallesham,Lu, Thien Nhan,Mandava, Suresh,Hwang, Jungjoong,Bogonda, Ganganna,Kim, Donghoon,Park, Haeil,Kim, Deukjoon,Lee, Jongkook American Chemical Society 2018 ORGANIC LETTERS Vol.20 No.20
<P>A stereoselective protection-free asymmetric total synthesis of (+)-chamuvarinin (<B>1</B>), a potent anticancer and antitrypanosomal agent, has been accomplished. The adjacently linked [bis(tetrahydrofuran)]tetrahydropyran (THF-THF-THP) core of this natural product with seven stereogenic centers was constructed in a completely substrate-controlled fashion. The inter-ring stereochemistry (<I>threo,threo,threo</I>) of the oxatricyclic core was established in a stereoselective fashion by a chelation-controlled Keck allylation, whereas the intraring <I>cis</I> or <I>trans</I> relative stereochemistry was controlled by a stereoselective internal alkylation.</P> [FIG OMISSION]</BR>
Ahmad, Firoz,Mohota, Rupali,Sanap, Savita,Mandava, Swarna,Das, Bibhu Ranjan Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.3
Mutations in the DNMT3A and IDH genes represent the most common genetic alteration after FLT3/NPM1 in acute myeloid leukemia (AML). We here analyzed the frequency and distribution pattern of DNMT3A and IDH mutations and their associations with other molecular markers in normal karyotype AML patients. Fortyfive patients were screened for mutations in DNMT3A (R882), IDH1 (R132) and IDH2 (R140 and R172) genes by direct sequencing. Of the 45 patients screened, DNMT3A and IDH mutations were observed in 6 (13.3%) and 7 (15.4%), respectively. Patients with isolated DNMT3A mutations were seen in 4 cases (9%), isolated IDH mutations in 5 (11.1%), while interestingly, two cases showed both DNMT3A and IDH mutations (4.3%). Nucleotide sequencing of DNMT3A revealed missense mutations (R882H and R882C), while that of IDH revealed R172K, R140Q, R132H and R132S. Both DNMT3A and IDH mutations were observed only in adults, with a higher frequency in males. DNMT3A and IDH mutations were significantly associated with NPM1, while trends towards higher coexistence with FLT3 mutations were observed. This is the first study to evaluate DNMT3A/IDH mutations in Indian patients. Significant associations among the various molecular markers was observed, that highlights cooperation between them and possible roles in improved risk stratification.