Taechowisan, ThongchaiTipparat, SamsawatWinyou, PuckdeeWaya, S. Phutdhawong2020-10-162020-10-162020-06Taechowisan Thongchai, Tipparat Samsawat, Winyou Puckdee, Waya S. Phutdhawong. Cytotoxicity activity of geldanamycin derivatives against various cancer cell lines. Journal of Applied Pharmaceutical Science. 2020 Jun; 2020 Jun: 012-0212231-3354http://imsear.searo.who.int/handle/123456789/210764Geldanamycin (1) was isolated as a major compound from Streptomyces zerumbet W14. It was then used as a precursor tosynthesize two new geldanamycins: 17-(tryptamine)-17-demethoxygeldanamycin (2) and 17-(5′-methoxytryptamine)-17-demethoxygeldanamycin (3). The cytotoxicity activity of these two new compounds was evaluated and comparedwith the cytotoxicity of compound 1. Cytotoxicity activity was evaluated against a normal cell line, and three cancercell lines using an 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) colorimetric assay. Thesolubility of these compounds was also determined. The solubility of compounds 2 and 3 in water was 290.69and 348.18 µM, higher than that of compound 1 by about 1.91 and 2.29 times, respectively. Compounds 2 and 3showed moderate cytotoxic activity on Vero and human cervical carcinoma cells with IC50 values of >200.00 µg/ml. The strongest cytotoxicity of compound 3 was observed in human breast carcinoma cells (MCF-7) and humanhepatocellular carcinoma cell line (HepG2) cells with IC50 values of 82.50 and 114.35 µg/ml, respectively, while theIC50 values of compound 2 against MCF-7 and HepG2 cells were 105.62 and 124.57 µg/ml, respectively. The findingsshowed that these new geldanamycin derivatives exhibited selective cytotoxicity toward some cancer cells at a lowerconcentration. Therefore, future studies on these compounds could be useful for the management of some cancersAnticancer activitycancer cell linescytotoxicity activitysolubilitytryptamine-geldanamycin hybridsCytotoxicity activity of geldanamycin derivatives against various cancer cell linesJournal ArticleIndiaDepartment of Microbiology, Faculty of Science, Silpakorn University, Nakhon Pathom 7300, Thailand.Department of Microbiology, Faculty of Science, Silpakorn University, Nakhon Pathom 7300, Thailand.Department of Microbiology, Faculty of Science, Silpakorn University, Nakhon Pathom 7300, Thailand.Department of Chemistry, Faculty of Science Silpakorn University, Nakhon Pathom 7300, Thailand.