The reconstruction of funnel chest deformity with the reversed transplantation of sternum-costicartilage flap carried by the abdominal rectus pedicle / 中华整形外科杂志

<p><b>OBJECTIVE</b>To investigate the reconstructive operative procedures of funnel chest with "sternum-costicartilage" flap carried by the abdominal rectus pedicle.</p><p><b>METHODS</b>(1) In accordance with the lesioned area of funnel-like depressed deformity of anterior thoracic wall, a perpendicular median incision was designed and made; (2) The "sternum-costicartilage" flap carrying the abdominal rectus pedicle was used and reversed and transplanted to reconstruct severe funnel chest deformity.</p><p><b>RESULTS</b>The procedure was used in 7 cases from 1999 to 2005. The results of surgery were satisfactory. There were no recurrence after operation.</p><p><b>CONCLUSIONS</b>The procedure reported here is rather safe, solid and sound with good therapeutic results, and is of great value in clinical practice.</p>

Three dimensional quantitative structure-activity relationship of a series of benzocylohepatpyridine farnesyltransferase inhibitors / 药学学报

<p><b>AIM</b>To build a three dimensional structure model that correlates the biological activities and the structures of a series of 1-(8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta-[1,2-]pyridin-11-yl) piperazines farnesyl protein transferase (FPTase) inhibitors.</p><p><b>METHODS AND RESULTS</b>Mutation in the ras oncogene takes place in many human cancers, involving 30%-50% of colon and 90% of pancreatic cancer. Ras proteins function as central switches for signals given by growth factors that direct cell growth and cell differentiation. The dependence of the transforming activity of Ras on the farnesylation has led to intense search for FPTase inhibitors that may have therapeutic pontetial as anticancer agents. This paper is to build a three dimensional structural model that correlates the biological activities and the structures of a series of FPTase inhibitors. The investigated sixty-nine inhibitors contain six types of structures, the optimal conformations of which were studied using system search. A three dimensional quantitative structure-activity relationship (3D-QSAR) model was constructed using the method of comparative molecular field analysis (CoMFA). The resulting cross-validation R2 is 0.581, non-cross-validation R2 0.968, SE 0.148, F 198.7. The predicted activities of 10 inhibitors using this 3D-QSAR model are comparable to the experimental activities, indicating that the 3D-QSAR model has ability to predict activities of new inhibitors and offers an approach to design new FPTase inhibitors.</p><p><b>CONCLUSION</b>The information of CoMFA model offers an approach to designing new FPTase inhibitors.</p>

7-imidazolylalkanamido-1-carboxylalkylbenzo-diazepine, a novel series of farnesyltransferase inhibitors / 药学学报

<p><b>AIM</b>Design, synthesis and evaluation of a series of 7-imidazolylalkanamido-1-carboxylalkylbenzodiazepine farnesyltransferase (FTase) inhibitors.</p><p><b>METHODS AND RESULTS</b>Coupling of imidazolylalkylcarboxylic acids and 1-substituted 7-aminobenzodiazepines (5a-5c) yielded 10 new compounds (6-12, 16-18) which were biologically tested against FTase using scintillation proximity assay method.</p><p><b>CONCLUSION</b>Five target compounds were found to be potential farnesyltransferase inhibitors.</p>