THIRTY FIVE YEARS OF OPERATIONAL RESEARCH PROJECT FOR DRYLAND AGRICULTURE : ACHIEVEMENTS AND IMPACTS (1976 to 2012)

Not AvailableAgriculture is the backbone of Indian economy and rainfed agro-ecosystem occupies an important place in Indian agriculture, covering 68 per cent of the cultivated area (96 m.ha) supporting 40 per cent human, 60 per cent livestock population and producing 44 per cent of the food requirements thus playing a pivotal role in India’s food security. Five out of ten Agro-Climatic Zones in Karnataka were classified as dry zones covering 63 per cent of the total geographical area and 71 per cent of the net sown area, with substantial contribution to agricultural production from dry lands. About 57 per cent of food grain production in Karnataka comes from rainfed areas while, 97 per cent of total pulses and 80 per cent oilseeds were produced in dry land areas. Research on dryland agriculture in the red soil regions of Karnataka was started in 1970 with the establishment of All India Coordinated Research Project for Dryland Agriculture (AICRPDA) at Gandhi Krishi Vignana Kendra (GKVK), Bangalore,Not Availabl

STK295900, a Dual Inhibitor of Topoisomerase 1 and 2, Induces G<inf>2</inf> Arrest in the Absence of DNA Damage

STK295900, a small synthetic molecule belonging to a class of symmetric bibenzimidazoles, exhibits antiproliferative activity against various human cancer cell lines from different origins. Examining the effect of STK295900 in HeLa cells indicates that it induces G2 phase arrest without invoking DNA damage. Further analysis shows that STK295900 inhibits DNA relaxation that is mediated by topoisomerase 1 (Top 1) and topoisomerase 2 (Top 2) in vitro. In addition, STK295900 also exhibits protective effect against DNA damage induced by camptothecin. However, STK295900 does not affect etoposide-induced DNA damage. Moreover, STK295900 preferentially exerts cytotoxic effect on cancer cell lines while camptothecin, etoposide, and Hoechst 33342 affected both cancer and normal cells. Therefore, STK295900 has a potential to be developed as an anticancer chemotherapeutic agent. © 2013 Kim et al

Synthesis and Crystal Structure of 1-Benzhydryl-4-Methane-Sulfonyl-Piperazine

The title compound, 1-benzhydryl-4-methanesulfonyl-piperazine, was synthesized by the nucleophilic substitution of 1-benzhydryl-piperazine with methyl sulfonyl chloride. The product obtained was characterized by spectroscopic techniques, and the structure was investigated by X-ray crystallography. The compound crystallizes in the monoclinic crystal class in the space group P21/c with cell parameters a = 9.5820(4) A○, b = 16.8150(12) A○, c = 13.5280(8) A○, β = 127.270(5)°, and V = 1734.5(2)A○ 3 for Z = 4. The structure reveals that the piperazine ring is in a chair conformation. There is a large discrepancy around the bond angles of the piperazine N atoms. The geometry around the S atom is distorted tetrahedral

10-(2-bromo-4,5-dimethoxybenzyl)-7-chloro-5-cyclopropyl-9-methyl-5,10-dihydro-4,5,6,10-tetraazadibenzo[a,d]cyclohepten-11-one

In the crystal structure of the title compound, C\sb 24H\sb 22BrClN\sb 4O\sb 3, there are C—-H⋅sO and C—-H⋅sBr intermolecular hydrogen bonds, and also C—-H⋅sO, C—-H⋅sBr and C—-H⋅sN intramolecular hydrogen bonds

7-Chloro-5-cyclopropyl-9-methyl-5H-4,5,6,10-tetraazadibenzo[a,d]cyclohepten-11(10H)-one

In the title compound, C15H13ClN4O, which is a chloro derivative of the drug Nevirapine, the diazepine ring is in a twisted boat conformation. The pyridine rings fused to the diazepine fragment form a dihedral angle of 58.44&amp;#8197;(10)&amp;#176; and the molecule adopts a butterfly shape. The molecules are joined via N&amp;#8212;H...N hydrogen bonding into polymeric chains down the b axis. All weaker C&amp;#8212;H...O interactions involve the carbonyl O atom as acceptor

