The Experts below are selected from a list of 321 Experts worldwide ranked by ideXlab platform
Sherif A F Rostom - One of the best experts on this subject based on the ideXlab platform.
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synthesis and in vitro Antitumor evaluation of some indeno 1 2 c pyrazol in es substituted with sulfonamide sulfonylurea thiourea pharmacophores and some derived thiazole ring systems
Bioorganic & Medicinal Chemistry, 2006Co-Authors: Sherif A F RostomAbstract:The synthesis of a series of 3-(4-chlorophenyl)-[1,2-c]pyrazol(in)es substituted with benzenesulfonamide, N1,N3-disubstituted sulfonylurea, sulfonylthiourea pharmacophores, and some derived thiazolidinone and thiazoline ring systems is described. All the newly synthesized target compounds were subjected to the NCI-in vitro disease-oriented Antitumor screening to be evaluated for their Antitumor activity. Eight compounds namely; 2-4, 7, 8, 10, 13, and 16; showed promising broad spectrum Antitumor activity against most of the tested subpanel tumor cell lines (GI50 < 100 microM). Compound 3, 4-(3-(4-chlorophenyl)-4H-indeno[1,2-c]pyrazol- 2-yl)-benzenesulfonamide; although it did not show the highest growth inhibitory value (GI50 (MG-MID) 13.2 microM), it proved to be the most active analog in this study with the highest cytostatic and cytotoxic potentials (TGI and LC50 (MG-MID) concentrations of 33.1 and 66.1 microM, respectively). In general, the oxidized pyrazoles displayed better Antitumor activity than their parent pyrazoline analogs, whereas the benzenesulfonamides and the N1, N3-disubstituted sulfonylureas showed significant better Antitumor spectrum than the sulfonylthioureido and the derived thiazole analogs.
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synthesis and in vitro Antitumor evaluation of some indeno 1 2 c pyrazol in es substituted with sulfonamide sulfonylurea thiourea pharmacophores and some derived thiazole ring systems
Bioorganic & Medicinal Chemistry, 2006Co-Authors: Sherif A F RostomAbstract:Abstract The synthesis of a series of 3-(4-chlorophenyl)-[1,2-c]pyrazol(in)es substituted with benzenesulfonamide, N1,N3-disubstituted sulfonylurea, sulfonylthiourea pharmacophores, and some derived thiazolidinone and thiazoline ring systems is described. All the newly synthesized target compounds were subjected to the NCI-in vitro disease-oriented Antitumor screening to be evaluated for their Antitumor activity. Eight compounds namely; 2–4, 7, 8, 10, 13, and 16; showed promising broad spectrum Antitumor activity against most of the tested subpanel tumor cell lines (GI50
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polysubstituted pyrazoles part 5 synthesis of new 1 4 chlorophenyl 4 hydroxy 1h pyrazole 3 carboxylic acid hydrazide analogs and some derived ring systems a novel class of potential Antitumor and anti hcv agents
European Journal of Medicinal Chemistry, 2003Co-Authors: Sherif A F Rostom, Manal Shalaby, Maha A EldemellawyAbstract:Abstract A novel series of 1-(4-chlorophenyl)-4-hydroxy-1H-pyrazole-3-carboxylic acid hydrazide analogs and some derived 4-substituted-1,2,4-triazolin-3-thiones, 2-substituted-1,3,4-thiadiazole and 2-substituted-1,3,4-oxadiazoles has been synthesized. Ten of the newly synthesized compounds were selected by the National Cancer Institute (NCI)-in vitro-disease oriented Antitumor screening to be evaluated for their Antitumor activity. Seven compounds, namely 7a–c, 9, 11, 13 and 14, exhibited potential and broad spectrum Antitumor activity against most of the tested subpanel tumour cell lines (GI50
Lizeng Cheng - One of the best experts on this subject based on the ideXlab platform.
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Antitumor activity of se containing tea polysaccharides against sarcoma 180 and comparison with regular tea polysaccharides and se yeast
International Journal of Biological Macromolecules, 2018Co-Authors: Lizeng Cheng, Liang Chen, Qiongqiong Yang, Yuanfeng Wang, Xinlin WeiAbstract:Selenium (Se)-containing polysaccharide, a Se-conjugate macromolecule, generally exhibited higher Antitumor activity than its regular polysaccharide. Previously, we extracted Se-containing tea polysaccharides (Se-TPS) from Se-enriched tea, and explored its structure and antioxidant activity. In this study, we investigated Antitumor activity of Se-TPS on sarcoma 180 (S-180), and compared with its regular polysaccharides TPS and dietary supplement Se-yeast. In vitro Antitumor activity of Se-TPS was evaluated by MTT and LDH assays, and the results indicated that Se-TPS can significantly inhibit the proliferation of S-180 in dose-dependent manner (R2=0.97, p<0.0001). In S-180 cancer xenograft model in Kunming mice, Se-TPS oral administration at three doses of 50, 100 and 200mg/kg body weight daily for 13days resulted in significant tumor regression. At the same dose, Se-TPS exhibited significantly higher Antitumor activity than TPS and Se-yeast. Importantly, Se-TPS can significantly increase the spleen and thymus indices of tumor-bearing mice, suggesting the safety and immunomodulatory activity of Se-TPS. Therefore, Se-TPS may be a desirable Antitumor agent for therapeutic and immunomodulatory applications.
