TY - JOUR AU - Gadad, Andanappa K.; Karki, Subhas S.; Rajurkar, Vikas G.; Bhongade, Bhoomendra A. TI - Synthesis and Biological Evaluation of 5-Formyl-6-arylimidazo(2,1-b)-1,3,4-thiadiazole-2-N-(dimethylaminomethino)sulfonamides as Antitumor Agents SN - 0004-4172 SN - 1616-7066 PY - 1999 JO - Arzneimittelforschung JF - Arzneimittelforschung LA - EN VL - 49 IS - 10 SP - 858 EP - 863 DA - 2011/12/28 KW - Antitumor agents KW - 5-Formyl-6-arylimidazo(2,1-b)-1,3,4-thiadiazole-2-N-(dimethylaminomethino) KW - sulfonamides, in vitro studies, synthesis AB - In search for potential anti cancer drug candidates in imidazo (2,1-b)-1,3,4-thiadiazole series, two series of 5-formyl-6-arylimidazo(2,1-b)-1,3,4-thiadiazole-2-N-(dimethylaminomethino) sulfonamides and 5-bromo-6-aryl/ethylacetateimidazo(2,1-b)-1,3,4-thiadiazole-2-sulfonamides were synthesised. All compounds showed significant cytotoxic effects (log10 GI50 < −4.0, log molar drug concentration required to cause 50% growth inhibition) against a variety of human tumor cell lines of the National Cancer Institute in vitro screen, including cells derived from solid tumors such as non-small cell lung, colon, central nervous system, melanoma, ovarian, prostate and breast cancer, and also few cell lines of leukemia and renal cancer. Introduction of a formyl group at the 5- and substituted aromatic group at 6-position generated compounds with potent antitumor activity. Incorporation of a bromo at 5- and ester group at 6-position produced compounds with reduced activity. PB - Editio Cantor Verlag DO - 10.1055/s-0031-1300515 UR - http://www.thieme-connect.de/products/ejournals/abstract/10.1055/s-0031-1300515 ER -