- Benzofuran-chalcone hybrids as potential multifunctional agents against Alzheimer's disease: Synthesis and in vivo studies with transgenic Caenorhabditis elegans
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In the search for effective multifunctional agents for the treatment of Alzheimer's disease (AD), a series of novel hybrids incorporating benzofuran and chalcone fragments were designed and synthesized. These hybrids were screened by using a transgenic Ca
- Sashidhara, Koneni V.,Modukuri, Ram K.,Jadiya, Pooja,Dodda, Ranga Prasad,Kumar, Manoj,Sridhar, Balasubramaniam,Kumar, Vikash,Haque, Rizwanul,Siddiqi, Mohammad Imran,Nazir, Aamir
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- Discovery of coumarin-dihydroquinazolinone analogs as niacin receptor 1 agonist with in-vivo anti-obesity efficacy
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In this study, we presented rational designing and synthesis of coumarin-dihydroquinazolinone conjugates to evaluate their agonist activity at GPR109a receptor. Among the synthesized small molecule library, compound 10c displayed robust agonist action at
- Singh, L. Ravithej,Kumar, Ajeet,Upadhyay, Akanksha,Gupta, Sampa,Palanati, Gopala Reddy,Sikka, Kamakshi,Siddiqi, Mohammad Imran,Yadav, Prem N.,Sashidhara, Koneni V.
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supporting information
p. 208 - 222
(2018/05/14)
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- Synthesis and study of benzofuran-pyran analogs as BMP-2 targeted osteogenic agents
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Twenty-four novel benzofuran-pyran derivatives were synthesized and evaluated for their anti-osteoporotic activity in primary cultures of rat calvarial osteoblasts in vitro. Among all the compounds screened for the alkaline phosphatase activity, three compounds 4e, 4j and 4k showed potent activity at picomolar concentrations in osteoblast differentiating stimulation. Additionally, these compounds were found effective in mineralization, assessed by alizarin red-S staining assay. Compounds were again validated through a series of other in vitro experiments. Moreover, molecular dynamics simulations demonstrated that both benzofuran and pyran moieties are requisite to fit into the active site of BMP-2 receptor, a key target of the osteogenic agents. The obtained results strongly convey that compound 4e is a potential bone anabolic agent among synthesized series, which can be further explored as a drug lead for treating osteoporosis.
- Kushwaha, Pragati,Tripathi, Ashish Kumar,Gupta, Sampa,Kothari, Priyanka,Upadhyay, Akanksha,Ahmad, Naseer,Sharma, Tanuj,Siddiqi,Trivedi, Ritu,Sashidhara, Koneni V.
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p. 103 - 117
(2018/07/06)
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- Benzofuran-pyran hybrids: A new class of potential bone anabolic agents
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Benzofuran moiety is an important pharmacophore showing positive effects on bone health. In the present study, sixteen benzofuran-pyran hybrids were synthesized and were evaluated for their osteogenic effects on primary osteoblast cells isolated from calv
- Gupta, Sampa,Adhikary, Sulekha,Modukuri, Ram K.,Choudhary, Dharmendra,Trivedi, Ritu,Sashidhara, Koneni V.
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supporting information
p. 1719 - 1724
(2018/05/04)
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- Synthesis and bio-evaluation of indole-chalcone based benzopyrans as promising antiligase and antiproliferative agents
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DNA replication and repair are complex processes accomplished by the concerted action of a network of enzymes and proteins. DNA ligases play a crucial role in these processes by catalyzing the nick joining between DNA strands. As compared to normal cells,
- Gupta, Sampa,Maurya, Pooja,Upadhyay, Akanksha,Kushwaha, Pragati,Krishna, Shagun,Siddiqi, Mohammad Imran,Sashidhara, Koneni V.,Banerjee, Dibyendu
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p. 1981 - 1996
(2017/11/27)
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- Benzthiazole-derived chromogenic, fluorogenic and ratiometric probes for detection of hydrazine in environmental samples and living cells
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Benzothiazole-based chromogenic and ratiometric fluorescent chemodosimetric probes CD1 and CD2, were synthesized and characterized. The probes are designed in such a way that the excited state intramolecular proton transfer (ESIPT) of the benzothiazole moiety gets blocked. Upon treatment with hydrazine in organo-aqueous medium[DMSO: H2O; 2:1 (v/v)] at physiological pH, the aectyl protective group of probes CD1 and CD2 were removed readily in presence hydrazine and ESIPT of the probes were switched on, which resulted remarkable photo-physical changes. These two ESIPT–based ratiometric fluorescent probes were shown to be selective and sensitive for hydrazine among different cations, anions and amines studied in organo-aqueous medium[DMSO: H2O; 2:1 (v/v)] at physiological pH, by fluorescence, absorption, and visual emission color change. These key features allows the two probes to be employed for hydrazine detection by simple visual inspection. DFT and TDDFT calculations were performed in order to demonstrate the sensing mechanism and the electronic properties of probe and hydrazinolysis product. An easy-to-prepare test strips, obtained by dipping the TLC plates into the solution of CD1 and CD2, were able to detect hydrazine in practical samples. Moreover, the utility of the probes CD1 in showing the hydrazine recognition in live cells has also been demonstrated using Vero cells as monitored by fluorescence imaging.
