I, R.ELANCHERAN, Senior Research Fellow under the DBT project at the Life Sciences Division, Institute of Advanced Study in Science and Technology (IASST), Guwahati, India. I received my M.Sc. in Organic Chemistry from Annamalai University, Tamil Nadu, India. I have worked two years with Orchid Chemicals & Pharmaceutical Pvt Ltd, Chennai, as a Research Executive in Medicinal Chemistry Department. Currently, I am doing my Ph.D. in Chemistry from Gauhati University at Institute of Advanced Study in Science and Technology (IASST), Govt. of India (DST institute), Guwahati, Assam-781035. My research topic is “Design and Development of therapy for prostate cancer based on synthetic and semi-synthetic molecules”. My current research interests include cancer drug-design-development, phyto- chemistry and organic synthesis. Supervisors: Dr.Jibon Kotoky Phone: 09085936358 Address: Guwahati
The structural modification and molecular docking-based screening approaches on thiazole-based is... more The structural modification and molecular docking-based screening approaches on thiazole-based isoin-dolinediones were imposed to find the novel 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives. The best fit compounds (6a-n) were synthesized and evaluated their antiproliferative activities on the prostate cancer cell lines (PC-3 & LNCaP). Among them, the compound, 6m exhibited good activity, particularly on LNCaP (IC 50 = 5.96 ± 1.6 lM), moderately active against PC-3 cell lines as compared to bicalutamide. The compound, 6m decreased the androgen-mediated transcription of ARE-mRNA in PSA, TMPRSS2, c-myc and cyclin D1 than R-bicalutamide. The compounds, 6e and 6f were reconfirmed through single crystal XRD analysis. The ADME profiling of the test compounds was evaluated to find the drug-likeness and pharmacokinetic parameters. These findings may provide vital information for the development of anti-prostate cancer agents.
The study aimed to identify the phenolic compounds present in Centella asiatica (L.) (C. asiatica... more The study aimed to identify the phenolic compounds present in Centella asiatica (L.) (C. asiatica) extract and evaluate the respective antioxidant potential as well as its cholesterol-lowering effects in the experimental animal model. Herein, the antioxidant potential of extracts was assessed by its free radical scavenging activity such as 2, 2-diphenyl-1-picrylhydrazyl as well as reducing capability. The anti-hyperlipidemic effects of C. asiatica extract (CAE) were evaluated in high cholesterol-fed (HCF) rats for 4 weeks, where different concentrations of extracts (0.25, 0.5, and 1 g/kg/day) were orally administrated daily. Lipid and antioxidant profiles, including total cholesterol (TC), triglyceride (TG), low density lipoprotein cholesterol (LDL-C), high density lipoprotein cholesterol (HDL-C) and superoxide dismutase (SOD), together with the indices of hepatic functions were also examined. C. asiatica revealed excellent free radical scavenging activity as revealed by 2-2-diphenyl-1-picryl-hydrazyl (DPPH) assay, with the IC 50 values (9.62 ± 0.88 µg/mL). Furthermore, C. asiatica extracts and fenofibrate remarkably lowered the level of TC, TG, LDL-C, and showed elevated levels of HDL-C, SOD. The histopathological observations further demonstrated clear differentiation and structural changes in liver of HCF and CAE treated group. Furthermore, gulonic acid, ferulic acid, kaempferol, chlorogenic acid, and asiatic acid were identified to be the major components which might be responsible for the antioxidant activity of the C. asiatica extract as evidenced from an ultra-high performance liquid chromatography– mass spectrometer. Taken together, these results signifies the excellent antioxidant and anti-hyperlipidemic properties of C. asiatica leaf extracts, which might be useful for the treatment of oxidative-stress related diseases such as hyperlipidemia.
Breast cancer is the most prominent cause of cancer death in women worldwide. The highlights of t... more Breast cancer is the most prominent cause of cancer death in women worldwide. The highlights of this review are to provide an overview of the targeted therapeutic agents, challenges with metastatic breast cancer (MBCa), mechanisms of action through Hedgehog/Gli 1 signaling pathway and future prospective. Over a decade of success, several drugs have been approved and are in the advanced stages of clinical trials that target the receptors such as estrogen receptor, growth factor receptor, receptor activator of nuclear factor kappa-B, etc. Currently, several monoclonal antibodies are also used for the treatment of breast cancer. Advances in understanding tumor biology, particularly signaling pathways such as Notch signaling pathway, Hedgehog/Gli 1 signaling pathway, and inhibitors are considered to be important for bone metastasis. These studies may provide vital information for the design and development of new strategies with respect to efficacy, reduction of the side effects, and treatment strategies.
