• Archives of Pharmacal Research
• /
• v.20 no.6
• /
• pp.610-619
• /
• 1997

Some new 9H-thioxanthen-9-one incorporated into heterocyclic systems such as pyridone 8, pyrazoline 9, pyranone 11, iminopyrane 12, furopyrimidine 17, imidazothiazole 19, thiazole 21, triazine 24 and other related compounds through a para imminophenyl grouping at position-1 of the thioxanthenone ring were synthesized and tested as antitumor agents against L1210 leukemia in mice. Some of the new compounds showed considerable antitumor activity.

• Tuberculosis and Respiratory Diseases
• /
• v.42 no.3
• /
• pp.302-313
• /
• 1995

Background: Tumor necrosis factor(TNF) showed antitumor cytolytic effects on sensitive tumor cells in numerous in vivo and in vitro studies. But it could not be administered systemically to human because of severe systemic adverse effects at effective concentrations against tumor cells. Many studies showed that a high concentrations of TNF in the local milieu may evoke in vivo TNF-responsive mechanisms sufficient to suppress tumor growth. Recently developed technique of TNF gene transfer to tumor cells using retrovirus vector could be a good candidate for local TNF administration. TNF is also known to synergistically enhance in vitro cytotoxicity of chemotherapeutic drugs targeted to DNA topoisomerase II against TNF-sensitive tumor cell lines. In this study the in vitro chemosensitivity against DNA topoisomerase II targeted chemotherapeutic drugs was evaluated using some respiratory cancer cell lines to which TNF gene had been transferred. Method: NCI-H2058, a human mesothelioma cell line, A549, a human lung adenocarcinoma cell line and WEHI 164 cell line, a murine fibrosarcoma cell line were treated with etoposide and doxorubicin, which are typical topoisomerase II - targeted chemotherapeutic agents, at different concentration. The resultant cytotoxicity was measured by MIT assay. Then the cytotoxicity of the same chemotherapeutic agents was measured after TNF-$\alpha$ gene-transfer and the two results were compared. Results: The cytotoxicity was not increased significantly in WEHI164 cell line and A549 cell line but statistically significant increase was observed in H2058 cell line when TNF-$\alpha$ gene was transferred(p<0.05). Conclusion: These findings show that TNF-$\alpha$ gene transfer to respiratory cancer cell lines results in variable effects on chemosensitivity against topoisomerase II inhibitor among different cell lines in vitro and can be additively cytotoxic in certain selective tumor cell lines.

• Archives of Pharmacal Research
• /
• v.12 no.2
• /
• pp.135-137
• /
• 1989

A convenient route is reported for the synthesis of certain series of 4H-thieno[2,3-b][1]benzothiopyran-4-ones, carrying various substituents at position 2 such as arylazomethines (7,8), thiazolidin-4-ones (9-13), ${\alpha},\;{\beta}-unsaturated$ ketones (16,17), 2-pyridones (19-23), tetrahydrothiophen-4-ones (24,28), and nitroalkenes (29,30), as potential schistosomicidal or antihistaminic agents.

• BMB Reports
• /
• v.36 no.3
• /
• pp.269-274
• /
• 2003

In the fight against cancer, novel chemotherapeutic agents are constantly being sought to complement existing drugs. Various studies have presented evidence that the apoptosis that is induced by these anticancer agents is implicated in tumor regression, and Bcl-2 family genes play a part in apoptosis following treatment with various stimuli. Here, we present data that a styrylpyrone derivative (SPD) that is extracted from the plant Goniothalamus sp. showed cytotoxic effects on the human breast cancer cell line MCF-7. SPD significantly increased apoptosis in MCF-7 cells, as visualized by phase contrast microscopy and evaluated by the Tdt-mediated dUTP nick end-labeling assay and nuclear morphology. Western blotting and immunostaining revealed up-regulation of the proapoptotic Bax protein expression. SPD, however, did not affect the expression of the anti-apoptotic protein, Bcl-2. These results, therefore, suggest SPD as a potent cytotoxic agent on MCF-7 cells by inducing apoptosis through the modulation of Bax levels.

• Pediatric Gastroenterology, Hepatology & Nutrition
• /
• v.3 no.1
• /
• pp.84-88
• /
• 2000

Secondary peptic ulceration and gastritis have been known to be associated with stress, exogenous agents, drugs or infection. Salicylate (aspirin) ingestion has been known to be associated with increased incidence of gastric ulcer and more frequently as the cause of hemorrhagic gastric erosions and gastritis. Some medications such as tetracyclines and iron preparations have been associated with ulceration of the gastrointestinal tract. Chemotherapeutic agents including cytoxan and methotrexate also have been implicated in the development of mucosal and gastrointestinal ulcers. We have experienced two cases of hemorrhagic gastric ulcers due to creosote ingestion in a 13 month and a 5 year old boys. Creosote is a main component of one of the popular digestives, Jungrohwan in Japan and Korea.

