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91.
Hamideh Ahadi Mohammad Shokrzadeh Zahra Hosseini-khah Nasrin Ghassemi Barghi Majid Ghasemian Saeed Emami 《Journal of biochemical and molecular toxicology》2023,37(6):e23334
Levofloxacin, the optical S-(-) isomer of ofloxacin, is a broad-spectrum antibacterial agent widely used to control various infections caused by Gram-positive and Gram-negative bacteria. While the COOH group is necessary for antibacterial activity, its modification can offer anticancer activity to the fluoroquinolone framework. Therefore, several levofloxacin carboxamides 11a-j and 12 containing 5-substituted-1,3,4-thiadiazole residue were synthesized and screened in vitro for their anticancer activity. The in vitro MTT viability assay revealed that the most compounds had significant activity against cancer cells MCF-7, A549, and SKOV3. In particular, the 3-chloro- and 4-fluoro- benzyl derivatives ( 11b and 11h ), with IC50 values of 1.69–4.76 μM were as potent as or better than doxorubicin. It should be noted that the mother quinolone levofloxacin showed no activity on the tested cancer cell lines. The SAR analysis demonstrated that the 3-chloro or 4-fluoro substituent on the S-benzyl moiety had positive effect on the activity. Further in vitro evaluations of the most promising compounds 11b and 11h by flow cytometric analysis and comet test revealed the ability of compounds in the induction of apoptosis and blockage of the cell proliferation at the G1-phase by nuclear fragmentation and DNA degradation in cancer cells. The obtained results demonstrated that the alteration of 6-COOH functional group in the levofloxacin structure and conjugation with a proper heterocyclic pharmacophore is a good strategy to obtain new anticancer agents. 相似文献
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Pugia MJ Jortani SA Basu M Sommer R Kuo HH Murphy S Williamson D Vranish J Boyle PJ Budzinski D Valdes R Basu SC 《Glycoconjugate journal》2007,24(1):5-15
Urinary trypsin inhibitors (uTi) suppress serine proteases during inflammation. After liberation from proinhibitors (P-alpha-I
and I-alpha-I) by the white blood cell (WBC) response, uTi readily pass through the kidneys into urine. A key uTi, bikunin,
is attached to O-linked and N-linked glycoconjugates. Recently, uTi inhibitors, called uristatins, were found to lack the
O-linked glycoconjugates. Monoclonal antibodies were produced using purified uristatin and screened for binding differences
to uristatin, bikunin, P-α-I, and I-α-I. Antibody-binding patterns were characterized using immunoaffinity binding onto protein-chip
surfaces and analysis by Surface Enhanced Laser Desorption/Ionization mass spectrometry (SELDI), using specimens from patients
and from purified uTi standards. Antibodies were developed and used in an enzyme-linked immunosorbent assay (ELISA) method
for uTi measurement in urine and plasma specimens. ELISA was performed on specimens from normal, presumed healthy, controls
and from patients who had been screened for inflammation using a high sensitivity C-reactive protein (CRP) test and a complete
blood count (CBC). Polyclonal antibody against uTi showed cross-reactivity with the Tamm–Horsfall protein (THP) and with proinhibitors.
Screening of anti-uTi monoclonal antibodies (Mab) revealed antibodies that did not cross-react with either of the above, thus
providing a tool to measure both uristatin and bikunin in urine with Mab 3G5 and in plasma with Mab 5D11. The monoclonal antibody
5D11 cross-reacts with specific N-linked glycoconjugates of uristatin present in plasma. In ca 96% of healthy adults, uTi
were present at <12 mg/l in urine and <4 mg/l in plasma. We also found that patients with an inflammation and a CRP of >2.0 mg/l
had higher urinary concentrations of uTi than the control population in every subject. Free uristatin and bikunin pass readily
into urine and are primarily bound to heavy chains that constitute the proinhibitor form in plasma. 相似文献
94.
Aghamohamadi Elham Asri † Nastaran Odak Aylin Rostami-Nejad Mohammad Chaleshi Vahid Hajinabi Yasaman Eslami Maryam Mohammadian Haftcheshmeh Saeed Gholam-Mostafaei Fahimeh Sadat Asadzadeh-Aghdaei Hamid Masotti Andrea Zali Mohammad Reza 《Molecular biology reports》2022,49(7):6085-6091
Molecular Biology Reports - Celiac disease (CeD) and inflammatory bowel disease (IBD) are accompanied by impaired immune responses. To study the immune regulation of these diseases, we evaluated... 相似文献
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Mohammad Charkhpour Hamed Ghavimi Saeed Ghanbarzadeh Bahman Yousefi Arash Khorrami Mehran Mesgari Kambiz Hassanzadeh 《Journal of biomedical science》2015,22(1)
Background
Morphine-induced tolerance is associated with the spinal neuroinflammation. The aim of this study was to explore the effects of oral administration of the pioglitazone, the peroxisome proliferator activated receptor gamma (PPAR-γ) agonist, on the morphine-induced neuroinflammation in the lumbar region of the male Wistar rat spinal cord.Results
Co-administration of the pioglitazone with morphine not only attenuated morphine-induced tolerance, but also prevented the up-regulation of pro-inflammatory cytokines (tumor necrosis factor alpha, interleukin-1beta, and interleukin 6) and nuclear factor-kappa B activity. Administration of the GW-9662 antagonized the above mentioned effects of the pioglitazone.Conclusions
It is concluded that oral administration of the pioglitazone attenuates morphine-induced tolerance and the neuroinflammation in the lumbar region of the rat spinal cord. This action of the pioglitazone may be, at least in part, due to an interaction with the spinal pro-inflammatory cytokine expression and the nuclear factor-kappa B activity. 相似文献100.
Ching-Hung Tseng Pei-Wen Chiang Hung-Chun Lai Fuh-Kwo Shiah Ting-Chang Hsu Yi-Lung Chen Liang-Saw Wen Chun-Mao Tseng Wung-Yang Shieh Isaam Saeed Saman Halgamuge Sen-Lin Tang 《BMC genomics》2015,16(1)