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21.
Arjun Basnet Pritam Thapa Radha Karki Hoyoung Choi Jae Hun Choi Minho Yun Byeong-Seon Jeong Yurngdong Jahng Younghwa Na Won-Jea Cho Youngjoo Kwon Chong-Soon Lee Eung-Seok Lee 《Bioorganic & medicinal chemistry letters》2010,20(1):42-47
For the development of novel antitumor agents, 2,6-dithienyl-4-furyl pyridine derivatives were prepared and evaluated for their topoisomerase I and II inhibitory activity as well as cytotoxicity against several human cancer cell lines. Among the 21 prepared compounds, compound 24 exhibited strong topoisomerase I inhibitory activity. In addition, a docking study with topoisomerase I and compound 24 was performed. 相似文献
22.
Ravindra N. Kharwar Surendra K. Gond Anuj Kumar Ashish Mishra 《World journal of microbiology & biotechnology》2010,26(11):1941-1948
Eucalyptus citriodora Hook, is frequently cultivated tree in India for its wood and medicinal usages. The endophytic and epiphytic fungi were estimated
from healthy leaves of E. citriodora growing in the premise of Banaras Hindu University, Varanasi, India. A total of 33 fungal species were isolated from leaf
segments. Of 33 taxa, 20 were recorded as endophytes, while 22 as epiphytes. Nine, out of 33 species were found to be common
in leaf tissues and surfaces (Alternaria alternata, Aspergillus fumigatus, A. terreus, Cladosporium cladosporioides, Drechslera rostrata, Humicola grisea, Nigrospora oryzae, Penicillium
cristata, and Pestalotia sp.). Out of 478 fungal isolates, 279 were epiphytic while only 199 were endophytic. Most isolates were anamorphic filamentous
fungi which often don’t produce sexual spores. The Sorensen’s index of similarity between endophytes and epiphytes (leaf surface
colonizers) was found to be at 0.300. Diversity index of fungal species was higher in endophytes than epiphytes. The frequency
of colonization differs greatly in both myco-populations. Cladosporium cladosporioides (26%) was dominant species on leaf surfaces while Botrytis cinerea (10.5%) was dominant in leaf tissues. Out of 16 endophytic isolates evaluated for antagonistic test, 8 (50%) gave the antagonistic
activity against variety of fungi representing pathogens to both humans and plants. 相似文献
23.
Since the initial discovery of cytoplasmic dynein, it has become apparent that this microtubule-based motor is involved in several cellular functions including cell division and intracellular transport. Another multisubunit complex, dynactin, may be required for most, if not all, cytoplasmic dynein-driven activities and may provide clues to dynein's functional diversity. Recent genetic and biochemical findings have illuminated the cellular roles of dynein and dynactin and provided insight into the functional mechanism of this complex motor. 相似文献
24.
25.
Bansal SK Layloff T Bush ED Hamilton M Hankinson EA Landy JS Lowes S Nasr MM St Jean PA Shah VP 《AAPS PharmSciTech》2004,5(1):151-158
The purpose of the use of analytical instruments is to generate reliable data. Instrument qualification helps fulfill this
purpose. No authoritative guide exists that considers the risk of instrument failure and combines that risk with users' scientific
knowledge and ability to use the instrument to deliver reliable and consistent data. In the absence of such a guide, the qualification
of analytical instruments has become a subjective and often fruitless document-generating exercise.
Taking its cue from the new FDA initiative, “Pharmaceutical GMP's for the 21st Century,” an efficient, science- and risk-based
process for AIQ was discussed at a workshop on analytical instrument qualification. This report represents the distillate
of deliberations on the complicated issues associated with the various stages of analytical instrument qualification. It emphasizes
AIQ's place in the overall process of obtaining quality reliable data from analytical instruments and offers an efficient
process for its performance, one that focuses on scientific value rather than on producing documents. Implementing such a
process should remove ambiguous interpretations by various groups. 相似文献
26.
27.
Pravin L. Kotian Raman Krishnan Scott Rowland Yahya El-Kattan Surendra K. Saini Ramanda Upshaw Shanta Bantia Shane Arnold Y. Sudhakar Babu Pooran Chand 《Bioorganic & medicinal chemistry》2009,17(11):3934-3958
Factor VIIa (FVIIa), a serine protease enzyme, coupled with tissue factor (TF) plays an important role in a number of thrombosis-related disorders. Inhibition of TF·FVIIa occurs early in the coagulation cascade and might provide some safety advantages over other related enzymes. We report here a novel series of substituted biphenyl derivatives that are highly potent and selective TF·FVIIa inhibitors. Parallel synthesis coupled with structure-based drug design allowed us to explore the S2 pocket of the enzyme active site. A number of compounds with IC50 value of <10 nM were synthesized. The X-ray crystal structures of some of these compounds complexed with TF·FVIIa were determined and results were applied to design the next round of inhibitors. All the potent inhibitors were tested for inhibition against a panel of related enzymes and selectivity of 17,600 over thrombin, 450 over trypsin, 685 over FXa, and 76 over plasmin was achieved. Two groups, vinyl 36b and 2-furan 36ab, were identified as the optimum binding substituents on the phenyl ring in the S2 pocket. Compounds with these two substituents are the most potent compounds in this series with good selectivity over related serine proteases. These compounds will be further explored for structure–activity relationship. 相似文献
28.
Govinda Rizal Shanta Karki Richard Garcia Nikki Larazo Michael Alcasid William Paul Quick 《PloS one》2015,10(4)
An efficient method for crossing green foxtail (Setaria viridis) is currently lacking. S. viridis is considered to be the new model plant for the study of C4 system in monocots and so an effective crossing protocol is urgently needed. S. viridis is a small grass with C4-NADP (ME) type of photosynthesis and has the advantage of having small genome of about 515 Mb, small plant stature, short life cycle, multiple tillers, and profuse seed set, and hence is an ideal model species for research. The objectives of this project were to develop efficient methods of emasculation and pollination, and to speed up generation advancement. We assessed the response of S. viridis flowers to hot water treatment (48°C) and to different concentrations of gibberellic acid, abscisic acid, maleic hydrazide (MH), and kinetin. We found that 500 μM of MH was effective in the emasculation of S. viridis, whilst still retaining the receptivity of the stigma to pollination. We also report effective ways to accelerate the breeding cycle of S. viridis for research through the germination of mature as well as immature seeds in optimized culture media. We believe these findings will be of great interest to researchers using Setaria. 相似文献
29.
Nischal Karki Satyam Vergish Brian D. Zoltowski 《Protein science : a publication of the Protein Society》2021,30(8):1521
Cryptochromes (CRYs) function as blue light photoreceptors in diverse physiological processes in nearly all kingdoms of life. Over the past several decades, they have emerged as the most likely candidates for light‐dependent magnetoreception in animals, however, a long history of conflicts between in vitro photochemistry and in vivo behavioral data complicate validation of CRYs as a magnetosensor. In this review, we highlight the origins of conflicts regarding CRY photochemistry and signal transduction, and identify recent data that provides clarity on potential mechanisms of signal transduction in magnetoreception. The review primarily focuses on examining differences in photochemistry and signal transduction in plant and animal CRYs, and identifies potential modes of convergent evolution within these independent lineages that may identify conserved signaling pathways. 相似文献
30.