- Mahapatra, Ajit Kumar,Karmakar, Parthasarathi,Manna, Srimanta,Maiti, Kalipada,Mandal, Debasish
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- Design, synthesis and anticancer activity of dihydropyrimidinone-semicarbazone hybrids as potential human DNA ligase 1 inhibitors
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A series of new dihydropyrimidinone-semicarbazone hybrids were successfully synthesised by integrating regioselective multicomponent reaction with the pharmacophore hybridization approach. All the synthesised compounds were evaluated for their hLig1 inhibition potency and most of them were found to be good to moderately active. Out of the tested derivatives, compound 6f showed selective anti-proliferative activity against HepG2 cells in a dose-dependent manner with an IC50 value of 10.07 ± 1.2. It also reduced cell survival at ≤20 μM concentration. Further, analysis of treated HepG2 cell lysates by western blot assay showed increased γ-H2AX levels and upregulation of p53, leading to apoptosis. In silico docking results explain the binding modes of compound 6f to the DNA-binding domain of hLig1 enzyme thereby preventing its nick sealing activity. In addition, the favourable pharmacokinetic properties suggest that this new class of hLig1 inhibitors could be promising leads for further drug development.
- Sashidhara, Koneni V.,Singh, L. Ravithej,Shameem, Mohammad,Shakya, Sarika,Kumar, Anoop,Laxman, Tulsankar Sachin,Krishna, Shagun,Siddiqi, Mohammad Imran,Bhatta, Rabi S.,Banerjee, Dibyendu
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p. 2349 - 2363
(2016/12/16)
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- Design, synthesis and in vitro evaluation of coumarin-imidazo[1,2-a]pyridine derivatives against cancer induced osteoporosis
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A series of biologically important 6-(imidazo[1,2-a]pyridin-2-yl)-2H-chromen-2-one derivatives were synthesized by employing the silver(I) catalysed Groebke-Blackburn-Bienayme multicomponent reaction. The synthesized compounds were tested in a primary calvarial osteoblast cells by alkaline phosphatase assay and an alizarin red-S staining assay for their possible osteoprotective properties. Further, the effects of active compounds 6h, 6l, and 6o on the expression of osteogenic genes BMP2, RUNX2, COL1, and OCN were measured by qPCR. Out of three promising compounds, 6l and 6o significantly induced apoptosis in MDA-MB-231 cancer cells via mitochondrial depolarisation without affecting normal cells. In an in vitro co-culture model of bone metastasis, we investigated the ability of coumarin-imidazo[1,2-a]pyridine hybrids to reverse the negative impact of MDA-MB-231 cancer cells on osteoblast differentiation. The results illustrate the potential of designed hybrids to re-establish the bone homeostasis. These findings demonstrate the significance of newly synthesized hybrids as lead molecules, possessing both anti-osteoporotic and anticancer properties that can be developed into new therapeutic agents to alleviate osteoporosis and bone metastasis.
- Sashidhara, Koneni V.,Singh, L. Ravithej,Choudhary, Dharmendra,Arun, Ashutosh,Gupta, Sampa,Adhikary, Sulekha,Palnati, Gopala Reddy,Konwar, Rituraj,Trivedi, Ritu
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p. 80037 - 80048
(2017/04/03)
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- Hybrids of coumarin-indole: Design, synthesis and biological evaluation in Triton WR-1339 and high-fat diet induced hyperlipidemic rat models
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In this study, a series of coumarin-indole hybrids have been synthesized and evaluated for their lipid lowering activity. Preliminary biological screening of the synthesized compounds was undertaken in an in vitro model of the HMG-CoA reductase enzyme, an
- Sashidhara, Koneni V.,Rao, K. Bhaskara,Sonkar, Ravi,Modukuri, Ram K.,Chhonker, Yashpal S.,Kushwaha, Pragati,Chandasana, Hardik,Khanna,Bhatta, Rabi S.,Bhatia, Gitika,Suthar, Manish Kumar,Saxena, Jitendra Kumar,Kumar, Vikash,Siddiqi, Mohammad Imran
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p. 1858 - 1869
(2016/09/28)
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- Highly efficient synthesis of chalcones from poly carbonyl aromatic compounds using bf3-et2o via a regioselective condensation reaction
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A new, simple, highly efficient method for the synthesis of different types of carbonyl chalcones through a regioselective condensation reaction of appropriate 5-acetyl-2-hydroxybenzaldehyde with various substituted acetophenones and 4-hydroxyisothalaldehyde with various substituted aldehydes using BF3-Et2O as a reagent is described.
