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Polysubstituted pyrazoles (5)(a-l), pyrazolines (7)(a-c), (8)(a-c) and pyrazolotriazine (10) derivatives of diazepam were synthesized. The structures of hitherto unknown compounds were established by analytical and spectral methods. Some of these compounds were screened to test their antibacterial activity against gram-positive (B. subtilis) and gram-negative (P. aeruginosa). All compounds showed potent activity against these bacteria. 相似文献
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Human papillomavirus infection in Egyptian esophageal carcinoma: correlation with p53, p21, mdm2, C-erbB2 and impact on survival 总被引:1,自引:0,他引:1
The etiological role of human papillomavirus (HPV) in esophageal carcinoma (EC) in relation to p53, mdm2, p21(waf), c-erbB2 and the overall survival (OS) rate was investigated. Tumor and normal tissues from 50 EC were evaluated by polymerase chain reaction and InnoLiPA for HPV. Single strand conformation polymorphism/sequencing were used to detect p53 gene mutations. Immunohistochemistry was performed to determine p53, mdm2, p21(waf)and c-erbB2 expression. Human papillomavirus was detected in 54% of tumors and in 24% of normal tissues. p53, mdm2 and c-erbB2 overexpression was detected in 68%, 70% and 60% of tumors and in 14%, 16% and 10% of normal samples, whereas loss of p21(waf) was evident in 64% of tumors. p53 mutations were detected in 20% of cases. Exon 8 and 5 showed the highest mutation rate (40% each), followed by exons 6 and 7 (10% each). There was a significant correlation between HPV and p53, mdm2, c-erbB2 overexpression. The OS was significantly associated with overexpression of p53 and loss of p21(waf). Human papillomavirus infection is frequent in Egyptian EC. Both p53-dependent and p53-independent pathways seem to be involved in HPV-associated EC. mdm2 and c-erbB2 are possible targets for HPV in the p53-independent pathway. However, only advanced stage and aberrant expression of p53 and p21(waf) are independent prognostic markers. 相似文献
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Ameyaw MM Tayeb M Thornton N Folayan G Tariq M Mobarek A Evans DA Ofori-Adjei D McLead HL 《Journal of human genetics》2002,47(4):172-175
HER-2, a protooncogene located on chromosome 17q21, encodes a transmembrane glycoprotein (p185) with tyrosine kinase activity.
Alterations of the HER-2 gene have been implicated in the carcinogenesis and prognosis of breast cancer and other solid tumors. It is also a cancer-therapeutic
target for antibody-based therapy against the HER-2 protein. A single-nucleotide polymorphism (SNP) at codon 655, resulting in a G-to-A transition (Ile655Val) in the transmembrane
domain-coding region of this gene has been associated with an increased risk of breast cancer, particularly among younger
women. To understand the importance of this finding throughout the world, we evaluated this polymorphism in Ghanaian, Kenyan,
Sudanese, Caucasian, African–American, Saudi, and Filipino subjects using a polymerase chain reaction-restriction fragment
length polymorphism assay. The frequency of the Val allele, which is associated with increased breast cancer risk, was highly
variable between populations (0%–24%). Continental African populations had a lower frequency of the Val allele than did Saudi,
Chinese, Filipino, Caucasian, and African–American subjects. The data suggest that this SNP has variable frequency in different
ethnic groups. The findings in this study correspond with the lower incidence and lower risk of breast cancer in African women
compared with Caucasian and African–American women.
Received: December 13, 2001 / Accepted: January 16, 2002 相似文献
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Ahmed E. Ahmed Ting F. Hsu Rokea A. el-Azhary Helmy Moawad Herbert H. Farrish Jr. John Costanzi 《Cancer chemotherapy and pharmacology》1982,8(3):271-276
Summary The kinetics of uptake and elimination, covalent binding, and macromolecular interactions of 14[C-ring] melphalan was studied after a single oral dose (20 mg/kg, 0.1 mCi/kg) in normal rats. Peak radioactivity level in tissues was observed at 2–4 h after administration. Uptake of label in most tissues was rapid, with a t1/2 of less than 1 h. Elimination was biphasic. Tissues of the gastrointestinal tract showed the most rapid rates of elimination, with t1/2 of 13, 24, 18, and 19 h for stomach, duodenum, and small and large intestines, respectively. Bone marrow also showed a fast rate of elimination of radioactivity, with a t1/2 of 30 h. Tissues with the slowest rates of elimination were skin, eye, spleen, pancreas, and lung, with t1/2 of 333, 241, 149, 122, and 109 h, respectively. Covalent binding studies showed that melphalan, or its metabolites, bound irreversibly to all tissue macromolecular fractions. The percentage of covalently bound radioactivity increased with time in all tissues except kidney and eye, reaching up to 70%–80% of the total radioactivity remaining at 72 h. Elimination of covalently bound radioactivity was slower in the DNA fractions of the tissues of the gastrointestinal tract and heart compared with the elimination rate from lipid, protein, or RNA fractions. Slow elimination rates of 14[C-ring] melphalan equivalents from the protein fraction were observed in the skin, eye, and brain. Accumulation, rather than elimination, of radioactivity in this fraction was most prominent in the pancreas. In the bone marrow accumulation of radioactivity was observed in the lipid fraction.Abbreviations used in this paper are L-Pam
Melphalan, l-phenylalanine mustard 4-bis (2-chloroethyl) amino-1-phenylalanine
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l-DOH
4-bis (2-hydroxyethyl) amino-1-phenylalanine
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l-MOH
4-2 hydroxyethyl 2 chloroethyl amino-1-phenylalanine
- HPLC
high-pressure liquid chromatography
- TCA
trichloroacetic acid
- AUC
area under the curve
- GIT
gastrointestinal tract 相似文献
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Abeer M Shaaban Valerie Speirs 《Clinical cancer research》2005,11(22):8222; author reply 8222-8222; author reply 8223
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Pfeiffer syndrome: oral healthcare management and description of new dental findings in a craniosynostosis
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Yazan Hassona PhD FFDRCSI DDS Abeer Al‐Hadidi PhD MSc DDS Thaer Abu Ghlassi DDS Hanin El Dali DDS; 《Special care in dentistry》2017,37(5):258-262
Pfeiffer syndrome is a rare fibroblast growth factor receptor‐related craniosynostosis with variable clinical presentations. We describe new dental findings of hypodontia, microdontia, dilacerations, and radicular dentin dysplasia in a 19‐year‐old girl, and discuss the oral health management. 相似文献