Design, synthesis of novel N, N'-bis-(halogenophenyl)-4- methoxybenzene-1, 3-disulfonamides and evaluation of their anti-platelet aggregation activity / 药学学报

Combining the structural features of picotamide and linotroban, a series of N,N'-bis-(halogenophenyl)-4-methoxybenzene-1, 3-disulfonamides were designed and synthesized on the basic principles of drug design. The structures of target compounds were confirmed by IR, 1H NMR and HR-MS, and the in vitro antiplatelet aggregation activity was evaluated by Born turbidimetric method with adenosine diphosphate (ADP) as the platelet aggregation inducers. The assay results showed that twelve compounds (4b, 4f, 4l, 5b, 5d-5g, 5j, 5k, 5m and 5n) were found to have superior anti-platelet aggregation activities than the positive drug picotamide. The preliminary structure-activity relationship (SAR) has been explored.

Preoperative induction chemotherapy for unresectable stage IIIA non-small-cell lung cancer / 中华肿瘤杂志

<p><b>OBJECTIVE</b>To evaluate the potential reconsideration of curative operative treatment for patients with unresectable stage IIIA (N2) non-small-cell lung cancer (NSCLC).</p><p><b>METHODS</b>From Jan. 1999 to Dec. 2002, 76 patients with unresectable stage IIIA (N2) NSCLC were entered in this study. They had all been proved by chest CT, chest film and fiberobronchoscopy. Twenty-one (27.6%) patients were examined by mediastinoscopy. All the patients received two cycles of chemotherapy with NVB (25 mg/m(2), D1, D5) and carboplatin (300 mg/m(2), D1). All the patients were staged again three weeks after induction chemotherapy. Sixty-four patients who achieved partial response (PR) or complete response (CR) were allowed to undergo surgery. Twelve patients who did not responde to chemotherapy received radiotherapy instead. Of the 64 surgically treated patients, 56 (84.7%) had a complete resection and then received 2 cycles of chemotherapy using the same regime, 8 patients had an incomplete resection and then received radiotherapy for the residual tumor.</p><p><b>RESULTS</b>The median survival for these 76 patients with unresectable stage IIIA (N2) NSCLC treated by either surgery or radiation after induction chemotherapy was 18.6 months with 1-, 2-, 3-year survival rate of 64.2%, 39.4% and 25.6%, respectively. The median survival for the 56 patients with a complete resection was 28.2 months with 1-, 2-, 3-year survival rate of 70.4%, 52.5% and 38.6%, respectively.</p><p><b>CONCLUSION</b>Preoperative induction chemotherapy with NVB plus carboplatin should be seriously considered for the patients with unresectable stage IIIA (N2) NSCLC, It is suggested that, whenever possible, surgery should be taken as the first choice for the patients who show down-staged benefits that complete resection can be attempted.</p>