The title isoindole, C18H8N3O2S, crystallizes with two independent molecules ( A and B) in the as... more The title isoindole, C18H8N3O2S, crystallizes with two independent molecules ( A and B) in the asymmetric unit whose geometrical features are similar. The benzonitrile ring is oriented at an angle of 2.1 (1) (molecule A) and 16.0 (1) (molecule B), with respect to the isoindole ring system. In the crystal, A molecules are linked via C—H N hydrogen bonds, forming C(15) chains propagating along the c axis. B molecules are linked via C—H O interactions, forming dimers with an R2(10) graph-set motif. C—H O and C—H N interactions, characterized by R2(15) and R12(7) motifs, are observed between molecules A and B.
Fatty foods, the most common diet today are the crux of many metabolic disorders which need urgen... more Fatty foods, the most common diet today are the crux of many metabolic disorders which need urgent attention. Garcinia pedunculata Roxb. (GP, Clusiaceae) is a plant found available in Northeast (NE) region of India, is considered to have versatile therapeutic properties. The people of this region has been using dried pulp of GP fruit for the treatment of different stomach related diseases traditionally. This study aimed at evaluating the potential therapeutic action of the polyphenol-rich methanolic extract of the fruit in experimental induced obese rats. In vitro antioxidant and antidiabetic activity of GP extracts, i.e., fruit extract (GF) and seed extract (GS) were determined by using various methods viz., 1,1-diphenyl-2 picrylhydrazyl (DPPH), 2,2-Azinobis (3-ethyl benzthiazoline-6-sulphonic acid) (ABTS • +), nitroblue tetrazolium (NBT) and α-glucosidase inhibition assay for detection of antihyperglycemic activity. In vivo antilipidemic and antiobesity activities were evaluated by administrating oral dose of GF for 60 days on a high-fat diet (HFD) induced hyperlipidemia in the rat. GF showed higher antioxidant activity than GS by DPPH radical scavenging (IC 50 = 4.01 µg/ml), ABTS • + (IC 50 = 0.82 µg/ml), NBT (IC 50 = 0.07 µg/ml) and also showed notable α-glucosidase inhibitory activity (IC 50 = 19.26 µg/ml). Furthermore, GF treated rat revealed a reduction in the body weight (∼60%), serum total cholesterol (33%), triglycerides (32%), low-density lipoprotein (38%) and liver biomarker enzymes after 60 days HFD fed animals. Simultaneously, GF supplementation significantly protected the HFD induced changes in hematological parameters. Histological observations clearly differentiate the structural changes in liver of HFD and GF treated group. This novel dietary lipid adsorbing agent of GF exhibited prevention of hyperlipidemia induced by HFD in the rat.
The title acetamide, C11H9ClN2OS, crystallizes with two independent molecules
in the asymmetric u... more The title acetamide, C11H9ClN2OS, crystallizes with two independent molecules in the asymmetric unit whose geometrical features are similar. The phenyl ring is oriented at angles of 2.5 (1) and 6.2 (1) with respect to the thiazole ring in the two molecules. In the crystal, molecules are linked via C—H N hydrogen bonds which form C(10) chains along the [100] direction. The chains are linked by N—H O and C—H O hydrogen bonds, forming C(8) chains along the [100] direction.
The aim of the study was to identify the phenolic compounds present in Hydrocotyle sibthorpioides... more The aim of the study was to identify the phenolic compounds present in Hydrocotyle sibthorpioides (HS), Centella asiatica (CA) and Amaranthus viridis (AV) extracts and investigate their respective antioxidant activities. Herein, an ultra-high pressure liquid chromatography–mass spectrometer (UPLC-MS/MS) analytical method has been developed for the separation, and systematic characterization of the phenolic compounds in HS, CA and AV extracts and was compared along with ten standard phenolic compounds. Additionally, in vitro antioxidant activity of the phenolic compounds was also determined. The HS extract revealed excellent antioxidant activity such as 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity (IC50 = 19.7 ± 1.2 μg/mL), total reduction capability (0.169 ± 0.003 at 100 μg/mL), nitric oxide radical scavenging activity (IC50= 39.33 ± 3.2 μg/mL), metal chelating activity (IC50 = 56.51 ± 3.6 μg/mL) and inhibition of lipid peroxidation (IC50 = 12.34 ± 2.3 μg/mL) as compared to CA and AV extracts. Furthermore, catechin, epicatechin, quercetin and chlorogenic acid were found to be the major components responsible for the antioxidant activity of the HS extract as evidenced from UPLC-MS/MS. Taken together, this study demonstrates the promising antioxidant properties of the HS extract, which can further be utilized in various pharmaceutical, food, and agricultural applications.