Xinlin Wei - One of the best experts on this subject based on the ideXlab platform.
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Antitumor activity of se containing tea polysaccharides against sarcoma 180 and comparison with regular tea polysaccharides and se yeast
International Journal of Biological Macromolecules, 2018Co-Authors: Lizeng Cheng, Liang Chen, Qiongqiong Yang, Yuanfeng Wang, Xinlin WeiAbstract:Selenium (Se)-containing polysaccharide, a Se-conjugate macromolecule, generally exhibited higher Antitumor activity than its regular polysaccharide. Previously, we extracted Se-containing tea polysaccharides (Se-TPS) from Se-enriched tea, and explored its structure and antioxidant activity. In this study, we investigated Antitumor activity of Se-TPS on sarcoma 180 (S-180), and compared with its regular polysaccharides TPS and dietary supplement Se-yeast. In vitro Antitumor activity of Se-TPS was evaluated by MTT and LDH assays, and the results indicated that Se-TPS can significantly inhibit the proliferation of S-180 in dose-dependent manner (R2=0.97, p<0.0001). In S-180 cancer xenograft model in Kunming mice, Se-TPS oral administration at three doses of 50, 100 and 200mg/kg body weight daily for 13days resulted in significant tumor regression. At the same dose, Se-TPS exhibited significantly higher Antitumor activity than TPS and Se-yeast. Importantly, Se-TPS can significantly increase the spleen and thymus indices of tumor-bearing mice, suggesting the safety and immunomodulatory activity of Se-TPS. Therefore, Se-TPS may be a desirable Antitumor agent for therapeutic and immunomodulatory applications.
Thomas E Wagner - One of the best experts on this subject based on the ideXlab platform.
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whole tumor cell vaccine with irradiated s180 cells as adjuvant
Vaccine, 2009Co-Authors: Jinhua Li, Ada V King, Sara L Stickel, Kelly E Burgin, Thomas E Wagner, Xinhai ZhangAbstract:Whole tumor cell vaccines have been widely studied and remain promising cancer immunotherapies. In the present study, we discovered that vaccination with irradiated mouse sarcoma S180 tumor cells stimulated robust Antitumor immunity to autologous tumor cells in both syngenic and allogenic mice. The Antitumor activity requires both T and B cells, but not NK cells. When a mouse lung carcinoma (TC-1) whole tumor cell vaccine was combined with the S180 vaccine, the Antitumor immunity against live TC-1 tumor cells is significantly enhanced compared to a TC-1 whole cell vaccine alone. This Antitumor immunity not only prevents live tumor challenge but also eradicates existing tumor cells. A similar phenomenon was also observed when S180 vaccine was combined with LL2 Lewis lung carcinoma tumor cells. Therefore, S180 vaccine may serve as an adjuvant for other whole tumor cell vaccines.
Hideaki Tahara - One of the best experts on this subject based on the ideXlab platform.
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therapeutic and specific Antitumor immunity induced by co administration of immature dendritic cells and adenoviral vector expressing biologically active il 18
Gene Therapy, 2002Co-Authors: Michael T Lotze, Fujie Tanaka, Wataru Hashimoto, Paul D Robbins, Hideaki TaharaAbstract:Interleukin-18 is a potent cytokine expressed early in the immune response following cleavage in activated composes. We have investigated the in vivo Antitumor effects of intratumoral (i.t.) administration of an adenoviral vector expressing biologically active murine interleukin (IL)-18 (Ad.PTH.IL-18). Substantial Antitumor effects were observed when established MCA205 fibrosarcoma was treated in syngeneic immunocompetent mice with intratumoral injection of Ad.PTH.IL-18 (P = 0.0025 versus control vector treatment), generating potent cytotoxic T lymphocytes (CTLs) in culture. In contrast, the Antitumor effect was absent, and cytotoxic activity was significantly less (P = 0.021) in gld mice (Fas ligand deficient). To enhance the in vivo Antitumor activity of the treatment using Ad.PTH.IL-18, we co-injected immature DC and Ad.PTH.IL-18 i.t. into established, day 7 MCA205 fibrosarcoma and MC38 adenocarcinoma. Co-injection of both Ad.PTH.IL-18 and DC was associated with complete abrogation of injected tumors. Furthermore, the Antitumor effects were also observed on distant tumors inoculated i.d. in the contralateral flank of the animal. The induced cytolytic activity was tumor-specific and MHC class I-restricted. As we have previously demonstrated in vitro (Tanaka F et al, Cancer Res 2000; 60: 4838–4844) and consistent with these findings in vivo, NK, T and dendritic cells coactivately mediate the IL-18 enhanced Antitumor effect. This study suggests that the coactivate strategy could be used in the clinical setting to treat patients with cancer.