Decarboxylative Annulation of α‑Amino Acids with β‑Ketoaldehydes

Indolizidine and quinolizidine derivatives are readily assembled from l-proline or (±)-pipecolic acid and β-ketoaldehydes via a decarboxylative annulation process. These reactions are promoted by acetic acid and involve azomethine ylides as reactive intermediates

Synthesis and antimicrobial studies of novel 1-benzhydryl-piperazine sulfonamide and carboxamide derivatives

A series of novel substituted 1-benzhydryl-piperazine sulfonamide 8(a–f) and benzamides 9(a–h) were synthesized and their antimicrobial activities evaluated in vitro by paper disc diffusion and micro dilution method against standard strains of Gram-positive (Staphylococcus aureus ATCC 25953, Staphylococcus epidermis 25212, Bacillus cereus 11778, Bacillus substilis 6051) and Gram-negative (Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 2853, Proteus vulgaris ATCC 2853 and Salmonella typhi ATCC 9484) bacteria. Among the synthesized new compounds 8d, 8e, 9c, 9e, 9f and 9 h showed potent antimicrobial activities compared to the standard drug streptomycin

Synthesis and biological evaluation of novel 1-(4-methoxyphenethyl)-1H-benzimidazole-5-carboxylic acid derivatives and their precursors as antileukemic agents

We report here the synthesis and preliminary evaluation of novel 1-(4-methoxyphenethyl)-1H-benzimidazole-5-carboxylic acid derivatives 6(a-k) and their precursors 5(a-k) as potential chemotherapeutic agents. In each case, the structures of the compounds were determined by FTIR, H-1 NMR and mass spectroscopy. Among the synthesized molecules, methyl 1-(4-methoxyphenethyl)-2-(4-fluoro-3-nitrophenyl)-1H-benzimidazole-5-car boxylate (5a) induced maximum cell death in leukemic cells with an IC50 value of 3 mu M. Using FACS analysis we show that the compound 5a induces S/G2 cell cycle arrest, which was further supported by the observed down regulation of CDK2, Cyclin B1 and PCNA. The observed downregulation of proapoptotic proteins, upregulation of antiapoptotic proteins, cleavage of PARP and elevated levels of DNA strand breaks indicated the activation of apoptosis by 5a. These results suggest that 5a could be a potent anti-leukemic agent. (C) 2009 Elsevier Ltd. All rights reserved

Synthesis and in vitro antiproliferative activity against human cancer cell lines of novel 5-(4-methyl-benzylidene)-thiazolidine-2,4-diones

A series of novel 5-(4-methyl-benzylidene)-thiazolidine-2,4-dione derivatives 6 (a–d) and 7 (a–g) were synthesized with different substituted aromatic sulfonyl chlorides (R–SO2–Cl) and alkyl halides (R–X) and were characterized by 1H NMR, LC/MS, FTIR and elemental analyses. All the compounds synthesised were evaluated for their cell antiproliferation activity by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. The antiproliferative effects of the synthesised compounds were tested against viable human skin fibroblast cell line and carcinoma cell lines namely HeLa cells, HT-29 cells, MCF-7 cells, HepG-2 cells by adopting positive and negative control. The importance of the nitro group on thiazolidinone moiety was confirmed and it was concluded that the fourth position of the substituted aryl ring plays a dominant role and was responsible for the antiproliferative activity. Among the synthesized compounds only 6a, 7e and 7g have potent antiproliferative activity on all the carcinoma cell lines tested

Effect of novel N-arylurea- substituted 3-morpholino arecoline derivatives as muscarinic receptor 1 agonists in Alzheimer's dementia models

The cholinergic hypothesis of Alzheimer's disease has spurred the development of numerous compounds aimed at increasing central cholinergic neurotransmission. Symptomatic treatment can be given by cholinomimetics with the pharmacological profile of muscarinic receptor 1 (M1 receptor) agonist and/or acetylcholineesterase (AChE) inhibitors. Novel bioactive six-membered N-arylurea-substituted 3-morpholino arecoline derivatives were synthesized by N-benzyl aminoethanol coupling with alpha-bromoacetylpyridine followed by reduction and cyclization. Five of the derivatives showed high M1 receptor binding affinity in vitro and elicited beneficial effects in in vivo memory and learning models in rats