Antiandrogens are a novel class of anticancer agents that inhibit cancer cell proliferation and i... more Antiandrogens are a novel class of anticancer agents that inhibit cancer cell proliferation and induce apoptosis in various cell lines. To find the lead compound from the oxobenzimidazole derivatives, receptor-ligand docking studies were initially performed using Schrödinger software. The best fit molecules were synthesized and characterized through IR, 1H-NMR, 13C-NMR and HRMS analyses. The structure of compound (9b) was further confirmed by single crystal XRD analysis. The cell viability of the compounds was determined by MTT assay to find IC50 values against prostate cancer and breast cancer cell lines (PC-3, LNCaP, MCF-7 and MDA-MB-231). The ADME/T property studies were performed to rationalize the inhibitory properties of these compounds. It can be concluded from the study that 9b is the most active compound from the series against PC-3 & LNCaP cell lines.
The main focus of the review is to discuss the discoveries and developments of various therapies ... more The main focus of the review is to discuss the discoveries and developments of various therapies for prostate cancer. The AR has played an important role in Prostate cancer growth and functions. In this review, we discussed several groups of drugs that have sparingly good anti-cancer activities, also have a similar structure and behaviour. Recent new-generation AR antagonists, Enzalutamide (MDV3100) has approved for the treatment of advanced/metastatic Prostate Cancer. The Nonsteroidal antiandrogens represent an important class of molecules acting as either antagonists or agonists. Recently, many therapeutic agents for Prostate cancer have been approved that target the androgen receptor and reduces the Prostate tumour growth. The strong response to this new use of Enzalutamide provides a viable, less toxic alternative to chemotherapy. The current status of Prostate cancer drugs have been discussed here, but it is evident that much work for improvements in respect of efficacy, reduction of side effects and treatment strategies are to be addressed.
The structural modification and molecular docking-based screening approaches on thiazole-based is... more The structural modification and molecular docking-based screening approaches on thiazole-based isoin-dolinediones were imposed to find the novel 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives. The best fit compounds (6a-n) were synthesized and evaluated their antiproliferative activities on the prostate cancer cell lines (PC-3 & LNCaP). Among them, the compound, 6m exhibited good activity, particularly on LNCaP (IC 50 = 5.96 ± 1.6 lM), moderately active against PC-3 cell lines as compared to bicalutamide. The compound, 6m decreased the androgen-mediated transcription of ARE-mRNA in PSA, TMPRSS2, c-myc and cyclin D1 than R-bicalutamide. The compounds, 6e and 6f were reconfirmed through single crystal XRD analysis. The ADME profiling of the test compounds was evaluated to find the drug-likeness and pharmacokinetic parameters. These findings may provide vital information for the development of anti-prostate cancer agents.
The study aimed to identify the phenolic compounds present in Centella asiatica (L.) (C. asiatica... more The study aimed to identify the phenolic compounds present in Centella asiatica (L.) (C. asiatica) extract and evaluate the respective antioxidant potential as well as its cholesterol-lowering effects in the experimental animal model. Herein, the antioxidant potential of extracts was assessed by its free radical scavenging activity such as 2, 2-diphenyl-1-picrylhydrazyl as well as reducing capability. The anti-hyperlipidemic effects of C. asiatica extract (CAE) were evaluated in high cholesterol-fed (HCF) rats for 4 weeks, where different concentrations of extracts (0.25, 0.5, and 1 g/kg/day) were orally administrated daily. Lipid and antioxidant profiles, including total cholesterol (TC), triglyceride (TG), low density lipoprotein cholesterol (LDL-C), high density lipoprotein cholesterol (HDL-C) and superoxide dismutase (SOD), together with the indices of hepatic functions were also examined. C. asiatica revealed excellent free radical scavenging activity as revealed by 2-2-diphenyl-1-picryl-hydrazyl (DPPH) assay, with the IC 50 values (9.62 ± 0.88 µg/mL). Furthermore, C. asiatica extracts and fenofibrate remarkably lowered the level of TC, TG, LDL-C, and showed elevated levels of HDL-C, SOD. The histopathological observations further demonstrated clear differentiation and structural changes in liver of HCF and CAE treated group. Furthermore, gulonic acid, ferulic acid, kaempferol, chlorogenic acid, and asiatic acid were identified to be the major components which might be responsible for the antioxidant activity of the C. asiatica extract as evidenced from an ultra-high performance liquid chromatography– mass spectrometer. Taken together, these results signifies the excellent antioxidant and anti-hyperlipidemic properties of C. asiatica leaf extracts, which might be useful for the treatment of oxidative-stress related diseases such as hyperlipidemia.