- Julakanti, Satyanarayana Reddy,Patel, Manimala,Ponneri, Venkateswarlu
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p. 570 - 576
(2016/06/09)
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- Designing, synthesis of selective and high-affinity chalcone-benzothiazole hybrids as Brugia malayi thymidylate kinase inhibitors: In vitro validation and docking studies
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In our continuing search for safe and efficacious antifilarials, a series of novel chalcone-benzothiazole hybrids have been synthesized and evaluated for their Brugia malayi thymidylate kinase (BmTMK) enzyme inhibition activity. Their selectivity towards BmTMK was studied and compared to the human TMK (HsTMK) by an in silico method. Out of seventeen derivatives, compounds 34 and 42 showed higher interactions with the BmTMK active site. MolDock docking model revealed the interactions of these two derivatives and the results corroborated well with their in vitro antifilarial activities. Our studies suggest that these hybrids are selective towards the BmTMK enzyme and may serve as potential therapeutic agents against filariasis.
- Sashidhara, Koneni V.,Avula, Srinivasa Rao,Doharey, Pawan Kumar,Singh, L. Ravithej,Balaramnavar, Vishal M.,Gupta, Jyoti,Misra-Bhattacharya, Shailja,Rathaur, Sushma,Saxena, Anil K.,Saxena, Jitendra Kumar
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p. 418 - 428
(2015/09/28)
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- Design and synthesis of new series of coumarin-aminopyran derivatives possessing potential anti-depressant-like activity
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A new series of coumarin based aminopyran derivatives were designed, synthesized and evaluated for their preclinical antidepressant effect on Swiss albino mice. Among the series, compounds 21, 25, 26, 27, 32 and 33 exhibited significant activity profile i
- Sashidhara, Koneni V.,Modukuri, Ram K.,Singh, Seema,Bhaskara Rao,Aruna Teja,Gupta, Sampa,Shukla, Shubha
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supporting information
p. 337 - 341
(2015/02/19)
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- Synthesis and antifilarial activity of chalcone-thiazole derivatives against a human lymphatic filarial parasite, Brugia malayi
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Here we report the synthesis of novel chalcone-thiazole compounds and their antifilarial activity. The antifilarial properties of these hybrids were assessed against microfilariae as well as adult worms of Brugia malayi. Among all the synthesized compound
- Sashidhara, Koneni V.,Rao, K. Bhaskara,Kushwaha, Vikas,Modukuri, Ram K.,Verma, Richa,Murthy
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p. 473 - 480
(2014/06/09)
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- Synthesis and evaluation of new 3-phenylcoumarin derivatives as potential antidepressant agents
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A series of amine substituted 3-phenyl coumarin derivatives were designed and synthesized as potential antidepressant agents. In preliminary screening, all compounds were evaluated in forced swimming test (FST), a model to screen antidepressant activity i
- Sashidhara, Koneni V.,Rao, K. Bhaskara,Singh, Seema,Modukuri, Ram K.,Aruna Teja,Chandasana, Hardik,Shukla, Shubha,Bhatta, Rabi S.
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p. 4876 - 4880
(2014/12/11)
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- Coumarin chalcone fibrates: A new structural class of lipid lowering agents
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In our continuing search for safe and efficacious antidyslipidemic agents, structurally interesting coumarin-chalcone fibrates were synthesized and evaluated in triton WR-1339 induced hyperlipidemic rats. The most active compound 41 decreased the total cholesterol (TC), phospholipids (PL) and triglycerides (TG), of hyperlipidemic rats by 26, 24, and 25% respectively. In addition, the compound 41 significantly reversed the levels of VLDL, LDL HDL and also increased the LPL activity. Altogether, our data suggests that these novel hybrids would be a potential new class of therapeutic agents against dyslipidemia.