• BMB Reports
• /
• v.29 no.6
• /
• pp.489-492
• /
• 1996

A number of anticancer-chemotherapeutic agents induce cell death through the process of apoptosis. Effects of echinomycin, an anticancer agent on cancer progression, were investigated in P388 murine leukemia cells. First, according to the results of cytotoxicity measurement. $IC_{50}$ of echinomycin was 1.12 nM, a relatively lower value than the other examined anticancer agents, mitomycin-C and etoposide Second, the DNA fragmentation assay for echinomycin-treated cells exhibited that echinomycin was able to induce apoptosis in a shorter period of time and with a lower dose than mitomycin-C or etoposide. The data of DNA fragmentation were quite comparable to those of cytotoxicity measurement. Finally we showed that mitogen-activated protein (MAP) kinase, a key protein in cell mitosis, was translocated into the nucleus from the cytosol after treatment with echinomycin. These findings suggest that a MAP kinase-related process may be involved in apoptosis induced by echinomycin.

• Bulletin of the Korean Chemical Society
• /
• v.28 no.11
• /
• pp.1910-1916
• /
• 2007

Analyzed are recent advances in design of novel boronared conjugates of synthetic and natural porphyrins and chlorins. These compounds showed high efficacy as cytotoxic agents for tumor cells in culture and as phototoxins in photodynamic therapy of tumor xenografts. Thus, boronated porphyrins and chlorins emerge as promising class of anticancer agents with potentially multiple advantages: the chemotherapeutic drugs alone and photo- and radiosensitizers in binary treatments.

• Bulletin of the Korean Chemical Society
• /
• v.28 no.11
• /
• pp.1931-1938
• /
• 2007

Analyzed are recent advances in design of novel boronared conjugates of synthetic and natural porphyrins and chlorins. These compounds showed high efficacy as cytotoxic agents for tumor cells in culture and as phototoxins in photodynamic therapy of tumor xenografts. Thus, boronated porphyrins and chlorins emerge as promising class of anticancer agents with potentially multiple advantages: the chemotherapeutic drugs alone and photo- and radiosensitizers in binary treatments.

• Journal of Digestive Cancer Research
• /
• v.2 no.2
• /
• pp.52-55
• /
• 2014

The incidence of colorectal cancer (CRC) has continuously increased and CRC is a major cause of cancer-related death. Systemic chemotherapy has resulted in a significant improvement in overall survival in metastatic CRC. The development of biologic agents for the treatment of CRC has additionally expanded the options for the treatment. Cetuximab is useful in KRAS wild type tumors in combination with chemotherapy for metastatic disease in both the first and second line settings. It is also used as monotherapy after failure of both irinotecan and oxaliplatin containing regimens. Panitumumab has similar indications, and is primarily used in patients intolerant to cetuximab due to hypersensitivity reactions. Bevacizumab is primarily used as first line and second line therapy in metastatic CRC. However, the optimal way and duration to combine these chemotherapeutic agents are not yet established.

• Asian Pacific Journal of Cancer Prevention
• /
• v.15 no.11
• /
• pp.4623-4627
• /
• 2014

Background: The epidermal growth factor receptor (EGFR) plays a vital role in the activation and inactivation of receptor tyrosine kinases. Mutations in exons 19 and 21 of EGFR are commonly found to be associated with non small cell lung carcinoma and triple negative breast cancer, enhancing sensitivity to EGFR targeting chemotherapeutic agents. Since amplification and prolonged activation of EGFR molecules have been identified in oral squamous cell carcinomas (OSCC), we investigated whether OSCCs carried mutations in exons 19 and 21 of EGFR to their incidence. Materials and Methods: Tumor chromosomal DNA isolated from forty surgically excised oral squamous cell carcinoma tissues was subjected to PCR amplification with intronic primers flanking exons 19 and 21 of the EGFR gene. The PCR amplicons were subsequently subjected to direct sequencing to elucidate the mutation status. Results: Data analysis of the EGFR exon 19 and 21 coding sequences did not show any mutations in the forty OSCC samples that were analyzed. Conclusions: To the best of our knowledge, this is the first study to have investigated the genetic status of exons 19 and 21 of EGFR in Indian OSCCs and identified that mutation in EGFR exon 19 and 21 may not contribute towards their genesis. The absence of mutations also indicates that oral cancerous lesions may not be as sensitive as other cancers to chemotherapeutic agents targeting EGFR.