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101.
Runjhun Tandon Vijay Luxami Harsovin Kaur Nitin Tandon Kamaldeep Paul 《Chemical record (New York, N.Y.)》2017,17(10):956-993
The poor pharmacokinetics, side effects and particularly the rapid emergence of drug resistance compromise the efficiency of clinically used anticancer drugs. Therefore, the discovery of novel and effective drugs is still an extremely primary mission. Naphthalimide family is one of the highly active anticancer drug based upon effective intercalator with DNA. In this article, we review the discovery and development of 1,8‐naphthalimide moiety, and, especially, pay much attention to the structural modifications and structure activity relationships. The review demonstrates how modulation of the moiety affecting naphthalimide compound for DNA binding that is achieved to afford a profile of antitumor activity. The DNA binding of imide and ring substitution at naphthalimide, bisnaphthalimide, naphthalimide‐metal complexes is achieved by molecular recognition through intercalation mode. Thus, this synthetic/natural small molecule can act as a drug when activation or inhibition of DNA function, is required to cure or control the cancer disease. The present study is a review of the advances in 1,8‐naphthalimide‐related research, with a focus on how such derivatives are intercalated into DNA for their anticancer activities. 相似文献
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103.
The major histocompatibility complex (MHC) harbours genes that have a primary function of regulating immune responsiveness. Our data on the distribution patterns of molecular subtypes of HLA class I and II extended haplotypes in India suggest that: (1) Asian Indians have extreme diversity in the MHC region, with several novel and unique alleles and disease-associated MHC haplotypes (e.g. the autoimmune-favouring A26-B8-DR3 haplotype); (2) there have been selective environmental and microbial pressures in India that directed either the generation of novel alleles through founder effect or the expansion of other alleles due to geophysical or socio-economic barriers, and (3) Asian Indians have a unique repertoire of peptide-presenting molecules to deal with pathogen-derived autoreactive antigens. This level of polymorphism concentrated within the MHC presents a formidable obstacle to the development of peptide-based vaccines, e.g. for AIDS. Further, studies conducted by us and others have provided a genetic basis for the possible predisposition and fast progression of HIV infections in the Indian population. Since there is selective predominance of different HLA alleles and haplotypes in different populations, a dedicated global screening effort is required to develop MHC-based vaccines against infectious diseases. 相似文献
104.
Kundan Tayade Amanpreet Kaur Sandesh Tetgure G. Krishana Chaitanya Narinder Singh Anil Kuwar 《Analytica chimica acta》2014
The (13E,19E)-N1′,N3′-bis[4-(diethylamino)-2-hydroxybenzylidene]malonohydrazide (L) has been developed for the detection of Th4+ ions using dual channel signalling system. The UV–vis absorbance and fluorescence spectroscopic data revealed the formation of L–Th4+ complex in 1:1 equilibrium. The density functional theory (DFT) also confirms the optimum binding cavity for the recognition of metal ion. The binding constant computed from different mathematical models for an assembly of L–Th4+. The detection limit of L for Th4+ recognition is to a concentration down to 0.1 μM (0.023 μg g−1). The present sensing system is also successfully applied for the detection of Th4+ ion present in soil near nuclear atomic plants. 相似文献
105.
Expedient Protocols for the Installation of 1,5‐Benzoazepino‐Based Privileged Templates on the 2‐Position of 1,4‐Benzodiazepine Through a Phenoxyl Spacer
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An efficient novel strategy for the hetero‐annulation of 2‐chloro‐1,4‐benzodiazepine ring, substituted on its 5‐position with a carboxamido group ( 5 ), has been developed to allow the incorporation of 1,5‐benzodiazepine, 1,5‐benzothiazepine, and 1,5‐benzoxazepine ( 8 , 9 , 10 , 11 , 12 , 13 ) rings through their dimethylaminomethylene ketone intermediate ( 7 ). 相似文献
106.
Navjeet Kaur 《合成通讯》2014,44(22):3229-3247
The development of new strategies for synthesis of five-membered O,N,N-heterocycles has remained a highly attractive but challenging proposition. An overview of the application of microwave irradiation in oxygen and two nitrogen atoms containing five-membered heterocyclic compounds synthesis is presented, focusing on the developments in the past 5–10 years. This contribution covers the literature concerning the total synthesis of five-membered O,N,N-heterocycles. 相似文献
107.
The development of new strategies for synthesis of six-membered O-heterocycles has remained a highly attractive but challenging proposition. An overview of the application of microwave irradiation in oxygen-containing six-membered heterocyclic compounds synthesis is presented, focusing on the developments in the past 5–10 years. This contribution covers the literature concerning the total synthesis of six membered O-heterocycles. 相似文献
108.
Solid-phase organic synthesis is a rapidly expanding area of synthetic chemistry that is being widely exploited in the search for new medicinally important compounds using combinatorial techniques. In recent decades, a large number of reports related to solid-phase synthesis of heterocycles have appeared because of the wide variety of their biological activity. In this review, we report the important role of solid-phase synthesis in the synthesis of nitrogen containing six-membered ring heterocycles. 相似文献
109.
110.
Fernandez FM Hostetler D Powell K Kaur H Green MD Mildenhall DC Newton PN 《The Analyst》2011,136(15):3073-3082
Throughout history, poor quality medicines have been a persistent problem, with periodical crises in the supply of antimicrobials, such as fake cinchona bark in the 1600s and fake quinine in the 1800s. Regrettably, this problem seems to have grown in the last decade, especially afflicting unsuspecting patients and those seeking medicines via on-line pharmacies. Here we discuss some of the challenges related to the fight against poor quality drugs, and counterfeits in particular, with an emphasis on the analytical tools available, their relative performance, and the necessary workflows needed for distinguishing between genuine, substandard, degraded and counterfeit medicines. 相似文献