- Sashidhara, Koneni V.,Palnati, Gopala Reddy,Sonkar, Ravi,Avula, Srinivasa Rao,Awasthi, Chetan,Bhatia, Gitika
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p. 422 - 431
(2013/07/27)
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- Hybrid benzofuran-bisindole derivatives: New prototypes with promising anti-hyperlipidemic activities
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A series of different benzofuran-bisindole hybrids were synthesized and evaluated in vitro for their antioxidant and in vivo for antidyslipidemic activity in triton WR-1339 induced hyperlipidemic rats. Among the series, compounds 4a, 4c, 4h and 4j showed
- Sashidhara, Koneni V.,Modukuri, Ram K.,Sonkar, Ravi,Rao, K. Bhaskara,Bhatia, Gitika
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- Synthesis and evaluation of new coumarin-pyridine hybrids with promising anti-osteoporotic activities
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Anti-osteoporotic effects of the newly synthesized coumarin-pyridine hybrids were evaluated in primary cultures of rat calvarial osteoblasts in vitro. Compounds 6a, i, j and k were potent in stimulating osteoblast differentiation and mineralization as ass
- Sashidhara, Koneni V.,Modukuri, Ram K.,Choudhary, Dharmendra,Bhaskara Rao,Kumar, Manoj,Khedgikar, Vikram,Trivedi, Ritu
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p. 802 - 810
(2013/12/04)
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- Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent
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Development of new, targeted antibreast cancer drug which can treat both the hormone receptor (positive and negative) breast cancers is a very challenging task. The concept of molecular hybridization led us to discover a novel class of coumarin-monastrol
- Sashidhara, Koneni V.,Avula, Srinivasa Rao,Sharma, Komal,Palnati, Gopala Reddy,Bathula, Surendar Reddy
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p. 120 - 127
(2013/03/29)
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- Coumarin-trioxane hybrids: Synthesis and evaluation as a new class of antimalarial scaffolds
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First synthesis of novel coumarin-trioxane hybrids is reported. The synthesis was achieved via condensation of β-hydroxyhydroperoxides with coumarinic-aldehydes in presence of p-toluenesulfonic acid in good yields and the novel hybrids were evaluated for
- Sashidhara, Koneni V.,Kumar, Abdhesh,Dodda, Ranga Prasad,Krishna, Naikade Niraj,Agarwal, Pooja,Srivastava, Kumkum,Puri
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supporting information; experimental part
p. 3926 - 3930
(2012/07/03)
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- In vitro and in vivo antifilarial activity evaluation of 3,6-epoxy [1,5]dioxocines: A new class of antifilarial agents
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A series of 3,6-epoxy [1,5]dioxocines were synthesized and evaluated for their antifilarial activity against adult parasites of human lymphatic filarial parasite Brugia malayi (sub-periodic strain) in vitro. Out of these, six compounds (4a-f) possessed im
- Sashidhara, Koneni V.,Kumar, Abdhesh,Rao, K. Bhaskara,Kushwaha, Vikas,Saxena, Kirti,Murthy
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scheme or table
p. 1527 - 1532
(2012/03/26)
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- Antiplasmodial activity of novel keto-enamine chalcone-chloroquine based hybrid pharmacophores
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A series of novel keto-enamine chalcone-chloroquine based hybrids were synthesized following new methodology developed in our laboratory. The synthesized compounds were screened against chloroquine sensitive strain (3D7) of Plasmodium falciparum in an in
- Sashidhara, Koneni V.,Kumar, Manoj,Modukuri, Ram K.,Srivastava, Rajeev Kumar,Soni, Awakash,Srivastava, Kumkum,Singh, Shiv Vardan,Saxena,Gauniyal, Harsh M.,Puri, Sunil K.
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scheme or table
p. 2971 - 2981
(2012/07/02)
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- Discovery and synthesis of novel 3-phenylcoumarin derivatives as antidepressant agents
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A series of 3-phenylcoumarins were synthesized and screened for potential antidepressant activity by tail suspension test (TST) in mice. Three compounds (6, 7 and 13) exhibited impressive antidepressant activity, measured in terms of percentage decrease i
- Sashidhara, Koneni V.,Kumar, Abdhesh,Chatterjee, Manavi,Rao, K. Bhaskara,Singh, Seema,Verma, Anil Kumar,Palit, Gautam
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supporting information; experimental part
p. 1937 - 1941
(2011/04/24)
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- BENZOPYRAN COMPOUNDS USEFUL FOR TREATING INFLAMMATORY CONDITIONS
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The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula (1). Wherein Z, X, R1, R2, R3, and R4 are as described in specification.
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Page 515-516
(2010/02/08)
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- CHROMENE DERIVATIVES AS ANTI-INFLAMMATORY AGENTS
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The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula (I). Wherein Z, X, R1, R2, R3, and R4 are as described in the specification.
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Page 515-516
(2010/02/08)
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