Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.

A series of N-heterocyclic indolyl glyoxylamides were synthesized and evaluated for in vitro and in vivo anticancer activities. They exhibited a broad spectrum of anticancer activity not only in murine leukemic cancer cells but also in human gastric, breast, and uterus cancer cells as well as their multidrug resistant sublines with a wide range of IC(50) values. They also induced apoptosis and caused DNA fragmentation in human gastric cancer cells. Among the compounds studied, 7 showed the most potent activity of growth inhibition (IC(50) = 17-1711 nM) in several human cancer cells. Given orally, compounds 7 and 13 dose-dependently prolonged the survival of animals inoculated with P388 leukemic cancer cells. N-Heterocyclic indolyl glyoxylamides may be useful as orally active chemotherapeutic agents against cancer and refractory cancerous diseases of multidrug resistance phenotype.

Management of patients with coronary stents in elective thoracic surgery.

PURPOSE: Interruption of oral antiplatelet agents for noncardiac surgery places patients who have received coronary stent implantation at high risk of coronary events, including stent thrombosis. We investigated retrospectively perioperative management for patients with coronary stents undergoing thoracic surgery. METHODS: We investigated 38 patients (age, 38-83 years; 33 men and 5 women) who underwent thoracic surgery (35 lung cancer resections and 3 other procedures) after coronary stent implantation at our hospital between January 2006 and August 2010. Data on implanted stents, perioperative medications, and cardiac and hemorrhagic complications were analyzed. RESULTS: Sirolimus-eluting stents (n = 18) and bare-metal stents (n = 20) were implanted. Regarding oral antiplatelet agents, 21 patients received aspirin, 16 received thienopyridine derivative and aspirin, and 1 received no oral antiplatelet agents. Oral antiplatelet agents were stopped 3-7 days before surgery. Perioperative heparinization was performed in 16 patients. Oral antiplatelet agents were restarted after confirmation of hemostasis and the lack of need for further invasive procedures (median, 4 days after surgery). No major cardiac events including stent thrombosis developed. There were no excessive intraoperative bleeding events related to oral antiplatelet agents or heparin. CONCLUSIONS: In our patients, no coronary events occurred with the short-term stopping of oral antiplatelet agents for thoracic surgery.

Non-surgical closure of post-pneumonectomy empyema with bronchopleural fistula after open window thoracotomy using basic fibroblast growth factor.

Empyema with bronchopleural fistula (BPF) is one of the severest complications following pneumonectomy. Many papers have reported that it is difficult to cure, with a high rate of associated mortality. Closure of the fistula and an appropriate choice of obliteration materials are crucial for successful treatment. However, obliteration is sometimes impractical because of a lack of suitable materials, excessive surgical risk, or lack of patient willingness to undergo the procedure. We report a case of post-pneumonectomy empyema with BPF that was treated by non-surgical closure after open-window thoracotomy (OWT) with the use of basic fibroblast growth factor (bFGF), which was sprayed into the unepithelialized empyema cavity transiting from epidermis and surrounding the fistula. After spraying, the orifice of the OWT was covered by a film dressing. This procedure yielded successful results after two months.