Breast cancer is the most prominent cause of cancer death in women worldwide. The highlights of t... more Breast cancer is the most prominent cause of cancer death in women worldwide. The highlights of this review are to provide an overview of the targeted therapeutic agents, challenges with metastatic breast cancer (MBCa), mechanisms of action through Hedgehog/Gli 1 signaling pathway and future prospective. Over a decade of success, several drugs have been approved and are in the advanced stages of clinical trials that target the receptors such as estrogen receptor, growth factor receptor, receptor activator of nuclear factor kappa-B, etc. Currently, several monoclonal antibodies are also used for the treatment of breast cancer. Advances in understanding tumor biology, particularly signaling pathways such as Notch signaling pathway, Hedgehog/Gli 1 signaling pathway, and inhibitors are considered to be important for bone metastasis. These studies may provide vital information for the design and development of new strategies with respect to efficacy, reduction of the side effects, and treatment strategies.
The title isoindole, C18H8N3O2S, crystallizes with two independent molecules ( A and B) in the as... more The title isoindole, C18H8N3O2S, crystallizes with two independent molecules ( A and B) in the asymmetric unit whose geometrical features are similar. The benzonitrile ring is oriented at an angle of 2.1 (1) (molecule A) and 16.0 (1) (molecule B), with respect to the isoindole ring system. In the crystal, A molecules are linked via C—H N hydrogen bonds, forming C(15) chains propagating along the c axis. B molecules are linked via C—H O interactions, forming dimers with an R2(10) graph-set motif. C—H O and C—H N interactions, characterized by R2(15) and R12(7) motifs, are observed between molecules A and B.
Fatty foods, the most common diet today are the crux of many metabolic disorders which need urgen... more Fatty foods, the most common diet today are the crux of many metabolic disorders which need urgent attention. Garcinia pedunculata Roxb. (GP, Clusiaceae) is a plant found available in Northeast (NE) region of India, is considered to have versatile therapeutic properties. The people of this region has been using dried pulp of GP fruit for the treatment of different stomach related diseases traditionally. This study aimed at evaluating the potential therapeutic action of the polyphenol-rich methanolic extract of the fruit in experimental induced obese rats. In vitro antioxidant and antidiabetic activity of GP extracts, i.e., fruit extract (GF) and seed extract (GS) were determined by using various methods viz., 1,1-diphenyl-2 picrylhydrazyl (DPPH), 2,2-Azinobis (3-ethyl benzthiazoline-6-sulphonic acid) (ABTS • +), nitroblue tetrazolium (NBT) and α-glucosidase inhibition assay for detection of antihyperglycemic activity. In vivo antilipidemic and antiobesity activities were evaluated by administrating oral dose of GF for 60 days on a high-fat diet (HFD) induced hyperlipidemia in the rat. GF showed higher antioxidant activity than GS by DPPH radical scavenging (IC 50 = 4.01 µg/ml), ABTS • + (IC 50 = 0.82 µg/ml), NBT (IC 50 = 0.07 µg/ml) and also showed notable α-glucosidase inhibitory activity (IC 50 = 19.26 µg/ml). Furthermore, GF treated rat revealed a reduction in the body weight (∼60%), serum total cholesterol (33%), triglycerides (32%), low-density lipoprotein (38%) and liver biomarker enzymes after 60 days HFD fed animals. Simultaneously, GF supplementation significantly protected the HFD induced changes in hematological parameters. Histological observations clearly differentiate the structural changes in liver of HFD and GF treated group. This novel dietary lipid adsorbing agent of GF exhibited prevention of hyperlipidemia induced by HFD in the rat.
