PHARMACOLOGICAL ACTIVITY OF LHT-17-19 IN CULTURES OF EGFR-EXPRESSING EPITHELIAL TUMORS

Kudryavtsev M.Yu., Tumutolova O.N., D. O.N., Epishkina A.A., Vavilova O.S., Gilevskaya Yu.S., B. E.V.
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引用次数: 1

Abstract

Abstract. . In the study, the pharmacological activity of the pyridine derivative LHT-17-19 was studied in relation to the culture of pancreatic cancer cells PANC-1 and the culture of bladder cancer cells HT-29 expressing the epidermal growth factor receptor. The cultures were obtained from the library of tumor strains of the Moscow Research Institute of Oncology. P.A. Herzen - a separate structural subdivision of the Federal State Budgetary Institution "NMITs Radiology" of the Ministry of Health of Russia. LHT-17-19 was synthesized in the Department of Chemistry, Technology of Synthetic Medicines and Analytical Control of JSC VNTs BAV (Russia). LHT-17-19 and the reference drug "Doxorubicin" 50 mg each were added to the cultivation medium in the concentration range from 10-8 to 10-v. Compounds LHT-17-19 were shown to be able to induce death and suppress the growth of pancreatic cancer squamous culture (PANC-1) and bladder (HT-29) tumor cells expressing EGFR over a wide range of concentrations. So for pancreatic cancer (PANC-1), the effective inhibitory concentration for the compound LHT-17-19 was 1.3 × 10-7 M, while for the reference substance doxorubicin it was 6.0 × 10-5 M. bubble (NT-29) - 2.4 × 10-7 M and 5.2 × 10-4 M, respectively.
lt -17-19在表达egfr的上皮肿瘤培养中的药理活性
摘要本研究研究了吡啶衍生物LHT-17-19在胰腺癌细胞PANC-1和表达表皮生长因子受体的膀胱癌细胞HT-29培养中的药理活性。培养物来自莫斯科肿瘤研究所肿瘤菌株文库。P.A. Herzen——俄罗斯卫生部联邦国家预算机构"NMITs放射学"的一个独立的结构分支。LHT-17-19由俄罗斯JSC VNTs BAV化学、合成药物技术和分析控制部门合成。将LHT-17-19和参比药“阿霉素”各加50 mg,浓度范围为10-8 ~ 10-v。化合物LHT-17-19被证明能够诱导死亡并抑制多种浓度表达EGFR的胰腺癌鳞状培养(PANC-1)和膀胱(HT-29)肿瘤细胞的生长。因此,对于胰腺癌(PANC-1),化合物LHT-17-19的有效抑制浓度为1.3 × 10-7 M,而对照品阿霉素的有效抑制浓度为6.0 × 10-5 M,泡(NT-29)分别为2.4 × 10-7 M和5.2 × 10-4 M。
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