The title acetamide, C11H9ClN2OS, crystallizes with two independent molecules
in the asymmetric u... more The title acetamide, C11H9ClN2OS, crystallizes with two independent molecules in the asymmetric unit whose geometrical features are similar. The phenyl ring is oriented at angles of 2.5 (1) and 6.2 (1) with respect to the thiazole ring in the two molecules. In the crystal, molecules are linked via C—H N hydrogen bonds which form C(10) chains along the [100] direction. The chains are linked by N—H O and C—H O hydrogen bonds, forming C(8) chains along the [100] direction.
The aim of the study was to identify the phenolic compounds present in Hydrocotyle sibthorpioides... more The aim of the study was to identify the phenolic compounds present in Hydrocotyle sibthorpioides (HS), Centella asiatica (CA) and Amaranthus viridis (AV) extracts and investigate their respective antioxidant activities. Herein, an ultra-high pressure liquid chromatography–mass spectrometer (UPLC-MS/MS) analytical method has been developed for the separation, and systematic characterization of the phenolic compounds in HS, CA and AV extracts and was compared along with ten standard phenolic compounds. Additionally, in vitro antioxidant activity of the phenolic compounds was also determined. The HS extract revealed excellent antioxidant activity such as 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity (IC50 = 19.7 ± 1.2 μg/mL), total reduction capability (0.169 ± 0.003 at 100 μg/mL), nitric oxide radical scavenging activity (IC50= 39.33 ± 3.2 μg/mL), metal chelating activity (IC50 = 56.51 ± 3.6 μg/mL) and inhibition of lipid peroxidation (IC50 = 12.34 ± 2.3 μg/mL) as compared to CA and AV extracts. Furthermore, catechin, epicatechin, quercetin and chlorogenic acid were found to be the major components responsible for the antioxidant activity of the HS extract as evidenced from UPLC-MS/MS. Taken together, this study demonstrates the promising antioxidant properties of the HS extract, which can further be utilized in various pharmaceutical, food, and agricultural applications.
Antiandrogens are a novel class of anticancer agents that inhibit cancer cell proliferation and i... more Antiandrogens are a novel class of anticancer agents that inhibit cancer cell proliferation and induce apoptosis in various cell lines. To find the lead compound from the oxobenzimidazole derivatives, receptor-ligand docking studies were initially performed using Schrödinger software. The best fit molecules were synthesized and characterized through IR, 1H-NMR, 13C-NMR and HRMS analyses. The structure of compound (9b) was further confirmed by single crystal XRD analysis. The cell viability of the compounds was determined by MTT assay to find IC50 values against prostate cancer and breast cancer cell lines (PC-3, LNCaP, MCF-7 and MDA-MB-231). The ADME/T property studies were performed to rationalize the inhibitory properties of these compounds. It can be concluded from the study that 9b is the most active compound from the series against PC-3 & LNCaP cell lines.
The main focus of the review is to discuss the discoveries and developments of various therapies ... more The main focus of the review is to discuss the discoveries and developments of various therapies for prostate cancer. The AR has played an important role in Prostate cancer growth and functions. In this review, we discussed several groups of drugs that have sparingly good anti-cancer activities, also have a similar structure and behaviour. Recent new-generation AR antagonists, Enzalutamide (MDV3100) has approved for the treatment of advanced/metastatic Prostate Cancer. The Nonsteroidal antiandrogens represent an important class of molecules acting as either antagonists or agonists. Recently, many therapeutic agents for Prostate cancer have been approved that target the androgen receptor and reduces the Prostate tumour growth. The strong response to this new use of Enzalutamide provides a viable, less toxic alternative to chemotherapy. The current status of Prostate cancer drugs have been discussed here, but it is evident that much work for improvements in respect of efficacy, reduction of side effects and treatment strategies are to be addressed.
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Papers by Elancheran R
in the asymmetric unit whose geometrical features are similar. The phenyl ring is
oriented at angles of 2.5 (1) and 6.2 (1) with respect to the thiazole ring in the
two molecules. In the crystal, molecules are linked via C—H N hydrogen
bonds which form C(10) chains along the [100] direction. The chains are linked
by N—H O and C—H O hydrogen bonds, forming C(8) chains along the
[100] direction.
in the asymmetric unit whose geometrical features are similar. The phenyl ring is
oriented at angles of 2.5 (1) and 6.2 (1) with respect to the thiazole ring in the
two molecules. In the crystal, molecules are linked via C—H N hydrogen
bonds which form C(10) chains along the [100] direction. The chains are linked
by N—H O and C—H O hydrogen bonds, forming C(8) chains along the
[100] direction.